Index

acceptors adenylate cyclase (continued) differentiation from NE receptor-coupled receptors 25 (continued) acetylcholine (ACh) & oxaprotiline enantiomers in brain 8 & carbamazepine 180 NE-sensitive y-acetylenic GABA & progabide 226 & bulbectomized rat 363-365 neurohumoral factors in Addison's disease regulation 6-7 & DST 247 & phospholipid matrix 6 adenosine triphosphate (ATP) & platelet a2-receptors 75 & message transmission 20 in platelets 334 adenylate cyclase protein constituents 4 & a2-adrenoceptors 66, 147 supersensitivity cholera toxin activation 293 & depressive reactivity 13 desensitization adenylate cyclase (continued) as homologous 5 as transducer 21 & DM1 + progabide 226 & 44 down-regulation adrenalectomy & DA receptors 290-294 & NE-sensitive adenylate as effector 4 cyclase 12 & 160 a2-adrenoceptors & G/F protein 289 & AD 67, 280 & guanine nucleotides 289 & adenylate cyclase 66 5-HT sensitive & affective disorders 55-64 & TCA 39 affinity states 77 & 1M1 mechanism of action in brain 69-73 22-29 & bulbectomy 360 Mg activation 292 conformation 79 NaF activation 293 & DA neuronal systems 59-62 NE receptor-coupled 3, 6-12 & ECT 145-158 & adenylate cyclase 6-12 & 1M1 145-158 & B-adrenoceptor 4, 6-12 molecular aspects of & 4 regulation 65-82 & corticosterone & NE release inhibition 65 & DM1 6, 8 in platelets 333-334 & ECT 4 presynaptic 'homologous' as autoreceptors 5 desensitization 9 regulation 65-82 & lesions 10, 12 storage effects 76

375 u2-adrenoceptors (continued) D-ala-D-leu-enkephalin subsensitivity 6 & u2-receptor binding 74 & TCA or MAOI 7, 253 alaproclate time course 79 activity 89 & TIQ 60 antihistamine vs antichol­ & 145-158 inergic activity 91 8-adrenoceptors block of mepyramine 89 81 vs 82 5 chronic treatment combination of mechanism of action 41 u2-adrenoceptor & 5-HT-2 receptors 43 & TCA or MAOI 7 high vs low affinity binding density 39-40, 94 & noradrenergic & 5-HT binding 33 subsensitivity 3 & 5-HT recognition site 301 desensitization & 5-HT uptake inhibition 36, & 5,7-DHT lesions 27 86 determination with & IMI binding 33 SH-dihydroalprenolol 3 NE vs 5-HT reuptake down-regulation inhibition 86-87 & action 5 QNB binding vs antichol­ & other CNS drugs 5 inergic activity 90 & ECT 145-158 & binding 33 & IMI 145-158 structure 36, 89 & NE receptor-coupled alprazolam adenylate cyclase 4 as AD 5 regulation vs IMI 342 & AD action 13 & adenylate cyclase 343-344 response vs IMI 343-344 & r, 11 & bulbectomized rat 362 & 5-HT input 12 & yohimbine binding 345-348 & yohimbine 145-158 vs IMI 345-348 adrenocorticotrophic hormone y-aminobutyric acid (GABA) (ACTH) actions 225 & stress 56 in brain affective disorders (also cf after bulbectomy 359-360 depression, mania) & brain 5-HIAA 227 & u2-adrenoceptors 55-64 & carbamazepine 179-180 & anxiety 267-274 & progabide 225 & carbamazepine 175-192 receptor agonists & DA receptors 55-64 as AD 225-232 E role 55-64 as antimanic 225-232 monoamine hypotheses receptor stimulation & IMI 23 & 5-HT neurons 227-228 aggression & mania 229-230 & carbamazepine 182-183 p-aminoclonidine (PAC) akinesia in u2-adrenoceptor studies tetrabenazine-induced 68-73 reversal by & u2-receptor binding 74, 75 oxaprotiline 122 binding assay 147

316 p-aminoclonidine (PAC) anticonvulsant(s) (continued) & 8-adrenoceptors 5 as partial a2-adrenoceptor carbamazepine 184 agonist 146, 147 antidepressant(s) (AD) (also of specific drugs & TCA) action on various receptors action 280 & 5-HT reuptake 85 as AD 258 & NE reuptake 85 in bulbectomized rat action of fluvoxamine 162 361-362 & a2-adrenoceptors 67, 78 vs oxaprotiline 319-330 & a2-adrenoceptor vs zimelidine 258 sub sensitivity 6 antihistamine activity 88-89 & cAMP 146 antihistamine vs antichol- carbamazepine 176, 183 inergic activity 91 & central a-receptors 146 block of mepyramine 88-89 & E reuptake 56 vs 206-207 233-240 & body weight 209 & 5-HT-1 receptor binding & cardiovascular effects cerebral cortex vs 210 hippocampus 39-43 & 5-HT receptors 135 & 5-HT-2 receptors 42-46, & 5-HT receptor 142 sub sensitivity 103-104 & 5-HT release 34 NE vs 5-HT reuptake & SP receptors 34 inhibition 86-87 & LSD binding 96 QNB binding vs antichol- mechanism of action 279 inergic activity 90 & 5-HT neurotransmission & sleep 277-284 35 & spiperone binding 136 receptor-receptor inter­ as twitch inhibitor 96 actions 301-318 & receptors 332 & spiperone binding 140 & neuroendocrines 49-51 oxaprotiline & brain cGMP 116 vs amitriptyline 319-330 hyperactivity & regulatory mechanisms 22 & bupropion 199 response & carbamazepine 179 & 5-HT receptors 33-54 & locomotor activity 116 & 1M1 binding sites 33-54 amygdala screening models 197-198 a2-receptor binding 72 & serotonergic receptor anorexia nervosa mechanisms 93-108 & DST 247 & serotonergic anticholinergic activity super-sensitivity 99 & AD 280 & sleep 275- 286 vs antihistamine activity 91 & spiperone-Iabeled 5-HT & carbamazepine 183 receptors 135-143 correlation with anti- subsensitivity of NE adeny­ histaminic activity 91 late cyclase 6-12 vs QNB binding 90 & down-regulation of structural factors 89-91 8-adrenoceptors 6-12

377 antidepressant(s) (AD) avoidance learning (continued) & 5-HT inhibition 95 therapy long term 102-104 & noradrenergic signal transfer 3-17 baclofen & noradrenergic & bulbectomized rat 363-365 sub sensitivity 3 barbiturates reducing NE signal transfer & 8-adrenoceptors 5 4-6 & cGMP 116 zimelidine 257-259 & DST 247 vs amitriptyline 258 & locomotor activity 116 antihistamine(s) benzodiazepine(s) activity of oxaprotiline & 8-adrenoceptors 5 enantiomers 128 benzodiazepine-GABA complex activity of various compounds & carbamazepine 180 88-89 benzodiazepine-receptor 267 vs anticholinergic activity & brain cGMP 116 91 & locomotor activity 116 & 8-adrenoceptors 5, 87 bicuculline structural factors 88-89 & progabide 229 anxiety binding & affective disorders assay technique 68-89 267-274 biogenic amine biological factors 269-271 hypothesis 196-197 & depression 268-269 bovine polypeptide (BPP) & DST 270 & respiration 311 & lactate 267, 269-271 brain (also of specific areas & pharmacological response 271 species) & REM latency 270 & a2-adrenoceptors 67-79 anxiolytic action in bovine 72 of carbamazepine 182-183 in human 72 apomorphine (Apo) areas apomorphine-induced circling in bulbectomized model of & SKF 64139 60-61 depression 367 & SKF 72223 60-61 brain-stem & brain cGMP 116 CA neurons & DA formation of cAMP 291 & estradiol 11 & locomotor activity 116 motor nuclei arginine vasopressin (AVP) & 5-HT 95 & carbamazepine 181 serotonergic atropine super-sensitivity 99 anticholinergic activity 131 brompheniramine autoreceptor(s) as antihistamine 87 presynaptic 146 antihistamine activity 88-89 as presynaptic antihistamine vs antichol- a2-adrenoceptors 5 inergic activity 91 avian pancreatic polypeptide block of mepyramine 88-89 (APP) as 5-HT & respiration 311-312 86 & clonidine 311

378 brompheniramine (continued) butyrophenones NE vs 5-HT reuptake inhibi­ & a-adrenoceptors 5 tion 86-87 pharmacological properties calmodulin 86 & DA 293 QNB binding vs antichol­ as regulatory protein 290 inergic activity 90 cancer bulbectomized rat & DST 247 behavioral changes 357-359 carbamazepine behavior in open field as AD 176 361-366 in affective illness 175-192 & amitriptyline 361 as anticonvulsant 178, 184 & psychotropic drugs & clonidine 178 361-366 & 6-0HDA 178 brain areas involved 367 vs yohimbine 178 changes in neurotransmitters as antimanic 176, 177 359-361 behavioral pharmacology hypothermia 358 182-183 & 362 & cAMP 180 as model of depression & cGMP 180 357-372 cholinergic effects 180 & sleep 358 & cognitive function 181 & various drugs 362-366 combination with 177 bupropion combination with neuroleptics as AD 5, 58 177 & amphetamine 199 & corticoid circadian rhythm & animal models of AD 181 activity 198-199 CSF levels 176 & body weight 209 & dexamethasone suppression vs amitriptyline 209 181 clinical profile 199-214 & diabetes 181 vs amitriptyline 206-207 dopaminergic mechanisms vs TCA 205-207 178-179 convulsant activity 211 & DST 247 drug dependence 211-214 endocrine effects 180-182 formula 198 formula 177 vs 1M1 & GABA 179-180 cardiovascular effects 209 metabolite 177 neurochemistry 214-219 & MHPG sulfate 178 & presynaptic DA receptors NE effects 177-178 58-59 neurophysiological mechanisms review 195-224 183-185 side-effects 208-211 & opiate system 182 structure 198 & pain 175 vs TCA & PRL 179 cardiovascular effects 210 & seizures 175 as Wellbutrin 208 serotonergic effects 179 y-butyrolactone (GBL) & somatostatin 182 & DOPA synthesis 59 & trigeminal neuralgia 175

379 carbamazepine-l0, ll-epoxide cholecystokinin (CCK) as anticonvulsant 177 CCK-4 as carbamazepine metabolite & spiperone binding 177 311-312 catecholamine(s) (CA) (also cf CCK-8 specific compounds) & spiperone binding hypothesis of affective dis­ 311-312 orders 320 choline weakness 29 in brain reuptake & carbamazepine 180 & 1M1 23 cholinergic catechol O-methyltransferase neuronal system & affective disorders 320 & central E 57 caudate nucleus a2-receptor binding 72 & spiperone binding 36, 45, cerebral cortex 136, 140 & AD treatment 33 cingulate gyrus 5-HT receptors q3 & 5-HT nerve cells 34 & 1M1 binding 24, 26 a2-receptor binding 72 & bulbectomized rat 363-365 spiperone binding 37, 48-49 as 5-HT reuptake inhibitor & 5-HT nerve terminals 37 86 cerebrospinal fluid (CSF) clenbuterol & carbamazepine 180 & NE receptor-coupled adeny­ carbamazepine 176 late cyclase 4 cCAMP & carbamazepine 180 antihistamine activity 89 E 56 antihistamine vs antichol- in depressed patients 58 inergic activity 91 GABA block of mepyramine 89 & carbamazepine 180 vs fluvoxamine 163-164 5-H1AA & 5-HT reuptake 85 & zimelidine 256 & NE 85 HVA NE vs 5-HT reuptake inhibi­ & carbamazepine 179 tion 86-87 & zimelidine 256 in vivo 86, 253 MHPG QNB binding vs antichol­ & carbamazepine 178 inergic activity 90 & zimelidine 256 receptor affinity 235 NE vs other drugs 235 & carbamazepine 178 & spiperone binding 140 somatostatin clonazepam & carbamazepine 182 as antimanic 184 clonidine & bulbectomized rat 362 in az-adrenoceptor studies as neuroleptic 179 68, 74 cholera toxin binding assay 147 adenylate cyclase activation & carbamazepine 178 293 380 clonidine (continued) coupler protein clonidine-induced in message transmission 20, hypoactivity 21 reversal by oxaprotiline Cushing's disease 125 & DST 247 clonidine-induced hypothermia cyclase reversal by oxaprotiline assay technique 68-69 124 cyclic adenosine monophosphate & DOPA synthesis 59-60 (cAMP) & firing of DA cells 61 & calmodulin 290 & -induced & carbamazepine 180 behavior 60 formation hypotensive response 333 5-HT stimulated 41, 44 as partial a2-adrenoceptor & zimelidine 44 agonist 146, 147 & protein kinases 4 as partial DA agonist 60 response to NE & plasma MHPG 333 sex differences 12 platelet binding as second messenger 4 depressed vs controls cyclic AMP phosphodiesterase 349-350 & calmodulin 290 & a2-receptor subsensitivity cyclic guanosine 3', 5' -mono- 333 phosphate (cGMP) clorgyline assay 110 as MAO-A I 7 & carbamazepine 180 & NE receptor 7, 9 cerebellar levels cocaine & diclofensine 114-116 & B-adrenoceptors 5 & 114-116 hyperactivity time course 117 & carbamazepine 179 & locomotor activity 110 corticoid(s) (also of specific compounds) & DST 247 circadian rhythm cytoplasmic receptors & carbamazepine 181 for steroids 11 coexistence (of neuro­ modulators) technique deprenyl 303-306 as MAO-B I 7 cognitive function & NE receptor 7, 9 & carbamazepine 181 depression & phenytoin 181 abnormal 5-HT vs NE conditioned avoidance response metabolism 55 (CAR) & brain CA 145 & 5-MeO-DMT 39 bulbectomized rat as model corpus striatum 357-372 & IMI binding 24 CSF E 58 corticosterone pharmacotherapy 253-265 & 5-HT mechanism 49 & platelet a2-adrenoceptors & NE-sensitive adenylate 331-356 cyclase 12 & sleep 275-277 cotransmitter function desensitization cotransmitter-receptor mechanism 9 interaction 22 381 desmethylimipramine (DM1) diazepam action on various receptors & bulbectomized rat 363-365 280 dibenzepine as AD 258 & spiperone binding 140 vs zimelidine 258 as twitch inhibitor 96 chronic treatment diclofensine & 5-HT receptors 42-43, as AD 109 93-108 & brain 5-H1AA 112 mechanism of action 41 & cerebellar cGMP 114-116 & down-regulation of time course 117 B-adrenoceptors 6-7, as clinical AD 117 11 & DA uptake inhibition 109 high vs low affinity binding high affinity uptake 39-40, 94 compared to nomifensine & 5-HT binding 33 110-113 & 5-HT receptors 135 & 5-HT uptake inhibition 109 & 5-HT uptake inhibition 36 metabolites & hyperactivity 129 & monoamine uptake 113-114 & 1M1 binding 33 structures 114 & locus coeruleus lesions 7 & transmitter uptake 114 & melatonin stimulation 12 & NE uptake inhibition 109 & NE-sensitive adenylate neurochemical effects cyclase 6 , 8 109-120 NE vs 5-HT reuptake =Ro 8-4650 109 inhibition 86-87 diethylstilbesterol 6-0HDA 7 & DST 247 QNB binding vs antichol­ dihydroalprenolol (DBA) inergic activity 90 binding receptor affinity 235 assay 147 vs other drugs 235 & DM1 11 & sleep 281 & effects of lesions 10 & spiperone binding 33, 46, & MAO-A vs MAO-B inhibition 136, 140 9 structure 36 & oxaprotiline 127-128 dexamethasone & determination of B-adreno­ suppression ceptors 3 & carbamazepine 181 & a2-receptor binding 74 suppression test (DST) (DHEC) 241-250 & a2-receptors 78 & anxiety 270 5,7-dihydroxytryptamine interferences 246-248 (5,7-DHT) interpretation 242-244 & DM1 regulation of B-adreno­ rationale 241 ceptors 7, 9, 10 uncertain applications & 1M1 binding 24, 26 244-246 lesions diabetes & B-adrenoceptor & carbamazepine 181 desensitization 27 & DST 247 & progabide 226 & lithium 181 Dilantin - cf phenytoin

382 DOPA (e) (continued) accumulation receptor affinity 235 & progabide 229 vs other drugs 235 movements as twitch inhibitor 96 & progabide 230 potentiation electrocardiogram (ECG) & bupropion 199 & fluvoxamine 161, 162 synthesis electroconvulsive shock (ECS) & GBL 59 & brain Q2-adrenoceptors (DA) 145-158 & affective disorders & brain B-adrenoceptors 219-220 145-158 & AMPT 60 & brain receptors & calmodulin 293 sequential effects 153 formation of cAMP 291 & carbamazepine 184 neuronal systems 58-59 & DBA binding 153 & a2-adrenoceptors 59-62 & noradrenergic effect of bupropion 58-59 sub sensitivity 146 non-inhibition by fluvoxamine treatment 148 160 electroconvulsive (shock) receptors therapy (ECT) & affective disorders & down-regulation of B-adren­ 55-64 oceptor density 1-3 desensitization 289-300 & NE receptor adenylate in striatum 289-300 cyclase 3, 4 subtypes 289 in treatment of depression uptake 146 & bupropion 219 electroencephalogram (EEG) uptake inhibition & sleep monitoring 275, by diclofensine 109 281-284 by nomifensine 109 epinephrine (E) dopaminergic as Q2-adrenoceptor agonist antagonism 146 & carbamazepine 141 in affective disorders 55-64 mechanisms & cholinergic neuronal system & carbamazepine 178-179 57 Doriden - cf glutethimide & oxotremorine 57 down-regulation in CSF 58 & differentiation of epinephrine-neuronal systems receptors from acceptors 55-58 25 localization in brain 55-56, doxepin(e) 57 antihistamine activity 88-89 & MAOI 58 antihistamine vs antichol­ & MAO inhibition 56 inergic activity 91 & PGE, stimulation 76 block of mepyramine 88-89 primate vs rat brain 56 QNB binding vs antichol­ & a2-receptor binding 75 inergic activity 90 reuptake & AD 56 & stress 56-57

383 epinephrine (E) (continued) fluvoxamine (continued) turnover clinical effects (continued) & nicotine 57 as AD 161-171 & scopolamine 57 comparison to clomipramine ergot alkaloids (also cf 163- 164 specific compounds) comparison to 1M1 165 affinity for a2-receptors 78 dosage 171 estradiol formu la 159 & brain-stem CA neurons 11 & 5-H1AA 160 estrogens & 5-HT reuptake inhibition & DST 247 160 ethanol & H 75/12 160 & cGMP 116 & H 77/77 160 & locomotor activity 116 lack of anticholinergic withdrawal effects 160 & DST 247 lack of antihistamine effects 160 fluoride metabolism 161 adeny1ate cyclase activation sleep effects 161 293 & muscarinic receptor 160 f1uoxetine =Myroxim 170 as AD 237, 233-240 as non-DA uptake inhibitor clinical efficacy 238 160 vs 1M1 237 as non-NE uptake inhibitor & B-adrenoceptors 5 160 chronic treatment & pargyline 160 & receptors 236-238 pharmacokinetics 161 as 5-HT uptake inhibitor 5, & prolactin 160 86, 233 & B-receptors 160 metabolism 236 & reserpine 160 & NE receptor-coupled review 159-173 adenylate cyclase 5 structure 159 receptor affinity 235 & tetrabenazine ptosis 160 vs other drugs 235 tolerance 165-167 & spiperone binding 45 frontal cortex uptake inhibition specificity spiperone-labeled 5-HT 234 receptors vs nisoxetine 234 & AD 135-143 B-flupenthixol & bulbectomized rat 362 GABA - cf y-aminobutyric acid fluvoxamine glaucoma as AD 159 & TCA 254 & adeny1ate cyclase 160 glutethimide animal pharmacology 160-161 =Doriden 247 anticholinergic effects & DST 247 166-169 G protein - cf guanine nucleo­ cardiovascular effects tide regulatory protein 167-170 GTP binding protein (G/F clinical effects 161-170 protein)

384 GTP binding protein (G/F hippocampus (continued) protein) (continued) a2-receptor binding 72 & GDP concentration 22 histaminergic & GTP concentration 22 receptors & message transmission 20, & AD 280 21 & TCA 253 guanine nucleotide regulatory homovanillic acid (HVA) protein (G protein) (N brain protein) & nomifensine 113 & adenylate cyclase 289 CSF & coupling to cyclase 4 & carbamazepine 179 & NE signal transfer 12 hormones (also cf compounds & & a2-receptor 147 groups) guanosine diphosphate (GDP) & NE regulation 11 & a2-adrenoceptor 66-67 & NE-sensitive adenylate & G/F protein 20, 22, cyclase 11-12 289-290 6-hydroxydopamine (6-0HDA) guanosine triphosphate (GTP) & carbamazepine 178 & a2-adrenoceptor 66-67, 147 lesions & G/F protein 20, 22, & 1M1 action 24 289-290 5-hydroxyindole acetic acid guanyl-5'-yl imidophosphate (5-H1AA) (GMP-PNP) brain in a2-adrenoceptor studies & carbamazepine 179 68 & diclofensine 112 & fluvoxamine 160 H 22/54 - cf a-pro­ & GABA 227 propyldopacetamide & nomifensine 112 H 75/12 & progabide 227 & 5-HT uptake 5-hydroxytryptophan (5-HTP) & fluvoxamine 160 & head twitch 95 & NE uptake & progabide 229 & fluvoxamine 160 as 5-HT precursor 95 H 77/77 hyperactivity & 5-HT uptake & DM1 129 & fluvoxamine 160 & oxaprotiline enantiomers & NE uptake 128-129 & fluvoxamine 160 hypophysectomy haloperidol & NE-sensitive adenylate haloperidol-induced behavior cyclase 12 drug potentiation 60 hypopituitarism spiperone binding 136, 140 & DST 247 Hamilton Depression Rating hypothalamus Scale & oxaprotiline E 56, 57 enantiomers 132-133 & 1M1 binding 24, 48 hippocampus NE 57 & 5-HT nerve cells 34 a2-receptor binding 72 5-HT supersensitivity 104 hypothermia & 1M1 binding 24, 26 clonidine-induced & 5-HT reuptake 27-28 reversal by oxaprotiline 124-125 385 (IM1) imipramine (IM1) (continued) action on receptors 22 down-regulation of ad reno­ as AD ceptors vs alprazolam 342 & 5-HT axon terminals vs fluoxetine 237 25-27 & adenylate cyclase 343-344 vs fluvoxamine 165 vs alprazolam 343-348 high affinity binding 24-25 anticholinergic activity 131 & 5,7 DHT lesions 24 antihistamine activity 89, & 6-0HDA 24 131 high vs low affinity binding antihistamine vs anti­ 39-40 cholinergic activity & 5-HT binding 33 91 & 5-HT receptors 135 anti 5-HT activity 131 & 5-HT uptake inhibition binding 36 to brain sections 313 imipramine-positive brain & 5,7-DHT lesions 26 areas 314 to "hi ppocampal membranes mechanism of action 22-29 26 & monoamine hypotheses of & 5-HT uptake mechanisms affective disorders 25 230 technique 304 NE vs 5-HT reuptake binding sites 301 inhibition 86-87, 253 & AD response 33-54 QNB binding vs anticholin­ in brain areas 46-49 ergic activity 90 multiplicity 25 receptor affinity 235 in platelets 333 vs other drugs 235 & reserpine 33 & reuptake of CA 23 block of mepyramine 89 & reuptake of 5-HT 23 & brain ~2-adrenoceptors & spiperone binding 33 145-158 structure 36, 89 & brain B-adrenoceptors & transsynaptic mechanisms 145-158 19-31 cardiovascular effects & yohimbine binding 345-348 vs bupropion 209 vs alprazolam 345-348 vs TCA 210 immunohistochemistry chronic treatment techniques 302-303 & head twitch 97 indomethacin & high vs low affinity & DST 247 binding 94 infections & 5-HT binding 39, 42 & DST 247 & 5-HT receptor activity ion gate 93 & transducer 20 & 5-HT receptors 42, 93-108 & 5-HT receptors 135 mechanism of action 41 & NE receptor-coupled adenyl­ & spinal 5-HT binding ate cyclase 4 sites 102 as non-blocker of NE uptake 7 & noradrenergic innervation of cortex 7 386 iprindole (continued) mania QNB binding vs antichol­ & carbamazepine 176, 184 inergic activity 90 & clonazepam 184 & spiperone binding 140 & GABA receptor stimulation isoproterenol 229-230 & DA formation of cAMP 291 & progabide 230 isoreceptor & valproic acid 184 interconversion 302 isozimelidine (=E-zimelidine) as AD 258 antihistamine activity 88-89 vs zimelidine 258 block of mepyramine 88-89 antihistamine activity 89 NE vs 5-HT reuptake antihistamine vs antichol- inhibition 87 inergic activity 91 block of mepyramine 89 lactate & hyperactivity 129 & anxiety 267, 269-271 NE vs 5-HT reuptake light-evoked responses inhibition 86-87 & 5-HT 104 QNB binding vs anticholin­ lipids ergic activity 90 membrane median forebrain bundle (MFB) & phospholipase A2 21 & 5-HT nerve cells 34 lithium medullectomy & B-adrenoceptor-sensitive & NE-sensitive adenylate adenylate cyclase 5 cyclase 12 & carbamazepine 177 melatonin & diabetes 181 stimulation locomotion & DM1 12 & 5-HT excitation 95-101 membrane receptors locus c(o)eruleus & adenylate cyclase 4 E 56, 57 & neurohormone action 3-4 NE 57 meprobamate LY 51641 & DST 247 as AD 58 mepyramine as MAO A inhibitor 58 block, by various compounds & central E 58 88-89 LY 141865 messenger RNA (mRNA) & DA formation of cAMP 291 & regulation of NE signal 11 formula 291 methaqualone lysergic acid diethylamide & DST 247 (d-LSD) =Quaalude 247 binding 5-methoxy-N,N-dimethyltryptamine & AD 96 (5-MeO-DMT) & spiperone binding 36, & CAR inhibition 39 135-136 & AD 39 head twitch 95-104 magnesium & DM1 93 adenylate cyclase activation & 1M1 93 292 & zimelidine 93 mammilary bodies a2-receptor binding 72 387 N-dimethyltryptamine mitral valve prolapse (5-MeO-DMT) (continued) & anxiety 271-272 hyperactivity 100 monoamine oxidase (MAO) & IMI 101 & effective disorders 320 & zimelidine 100-101 inhibition & tail flick 101 & E 56 3-methoxy-4-hydroxymandelic in platelets 333 acid (VMA) monoamine oxidase inhibitors from MHPG 321 (MAOI) 3-methoxy-4-hydroxyphenyl­ & AD decreases in receptor ethyleneglycol (MHPG) number 6 & affective disorders & B-adrenoceptors 7 320-321 MAO-A vs MAO-B effects 7, & oxaprotiline 319-330 9 & progabide 226 & central E 58 3-methoxy-4-hydroxypheny­ & 5-HT binding sites 94 lethyleneglycol sulfate MAO-A inhibitors (MOPEG-S0 4 ) & central E 58 brain & NE receptor-coupled adeny­ & nomifensine 113 late cyclase 4 & progabide 226 & sleep 284 & carbamazepine 178 multineuromodulator a-methyl-p-tyrosine (AMPT) storage 302 & DA antagonists 60 multitransmitter methyprylon storage 302 & DST 247 muscarinic receptors =Noludar & TCA 253 Myroxim - cf fluvoxamine anti 5-HT activity 131 & bulbectomized rat 363-365 naloxone mianserin(e) & a2-receptor binding 74 antihistamine vs antichol- neuralgia inergic activity 91 trigeminal & a2-blocking 151 & carbamazepine 175 & bulbectomized rat 362-365 neuroendocrines (also cf & 5-HT receptors 135 specific compounds) & NE receptor-coupled & AD 49-51 adenylate cyclase 4 neurohormone (also see specific NE vs 5-HT reuptake hormones) inhibition 86-87 & membrane receptors 3-4 in vivo 19-31 neuroleptics (also cf specific QNB binding vs anticholin­ drugs) ergic activity 90 & progabide 230 receptor affinity 235 neuropeptide Y (NPY) vs other drugs 235 & blood pressure 311 & B-receptors 151 NG 108-15 cells & spiperone binding 137-142 & a2-adrenoceptors 67, as twitch inhibitor 96 73-79, 154 & E 154 preparation 68

388 nicotine norepinephrine (NE) (continued) & E turnover 57 as Q2-adrenoceptor agonist nisoxetine 146 & uptake inhibition in brain regions 57 vs fluoxetine 234 in cortex Noludar - cf methyprylon after bulbectomy 359 nomifensin(e) desensitization as AD 109 & oxaprotiline 125-127 antihistamine activity 89 & down-regulation of adeny­ antihistamine vs anticholin- late cyclase 6-7 ergic activity 91 effects of carbamazepine block of mepyramine 89 177-178 & brain cGMP 116 neuron tolerance time course 117 & progabide 226 & brain 5-H1AA 112 non-inhibition by fluvoxamine & brain HVA 113 160 & brain MOPEG-S04 113 & progabide 226 & bulbectomized rat 362-365 receptors & cerebellar cGMP 114-116 down-regulation by TCA 279 & DA uptake inhibition 109 release inhibition high affinity uptake compared by Q2-adrenoceptors 65 to diclofensine reuptake 110-113 & AD action 85 as isoquinoline 109 reuptake inhibition & locomotor activity 116 vs 5-HT reuptake inhibition & monoamine release 109 86-88 & NE uptake inhibition 109 in telencephalon NE vs 5-HT reuptake inhibi- after bulbectomy 359 tion 86-87 uptake QNB binding vs anticholin­ & TCA 253 ergic activity 90 uptake inhibition & spiperone binding 140 by diclofensine 109 as twitch inhibitor 96 by nomifensine 109 noradrenergic activity action on various receptors & AD 280 280 "noradrenergic hypothesis" as metabolite of amitripty­ 146 line 278 properties & sleep 277-281 of oxaprotiline 122-128 as twitch inhibitor 96 signal transfer norzimelidine & AD therapy 3-17 as active metabolite 96 subsensitivity antihistamine activity 89 after ECS 146 block of mepyramine 89 subsensitivity after AD 3 lack of sedative action 85 & B-adrenoceptor density 3 NE vs 5-HT reuptake synapses inhibition 86-88 & 1M1 22 QNB binding vs anticholin­ norepinephrine (NE) ergic activity 90 & AD 55 pharmacokinetics 256

389 N protein - cf guanine nucleo­ pain tide regulatory protein & carbamazepine 175 NSD 1015 & chronic AD treatment as decarboxylase inhibitor 102-104 228 sensitivity & DOPA synthesis 59 & zimelidine 102 transmission 101 opiate systems pargyline & carbamazepine 182 & central E 58 Org 4360 & fluvoxamine 160 & bulbectomized rat 363-365 as MA01 58 Org 5859 & spiperone-labelled 5-HT & bulbectomized rat 363-365 receptors 135 Org 6582 pancreatic polypeptides (PP) ­ & bulbectomized rat 362-365 cf individual compounds ovariectomy (311) & 1M1 decrease in 5-HT recep­ Parkinson's disease tors 142 & nigro-striatal DA pathway oxaprotiline 289 as AD 5, 122, 319-330 pentylenetetrazole vs amitriptyline 319-330 & cGMP 116 & NE 6 & locomotor activity 116 & urinary MHPG 319-330 as anticholinergic 131 & DOPA synthesis 59 as antihistamine 128, 131 pheniramine(s) (also cf as anti 5-HT 131 specific compounds behavioral & neurophysio- antihistamine activity 88-89 logical studies block of mepyramine 88-89 122-123 & 5-HT reuptake 86 & DHA binding 127-128 & NE reuptake 86 enantiomer differences 6-9, phentolamine 121-134 as a-adrenergic antagonist & Hamilton Depression Rating 78 Scores 132-133 affinity for a2-receptor 78 & hyperactivity 128-129, 130 phenylethanolamine N-methyl- & NE desensitization 125-127 transferase (PNMT) & NE receptor-coupled adenyl- antiserum 55 ate cyclase 4, 8 localization in brain 55-56 neurobiochemical effects 127 primate vs rat brain 56 noradrenergic properties phenytoin 122-128 & cognitive function 181 reversal of reserpine =Dilantin 247 hypothermia 122 & DST 247 sedative-antiaggressive pro­ phospholipid(s) perties 128 matrix oxotremorine & adenylate cyclase 6 & central E 57 phospholipase A2 oxymetazoline & membrane lipids 21 in az-adrenoceptor studies phosphorylation 69 cascade 390 phosphorylation (continued) 3-PPP cascade (continued) & DA formation of cAMP 291 & noradrenergic signal formula 291 transfer 12-13 prazosin(e) of membranes & a2-receptor binding 74 in desensitized striatal & spiperone binding 140 slices 294-296 pregnancy & neurotransmission 290 & DST 247 & sulpiride 294 progabide picrotoxin as AD 225 & reversal of progab ide TH AD action 228 effect 229 &monoamine changes 228-229 as neuroleptic 179 & bicuculline 229 piperoxane & brain 5-H1AA 227 & firing of DA cells 61 & brain MHPG 226 & brain MOPEG-SO~ 226 as AD 142 & 5, 7-DHT lesions 226 & spiperone binding 140, 141 & L-DOPA movements 230 platelet(s) formula 225 adenylate cyclase 334, 335 as GABA receptor agonist 225 a-adrenoceptor 33-334 & 5-HT 227-228 & 5-HT transport 333 & 5-HTP twitches 229 & 5-HT uptake & mania 230 & fluoxetine 234 & NE 226 & nor-fluoxetine 234 & NE adenylate cyclase 226 human NE neuron tolerance 226 & a2-adrenoceptors 67-79 & neuroleptics 230 & 5-HT uptake 234 & reserpine ptosis 226 1M1 binding sites 333 =SL 76,002 225 & MAO 333 & tardive dyskinesia 230 as monoaminergic neuron & TH 229 models 333 & picrotoxin 229 & PG1 2-adenylate cyclase up-regulation of 5-HT-2 338-339 receptors 228 preparation 335 progesterones a2-receptor binding 335-336 & DST 247 a2-receptors 67-79, 154, prolactin (PRL) 331-356 & carbamazepine 179 & adenylate cyclase 75 & fluvoxamine 160 storage effects 76 & 5-HT mechanism 49-51 yohimbine binding 340 & zimelidine 160 pons a2-receptor binding 72 & 8-adrenoceptor density 5, Posolt behavioral despair model 13 & bupropion 199 as depressant 5 potassium & NE-sensitive adenylate channels cyclase 5 & 5-HT binding sites 41

391 a-propyldopacetamide receptor-receptor interactions =H 22/54 304 & AD 301-318 as hydroxylase REM inhibition 304 latency prostaglandin El (PGEl) & an xiety 270 & az-receptors 76 & depression protein kinase(s) & MA01 284 & cAMP 4 renal failure in striatal DA receptor & DST 247 desensitization 297 reserpine ptosis & B-adrenoceptor density 5, non-reversal by fluvoxamine 13 160 & brain cGMP 116 & progabide 226 & bulbectomized rat 363-365 reversal by oxaprotiline 122 as depressant 5, 55 putamen 5-HT depletion a2-receptor binding 72 & fluvoxamine 160 pyrilamine hypothermia antihistamine activity 131 reversal by oxaprotiline 122-123 Quaalude - cf methaqualone & 1M1 binding 33 quinuclidinyl benzylate (QNB) in various brain areas 48 receptor binding & locomotor activity 116 vs anticholinergic activity as monoamine depleter 55 90 & NE-sensitive adenylate cyclase 5 as sedative 55 as az-adrenoceptor antagonist Ro 4-1284 68-73, 146 & fluvoxamine 160 binding assay 147 Ro 8-4650 - cf diclofensine & aZ-receptor binding 74, Rolipram 75, 147 as phosphodiesterase inhibi­ receptor(s) (also cf specific tor 44 receptors & classes) & action of TCA 279 salbutamol & AD 146 as B-agonist 362 adrenergic & bulbectomized rat 362 & AD action 332 schizophrenia subsensitivity 332 & dopaminergic receptor 289 & TCA 332 scopolamine differentiation from & E turnover 57 acceptors 25 second messenger az-receptor generating enzymes & adenylate cyclase 147 & transducer 20 affinity states 147 & noradrenergic information conformation 151 flow 4 supersensitivity 146 sedative B-receptor properties of oxaprotiline & fluvoxamine 160 enantiomers 128

392 seizures (S-HT) (continued) & carbamazepine 175 & progabide 227-228 serotonergic receptor affinity effects & AD 280 of carbamazepine 179 receptors receptor mechanisms & AD response 33-54 & AD 93-108 regional variation 33-54 receptors & substance P 301 & TCA 253 receptor sub sensitivity & AD 280 & amitriptyline 103-103 synapses & zimelidine 103-104 & 1M1 22 receptor types 94 serotonin (5-HT) effect of chronic treat­ AD 55 ment 94 & up-regulation or down­ reuptake regulation of neuro­ & 1M1 23, 27-28 transmission 33, 34 reuptake inhibition assay 304 vs NE reuptake inhibition axon terminals 86-88 & 1M1 down-regulation of selective reuptake inhibi­ adrenoceptors 25-27 tors 85-92 binding & tail flick 101 & chronic drug treatment transport 41, 42 by platelets 333 & K channels 41 turnover, in brain bulbospinal pathways 101 after bulbectomy 359 & cAMP formation 41, 44 uptake co-storage with substance P & TCA 253 302 uptake i nhi bi t i on 5-HT-1 receptor binding by diclofensine 109 cerebral cortex vs by fluvoxamine 160 hippocampus 39-43 sex 5-HT-2 receptors differences & chronic AD treatment in cAMP response to NE 12 42-46 signal transfer & progabide 228 & AD ac tion 85 as regulatory sites 94 noradrenergic 5-HT-1 vs 5-HT-2 receptors & AD therapy 3-17 36-38 & 5-HT axon lesion 27 inhibition by fluoxetine 5 & mRNA 11 & light-evoked responses 104 neurobiological implica- neuron pathways 34 tions 12-13 & AD action 35 & phosphorylation cascade & SP-like immunoreactivity 12 34 reduction by AD 4-6 & TRH-like immunoreactivity SKF 38393 34 & DA formation of cAMP 291 neurons formula 291 & GABA receptor stimulation 227-228

393 SKF 64139 stress & Apo-induced circling 60-61 & ACTH 56 as DA antagonist 60 & brain cGMP 115-116 and DOPA synthesis 59 & E 56-57 & clonidine 59 striatum & pergolide 59 & adenylate cyclase & haloperidol-induced down-regulation behavior 60 290-294 SKF 72223 DA receptor desensitization & Apo-induced circling 60-61 289-300 as DA antagonist 60 Mg++ activation of adenylate & DOPA synthesis 59 cyclase 292 & clonidine 59 & phosphorylation of membrane & pergolide 59 proteins 294-296 & haloperidol-induced substance P (SP) behavior 60 & AD action 34 SL 76,002 - cf progabide co-storage with 5-HT 302-312 sleep as 5-HT comodulator 101 & AD 275-286 & 5-HT receptors 301 & amitryptyline 277-281 receptors & depression 275-277 & 5-HT binding sites & EEG monitoring 275 301-318 & fluvoxamine 161 substance-like immuno­ & nortriptyline 277-281 reactivity 34 stages 275 & 5-HT system 34 variables 276 substantia nigra spinal cord DA cells a2-receptor binding 72 & clonidine 61 spiperone & piperoxane 61 binding a2-receptor binding 72 & AD 94, 96 sulpiride & DMI 46 & bulbectomized rat 362 effect of various drugs as D-2 receptor antagonist 136, 140 294 & fluoxetine 45 & membrane phosphorylation technique 135-136 294 & TIQ 60 'super-high' affinity state & zimelidine 45 description 75 binding sites 36 synapse as regulatory sites 39 plasticity 20 receptor autoradiography synaptic transmission 36-39 mechanism 28-29 spiperone-labeled 5-HT schematic 315 receptors systolic pressor response & AD 135-143 & AD 332 steroid hormones (also cf hormones & specific tail flick compounds) from 5-HT inhibition 95 & NE regulation 11 as measure of pain 101 & zimelidine 101

394 tardive dyskinesia antidepressants (TCA) & progabide 230 (also cf antidepressants and telencephalon specific drugs) & 1MI binding 48 & adrenergic receptors 332 tetrabenazine & 6-adrenoceptors 7 & fluvoxamine 160 as 88-89 ptosis 160 atropine-like side effects sedation 254 & bupropion 198-199 vs bupropion 205-207 tetrahydroisoquinolines (T1Q) ­ cardiovascular effects 210 also cf SKF 64139 and cardiovascular side effects SKF 72223 254 & a2-adrenoceptors 60 chronic vs acute effects 279 & NE neuronal systems 60 effects on sleep 278 thalamus & high vs low affinity a2-receptor binding 72 binding 94 & 5-HT-2 receptors 94 as AD 142 & 5-HT sensitive adenylate as neuroleptic 179 cyclase 39 & spiperone binding 136-138, & 5-HT uptake 253 141 & in vivo demethylation 96 & spiperone-labelled 5-HT & NE receptor-coupled receptors 135 adenylate cyclase 4 TH1P & NE uptake 253 & bulbectomized rats 363-365 as receptor antagonists 253 (also cf response hormones ' specific & T3 11 compounds) (T3 ) & NE regulation 11 & 6-adrenoceptor response 11 thyroid releasing hormone & carbamazepine 180 (TRH) & response to TCA 11, 12 as 5-HT comodulator 101 twitches thyroid-like immunoreactivity from 5-HT excitation 95-101 & 5-HT system 34 & 1M1 97-98 thyroid stimulating hormone (TSH) induced by 5-MeO-DMT & carbamazepine 180 & DM1 93 thyroxine (T4) & 1M1 93 & carbamazepine 180 & zimelidine 93 transducer inhibition by various drugs & coupler protein 21 96 & ion gate 20 tyrosine hydroxylase (TH) & second messenger-generating & progabide 229 enzymes 20 & picrotoxin 229 transsynaptic mechanisms valproic acid & 1M1 19-31 as antimanic 184 y-vinyl GABA as AD 5 & bulbectomized rat 362-365 & bulbectomized rat 362-365 395 Wellbutrin - cf bupropion zimelidine (continued) chronic treatment (continued) yohimbine mechanism of action 41 as a2-adrenoceptor antagonist clinical pharmacology 68-73, 78, 146 255-257 as a2-antagonist 334 clinical trials 91 & platelets 334 & CSF metabolites 256 as anticonvulsant 178 'down-regulation' of 5-HT vs carbamazepine 178 inhibition 105 binding E-zimelidine cf isozimelidine in platelet membranes 77 high vs low affinity binding & platelets 340 39-40, 94 & brain a2-adrenoceptors & 5-HT binding 33 145-158 & 5-HT neuronal uptake 256 & brain e-adrenoceptors & 5-HT-2 receptors 94 145-158 & 5-HT receptor & bulbectomized 'r at 362-365 sub sensitivity 103-104 & a2-receptor conformation & 5-HT recognition site 301 151 as 5-HT reuptake inhibitor 86 zimelidine & 5-HT uptake inhibition 36, action on various receptors 95-105 280 & 1M1 binding 33 AD efficacy 257-259 & insomnia 260 vs amitriptyline 258 & locomotor activity 104 vs DM1 258 & 5-MeO-DMT-induced vs maprotiline 258 hyperactivity 100 adverse effects 259-260 metabolism 236, 256-257 anticholinergic effects 259 & NE receptor-coupled antihistamine activity 89 adenylate cyclase 4 antihistamine vs NE vs 5-HT reuptake an ticholinergic inhibition 86-88 activity 91 & pain sensitivity 102, 104 appetite & weight effects pharmacokinetics 256-257 259-260 & prolactin 49-51 & avoidance acquisition QNB binding vs anticholin­ 103, 104 ergic activity 90 block of mepyramine 89 & sleep 281 cardiovascular effects as specific 5-HT uptake 255-256, 260 inhibition 254 chronic treatment & spiperone binding 33, 45, & 5-HT 39, 40 140 & 5-HT adenylate cyclase structure 36, 89, 255 44 & tail flick 101 & 5-HT receptor activity & in vivo demethylation 96 93 ZK 62, 711 - cf Rolipram & 5-HT receptors 42-43, 93-108 & 1M1 binding sites 46-48 396