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467 Index a – pentylenetetrazol 357 ff. a interaction domain 71 – picrotoxin 357 a1 subunit 69 ff. antiepileptic drugs, receptor sites 9 a2-d subunit 57, 69 ff. antiepileptics 87 a-Dendrotoxin (DTX) 217 anxiety 369 – selectivity 219 – canopy test 369 ff. A-278637 344 ff. apamin 242, 244, 326 f. A- 411873 323 apoptosis 237 acetylcholine receptor deficiency 408 –Fas receptor 237 AChR 410 – mitochondria 237 action potential 44, 55 aryloxindole 321 adipocytes 244 ff. arylpyrrole 323 – brown fat 244 asthma 324 – glucose transporter 244 ATP-sensitive potassium channel KATP 335, – white fat 244 385 afterhyperpolarization 314 atrial effective refractory period (AERP) Agenelopsis aperta 131 291 alkaloid 319, 328 atrial fibrillation 276 ALMOND modul 432 ff. atrial vulnerability 291 Alzheimer’s disease 317 autism 396 ambasilide 278 autoantibodies 238 amiloride-sensitive epithelial sodium autoimmune diseases 247 ff. channel 397 autosomal dominant 4-aminopyridine 222 – juvenile myoclonic epilepsy 412 amiodarone 29, 278 – nocturnal frontal lobe epilepsy 410 amitriptyline, NaV blocking activity 186 auxiliary subunit in amlodipine 89 ff. –Kvb 11 amygdala-kindling model 357 ff., 361 – KChIp1-4 11 anandamide 91 – minK 11 ancillary calcium channel subunits 69 ff., auxiliary subunits 77 –Cava210 Andersen-Tawil syndrome 383 –Cavb 10 anesthetics 87 –Cavd 10 anosmia 251 –Cavg 10 antiarrhythmic drugs 9, 278 –Navb19 anticonvulsant –ofK+ channels 198 – amygdala-kindling 357 ff. AVE0118 287, 289 –6Hz model 361 azaindole 323 – maximal electroshock 357 ff. azimilide 278 Voltage-Gated Ion Channels as Drug Targets. Edited by D. Triggle Copyright c 2006 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim ISBN 3-527-31258-7 468 Index b – dialkyl-dipeptidylamines 132 b cell rest 341 – dihydropyridines 139 ff. b subunits 69 – ethanol 140 ff. b-cell overwork 341 – huwentoxin-I 127 b-tryptase inhibitors 440 – imidazolines 139 ff. b1-integrin 236 – non-specific N 128 B cell 215, 234, 237, 247 – piperazines 136 ff. – memory B cell 237 ff. – small organic molecule 132 ff. – proliferation 237 – substituted L-amino acids 132 –TCM 247 ff. – substituted piperidines 136 ff. –TEM 247 ff. – unsaturated hydrocarbons 138 ff. Ba2+ 86 – venom of the spiders 128 Ball, channel expression 238 – volatile anaesthetics 139 barnidipine 89 ff. BMS 191011 322 Bartter syndrome 406 BMS-180448 338 – type 2 383 BMS-189269 320 – type 4 407 BMS-191095 338 barttin 406 BMS-204352 312, 321 Becker’s syndrome 403 Boltzmann curve 23 benidipine 89 ff. Boltzmann function 26 benign familial neonatal bone resorption 250 – convulsions 388 borderline SMEI 395 – infantile seizures 396 Brugada syndrome 394 f. benzamides 235 bupivacaine 29, 171 – binding site 227 – structure 172 –Hill coefficient 227 –PAC 227 c – SAR 227 CACNA1A 401 f. – selectivity 227 CACNA1C 400 – trans-N-propyl-carbamoyloxy PAC 227 CACNA1F 401 benzimidazolinone 326, 329 CACNA1H 403 benzimidazolone 320 CACNA1S 399 benzooxazolone 326, 329 CACNB4 402 benzothiazepine class 103 calcium activators 100 bepridil 278 calcium channel 9, 65, 382, 399 binding 56 – L-type 27 biophysical properties 159 – N-type 122 – activation 160 –T-type 23, 27, 42, 84 – recovery from inactivation 160 calcium channel blockers 100 – state-dependent sodium channel – abscisic acid 108 blocker 161 – amlodipine 102 – steady-state inactivation 160 – benzacocine CGP 108 – use-dependent 162 – benzothiazepine 103 bladder 245 – BMY 20064 104 – hyperactivity 315 – calciseptine 115 –K+ channel expression 245 – calcludine 115 – overactivity 323, 326 – clotrimazole 114 blockers – 1,4-dihydropyridine 103 – aliphatic monoamines 138 ff. – diltiazem 101 ff. – v-agatoxin-IIIA 128 – dodecanol 114 – conclusions 140 ff. – dodecylamine 114 – v-conotoxin-GVIA 127 – felodipine 102 – v-conotoxin MVIIC 128 – FPL 64176 108 Index 469 – gene delivery 118 –TEM 247 – HOE 166 104 CD4+ 233 – isradipine 102 CD8+ 233 –L652,469 104 CD27 234, 237 – L-calchin 115 CD45RA 233 f. – MCI 176 104 –TEM 247 – McN-5691 104 CDP-840 434, 436 – McN-6186 104 central memory (TCM) 232 – MDL 12,330 104 cerebellar ataxia 314 – menthol 104, 114 cetiedil 324 – mibefradil 115 CFTR chloride channel 407 – nicardipine 102 CGS-7181 323 – nifedipine 101, 103 CGS-7184 323 – nimodipine 102 chalcone-16 230 – peptide toxins 115 – pharmacological properties 225 – phenylalkylamine 103 – selectivity 220 – praziquantel 117 channelopathy 381 ff., 412 – (–) S bay k 8644 108 charybdotoxin (ChTX) 57, 216 f., 318 – (+) S 202-791 108 – selectivity 219 –SR33557 104 – sequence 218 – structure–activity relationships 102 childhood absence epilepsy 396 – tetrandine 104 chloride channel 382, 403 – tinuvin 770 114 chloroquine 430 – verapamil 101, 103 chlorzoxazone 326 – vitamin D 115 CHO cells 429 –WAY 141520 117 chromanol 293B 278 calcium channel knockout 76 chronic constriction injury model 357 calcium currents chronic graft versus host disease (GvHD) – L-type 10, 65, 101 215, 237, 247 – N-type 10, 65, 123 – pathogenesis 250 –P/Q-type 10, 65 – therapies 250 – R-type 10, 65 ChTX 233, 235, 242, 245 f. –T-type 10, 65, 84 cisapride 430, 434 calcium ions 65 ClCa 50 calcium signaling 235 ClC-1 403 calcium-activated K+ channel 196, 199 ff., 310 ClC-2 404 calcium-dependent inactivation 70 ClC-5 405 candidate gene approach 381 CLC-7 406 f. canopy test 369 ClC-Ka and ClC-Kb channels 406 f. carbamazepine 21, 32 CLCN-K 406 – derivatives 173 CLCN1 403 – metabolism 173 CLCN2 404 – neuropathic pain 173 CLCN5 405 – structure 173 CLCN7 406 carrageenan model 359 Clofilium 278 Cav1.1 399 ClogP 431 Cav1.2 400 clotrimazole 242, 319, 324 – L-type 31 CMR 431 Cav1.4 401 CNG Channels 390 f. Cav2.1 401 CoMFA 434 Cav2.2 32, 403 CoMSiA 434 CC2-DMPE 52 cone snail toxins CCR7 233 f., 250 – disulfide pattern 221 470 Index – four disulfide bonds 221 – cardioprotective effects 338 congenital myasthenic syndromes 408 – b cell function 341 congenital stationary night blindness – hypoglycemia 336 type 2 401 – insulinomas 340 Conus catus 127 – nesidioblastosis 340 Conus geographus 130 – pharmacological tools 335 Conus magus 130 – polycystic ovary syndrome 340 – v-conotoxin-MVIIA 126 – side effects 341 conus striatus 130 DiBAC 51 f. v-conotoxin GVIA 66, 126 f. dichlorophenylpyrazolopyrimidines 228 v-conotoxin MVIIA 68 diclofenac 375 ff. CoroNa Green 58 dihydropyridine 21, 325 correolide 215, 217, 224, 235, 245 1,4-dihydropyrimidine 109 – C18-analog 227 1,4-dihydropyridine class 103 – binding-site 226 – activators 113 – pharmacological properties 225 – amlodipine 106, 108 – selectivity 220, 227 – benidipine 106 – spachea correa 226 – clinically available 110 – structure 223 – clinidipine 106 –Tcell proliferation 227 – conformational requirements 109 CP-339818 224 f. – felodipine 106 – selectivity 220, 225 – isradipine 106 – structure 223 – lacidipine 106 CRAC 234, 236 – lercanidipine 106 crobenetine – manidipine 106 – analgesic properties 177 – nicardipine 106 – regiochemistry 176 – nifedipine 106 – structure 177 – nilvadipine 106 – treatment of ischemic stroke 177 – nimodipine 106 cromakalim – nisoldipine 106 – bladder inhibitory effects 344 – nitrendipine 106 – cardioprotective effects 338 – NO-releasing activities 113 – clinical effects on bladder 343 – privileged structure 106, 114 –invitro (pig bladder strip) 347 – QSAR 109 – pharmacological tools 335 – state-dependence 110 cyclic nucleotide-gated channel 390 – state-dependent interactions 111 f. CYP2C9 inhibition 440 – stereoselectivity 107 cystic fibrosis 316, 407 – structure–activity relationships 107, 110 – vascular cardiac selectivity 111 d dihydropyridine KATP blocker 345 DC-EBIO 326 dihydropyridine KATP openers 345 de novo design 299 dihydropyridines 66, 89, 139 dehydrosoyasaponin-1 324 dihydroquinolones delayed type hypersensitivity (DTH) 236 – CP-339818 224 deltamethrin 55 – 125I-ChTX-displacement 224 dendrotoxin 57 – mechanism of channel block 224 Dent’s disease 405 – patch-clamp 224 DHS-1 324 – 86Rb-efflux 224 Di-ANEPPS 51, 55 – WIN-17317-3 224 diabetes 340 diisopyramide 28 dialkyl-dipeptidylamines 132 ff. diltiazem 21, 223, 278 diazoxide diphenylurea 320 – antihypertensive 336 disease association 162 Index 471 – channelopathies 162 Filistata hibernalis 128, 131 – febrile seizures plus (GEFS+) type 2 163 flecainide 28, 278 – GEFS+ type I 163 FLIPR 58 – hyperkalemic periodic paralysis 162 FLIPRr 33 – long Q-T syndrome type 3 163 flunarizine 88 ff. – myotonias 162 fluorescence 56 f. – paramyotonia congenita 163 fluorescence resonance energy transfer 429 – potassium aggravated myotonia 163 flupirtine (Katadolonr) 355 ff. – primary erythermalgia 163 formalin model 359 ff. disease indications 246 ff. frequency dependence 45 distribution of VGCCs 66 FRET 52 f., 55 dofetilide 57 dopamine 328 g drain plug model 434 Gbg 74 dronedarone 278 GABAA 412 drug acquired LQTS 447 – receptors 412 drug binding sites 207 gabapentin 57 d-sotalol 278 gain of function 382 ff., 385, 388, 390 f., ducky mouse 77 393 ff., 403, 410 gate 22 e gating 208 EAE 247 – state 19 1-EBIO 317, 326, 329 gene 214 effector memory (TEM) 232 generalized febrile epilepsy plus 395, 397 efonidipine 89 ff. genetic and acquired channelopathies 381 electrical signals 7 GIRK 50 ENaC 397 GLRA 410 ENaC channel 397 GLRB 410 encainide 28 glucose transporter 244 epilepsy 77, 355 ff. glyburide epilepsy with grand mal seizures – anti-arrhythmic activity 339 on awakening 404 – antidiabetic agent 336 episodic ataxia 76 – insulin-releasing properties 340 – type 1 386 – pharmacological tools 335 – type 2 401 glycine receptors 410 epithelia 245 goats model of AF 291 –K+ channel expression
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  • A A–803467, 98 Absorption, Distribution, Metabolism, Elimination

    A A–803467, 98 Absorption, Distribution, Metabolism, Elimination

    Index A Anxiety disorders, 55 A–803467, 98 APD. See Action potential duration Absorption, distribution, metabolism, Arrhythmias, 45, 46 elimination and toxicity Aryl sulfonamido indanes, 126–128, 130 (ADMET), 193 ATP-sensitive potassium channels (KATP Absorption, distribution, metabolism, channels), 61 excretion, and toxicity Atrial effective refractory period (AERP), 122, (ADMET), 68 124–126, 128, 129, 132, 138 Acetylcholine binding protein (AChBP), Autoimmune diseases, 254 61, 62, 64 AZD7009, 101 Acetylcholine receptor (AChR), 57, 64 Azimilide, 139 Action potential duration (APD), 120, 122, 123, 128, 132 B Action potentials, 243, 256, 259 Basis set, 69–70 ADME/T, 299, 304 b-Barrel membrane proteins AERP. See Atrial effective refractory period genome-wide annotation, 13 Agitoxin (AgTX), 60 machine-learning techniques Agonists, 59–61, 64 residue pair preference, 11 Alinidine, 40–42 TMBs, 10 ALS. See Amyotrophic lateral sclerosis pipeline, genomic sequences, 14 Alzheimer, 55, 61 statistical method, 9–10 AMBER, 61, 65 Bending hinge, 64 2-Amino–2-imidazolidinone, 123, 125 Benzanilide, 256–257 Ammi visnaga, 254 Benzimidazolone, 256–257 b-Amyloid peptide (Ab), 62–63, 65 Benzocaine, 140 Amyotrophic lateral sclerosis (ALS), 90, 94, Benzodiazepines, 245 101 Benzopyrane, 127–128 Anionic channel blockers Benzopyrans, 61, 246–251, 261 mechanism of action of, 329–330 Benzothiadiazine 1,1-dioxide, 252–254 Antagonists, 59, 60 Benzothiadiazines, 253 Antiarrhythmic, 65–66, 68, 99, 101 Benzothiazepine, 70 Antiarrhythmic agents Benzothiazine derivatives, 251–252 class I, 245 Benzotriazole, 256–257 class II, 245 Bestrophins, 321, 322, 330, 331 class III, 245 Big potassium channels (BK channels), Antidepressant, 65–67 256, 257 Antiepileptic, 46 Bupivacaine, 56, 58, 59, 64, 69, 140 S.P.