DOCSLIB.ORG

Back Matter (PDF)

Total Page：16

File Type：pdf, Size：1020Kb

Download full-text PDF Read full-text
Back Matter (PDF) INDEX Volume 21 3, April-June 1980 Aarbakke, J., see Gadeholt, G., tyl xanthine (MIX) on am- Anderson, D. F., Phernetton, T. muscle (dog), 150 196 phibian neuromyal transmis- M. and Rankin, J. H. G.: The Atria, positive isotropic action of Abboa-Offei, B. E., see Casey, F. sion, 586 measurement of placental digoxigenin, effects of sodium B., 432 Akera, T., see Yamamoto, S., 105 drug clearance in near-term (guinea pigs), 105 Acetaldehyde, effects on testicu- Alcohol sheep: Indomethacin, 100 Auber, M., see HalUshka, P. V., tar steroidogenesis (rats), 228 depression of myo-inositol 1- Anesthetics, local, frequency-de- 462 Acetaminophen phosphate in cerebral cortex pendent sodium channel Ayachi, S. and Brown, A. M.: Hy- probe analysis, hepatic gluts- (rat), 24 block in nerve (frog), 114 potensive effects of cardiac thione turnover in vivo deter- tolerance to (mice), 309 Angiotensin, comparison with ox- glycosides in spontaneously mined by (rats), 54 [‘4C]Allantoin, renal clearance ytocin in effect on prosta- hypertensive rats, 520 toxicity in lymphocytes in vitro (rabbit), 168 glandin release in IsOlated (man), 395 Allen, J. C., see Seidel, C. L., 514 uterus (rat), 575 Bainbridge, C. W. and Heistad, D. Acetazolamide Allergy, antiallergic properties of Anileridine, effects on body tem- D.: Effect of haloperidol on inhibition of bone resorption, SQ 13,847 and SQ 12,903 perature (mice), 273 ventilatory responses to do- lack of hypophosphateania (rats, mice, guinea pigs), 432, Anoxia, -induced contractions of pamine in man, 13 (rats), 441 437 coronary arteries, inhibition Barbitol, enhancement of effects inhibition of carbonic ashy- Allison, J. H. and Cicero, T. J.: by lidoflazine (dog), 179 of mus,cimol on dopamine drase, relation to cerebrospi- Alcohol acutely depresses Antibiotics, disposition, effects of turnover in retina (rat), 332 nat fluid (cats), 321 myo-inositol 1-phosphate 1ev- furosemide (rabbit), 600 Barbiturates, enhancement of ef- Acetylation, p-aminohippurate, ala in the male rat cerebral Antimycin A, inhibition of sodium fects of muscimol on dopa- by kidney (mice), 350 cortex, 24 transport and metabolism mine turnover in retina (rat), Acetylator phenotype Alloxan, -induced diabetes, alter- (toads), 375 332 inheritance (mice), 480 ations in dopamine-$-hy- Antinociception, alpha agonist- Barnett, A., see lorlo, L C., 445 relationship ofantinuclear anti- droxylase and norepineph- mediated, spinal cord phar- Baughman, W. L, see Dickinson, bodies to (mice), 485 rise (rats), 18 macology of (rats), 525 R G., 38 Acetylhydrazine, metabolism in p-Aminobenzoic acid, effects on Antinuclear antibodies, relation- Beek, D., see Kenakin, T. P., 406 vivo, hepatotoxic effect of bleomycin-induced pulmo- ship to acetylator phenotype Behavior (rats), 364 nary fibrosis (hamsters), 425 (mice), 485 methadone-induced attenua- Acetylisoniazid, metabolism in p-Aminohippurate, uptake and Antipyrine, half-life, hepatic, ef- tion of effects of 9-tetrahy- vivo, hepatotoxic effect of acetylation by kidney (mice), fects ofethanolfeeding (rats), drocannabinol on temporal (rats), 364 350 196 discrimination (pigeons), 247 t-a-Acetylmethadol, enterohe- /1-Aminopropiomtrile, effects on Antonissen, L A., Mitchell, R. W., schedule-controlled, effects of patic circulation (rats), 284 bleomycin-induced pulmo- Kroeger, B. A., Kepron, W., narcotic analgesics on (rats), Acetylsalicycic acid, antinocicep- nary fibrosis (hamsters), 425 Stephens, N. L and Bergen, 497 five effects, blockade by l-ly- 4-Aminopyridine and nicotine, ac- J.: Histamine pharmacology use of conditioned suppression sine (rat), 445 tion on sympathetic nerve in airway smooth muscle to evaluate neuroleptic-in- Actomyosin, in aorta, effect of hy- terminals (cat), 133 from a canine model of duced avoidance training dralazine-induced hypoten- Aminopyrine, antinociceptine ef- asthma, 150 (rat), 623 sion (rats), 514 fects, blockade by l-lysine Aorta Belinsky, S. A., see Reinke, L A., Adenosine 3’:S’-monophosphate (rat), 445 actomyosin and mechanical 70 (see Cyclic AMP) Amitriptyline properties, effect of hydrala- Belmaker, R H., see Ebstein, R ADP, effects of 6-keto-E1 on pal- effect on cerebral capillary zine-induced hypotension P., 161 monary hypertensive re- permeability in vivo (rat), 313 (rats), 514 Benzolamide, inhibition of car- sponse to (cats), 468 interaction with alpha and alpha adrenergic receptor, ef- bomc anhydrase, relation to Adrenergic agonists, apha, spinal muscarinic prejunctional re- fects of clonidine analogs cerebrospinal fluid (cats), 321 cord pharmacology of anti- ceptors in saphenous vein (rat), 267 Beninger, R. J., Mason, S. T., nociception mediated by (dog), 616 Arachidonic acid, -stimulated Phillips, A. G. and Fibiger, H. (rats), 525 Amphetamine short-circuit current in iso- C.: The use of conditioned Adrenergic receptor (see also effects on unit activity in medial lated urinary bladder (toads), suppression to evaluate the Adrenoreceptors) thalamus (rat), 580 462 nature of neuroleptic-in- ajpha, aorta, effects of clom- -induced mydriasis (cat), 49 Artery - duced avoidance deficits, 623 dine analogs (rat), 267 d-Amphetamine, acute responses coronary lidoflazine inhibition Bergen, J., see Antonissen, L A., Adrenoreceptors (see also Adre- to, role of amphetamine me- of contractions caused by 150 nergic receptors) tabolites (rats), 504 norepinephrine, 5-hydroxy- Berkowitz, B. A., Head, R., Joh, agonist, beta-i, prenalterol, tis- D-Amphetaimne, influence on tryptamine, potassium, an- T. and Hempstead, J.: Exper- sue selectivity (cats), 406 brain striatal-reduced biop- oxia and ergonovine maleate imental diabetes: Alterations beta, blocking activity, relation- term (rat), 569 (dog), 179 in circulating dopamine-$- ship with pharmacokinetics Anal coronary, smooth muscle, con- hydroxylase and norepineph- of dt-and l-propranolol (rab- effects on discrimination of tractile responses to potas- rise, 18 bit), 628 electric shock (monkeys), 234 sium and histamine, effects of Berner, P. F., DiSalvo, J. and Age, effects on hepatic glutathi- narcotic, tolerance to and en- R02-2985 (pig), 59 Schwartz, A.: Differential in- one turnover in vivo (rats), hancement of (rats), 418 systolic pressure, effects of car- hibitory effects of the iono- 54 nitrous oxide, attenuated aver- diac glycosides (rats), 520 phore RO2-2985 (X537A) on Akasu, T. and Karczmar, A. G.: siveness of electric shock dur- Asthma, canine model, histamine contractile responses to po- Effects of 1-methyl-3-isobu- ing (rat, monkey), 128 effects in airway smooth tassium and histamine in cor- 633 634 Index Vol. 213 onary artery smooth muscle, netics and plasma protein (dog), 509 a-Chloralose, effects on systolic 59 binding in (rats, man), 97 Carbon, R W., see Ruiz, C. E., arterial pressure and heart Biopterin, brain striatal-reduced, Butorphanol, effects on schedule- 414 rate (rats), 520 Influence of D-amphetanune controlled behavior (rats), Carpenter, H. M. and Mudge, G. Chiornaltrexamine, alkylating (rat), 569 497 H.: Uptake and acetylation of narcotic antagonist, pharma- Bircher, J., see Zysset, T., 173 p-aminohippurate by slices of cology (mice), 539 Bladders Caffeine mouse kidney cortex, 350 Chioroxymorphamine, alkylating urinary, isolated, effects of as- effects on unit activity in medial Caruso, T. P., Larson, D. L, Por- narcotic agonist, pharmacol- achidonic and eicosatrienoic thalamus (rat), 580 toghese, P. S. and Takemori, ogy (mice), 539 acids on short-circuit current -induced malignant hyperther- A. E.: Pharmacological stud- Choleretic effect, of valproic acid in (toad), 462 mis, properties of muscle ies with an alkylating nar- (monkey), 38 effects of furosemide and etha- (pig), 91 cotic agonist, chioroxymor- Choline uptake, sodium-depen- crynic acid on sodium trans- Calcitonin, inhibition of bone re- phamine, and antagonist, dent, brain, effects of h9- port and CO2 production in sorption hypophosphatemia chlornaltrexamine, 539 tetrahydrocannabinol and (toad), 383 after (rats), 441 Casey, F. B., Abboa-Offei, B. E. cannabidiol (rats), 216 effects of metabolic and trans- Calcium and Marretta, J.: Antiallergic Choroid plexus, carbonic ashy- port inhibitors on sodium effect on action of nicotine and properties of SQ 13,847, an drase inhibition, relation to transport and CO2 produc- 4-aminopyridine on sympa- orally effective agent. I. Ac- cerebrospinal fluid (cats), 321 tion in (toads), 375 thetic nerve terminals (cat), tivity in vivo, 432 Chou, D. T., Forde, J. H. and effects ofsodium and potassium 133 Catecholamines (see also specific Hirsh, K. R: Unit activity in on metabolism and sodium effect on vanadate inhibition of names) medial thalamus: Compara- transport in (toad), 390 renin secretion from kidney -induced malignant hyperther- tive effects of caffeine and Bleomycin, -induced pulmonary (rat), 144 mia, properties of muscle amphetamine, 580 fibrosis, evaluation of antifi- role in opiod action in ileum (pig), 91 Chronotropic effects, comparison brotic drugs in (hamsters), (guinea pig), 188 modulation of enkephalin-in- of prostacydlin and prosta- 425 synaptosomal uptake, inhibi- duced electrophysiological glandin E2 (dog), 261 Blood pressure, effect of p-by- tion by ethanol (rat, mice), responses in cerebral cortex Churchill, M. C., see Churchill, P. droxyamphetamine and p- 562 by (rats), 205 C., 144 hydroxynorephedrine (rats), Calcium-45 secretion, ionophore-induced, Churchill, P. C. and Churchill, M. 504 high and low affinity binding in 241 C.: Vanadate inhibits resin Blood vessels, increased resist- aortic
Load more

Recommended publications
  • (Ph OH N N Me O YO O YO
    US 20070265293A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2007/0265293 A1 Boyd et al. (43) Pub. Date: Nov. 15, 2007 (54) (S)-N-METHYLNALTREXONE Publication Classification (76) Inventors: Thomas A. Boyd, Grandview, NY (51) Int. Cl. (US); Howard Wagoner, Warwick, NY A6II 3L/4355 (2006.01) (US); Suketu P. Sanghvi, Kendall Park, A6M II/00 (2006.01) NJ (US); Christopher Verbicky, A6M I5/08 (2006.01) Broadalbin, NY (US); Stephen 39t. 35O C Andruski, Clifton Park, NY (US) (2006.01) A6IP 3L/00 (2006.01) Correspondence Address: St. 4. CR WOLF GREENFIELD & SACKS, P.C. (2006.01) 6OO ATLANTIC AVENUE 3G (i. 308: BOSTON, MA 02210-2206 (US) A6IP 33/02 (2006.01) C07D 489/00 (2006.01) (21) Appl. No.: 11/441,452 (52) U.S. Cl. .............. 514/282; 128/200.23; 128/202.17; (22) Filed: May 25, 2006 546/45 Related U.S. Application Data (57) ABSTRACT This invention relates to S-MNTX, methods of producing (60) Provisional application No. 60/684,570, filed on May S-MNTX, pharmaceutical preparations comprising 25, 2005. S-MNTX and methods for their use. O G M Br Br e (pH OH N N Me O YO O YO OH OH R-MNTX S-MNTX Patent Application Publication Nov. 15, 2007 Sheet 1 of 6 US 2007/0265293 A1 Fig. 1 OH OH Me-N Me-N D / O O -----BBr, O O CHCI NMP, 3 AUTOCLAVE, 70'C OMe OH 1 2 Br OH As GE) G As 69 GOH Me-N ION Me-N -lass O SO EXCHANGE O SO OH OH 3 S-MNTX 1 - OXYCODONE 2 - OXYMORPHONE 3 - ODIDE SALT OF S-MNTX Fig.
    [Show full text]
  • Psycho Pharmacology © by Springer-Verlag 1976
    Psychopharmacology 47, 65- 69 (1976) Psycho pharmacology © by Springer-Verlag 1976 Generalization of Morphine and Lysergic Acid Diethylamide (LSD) Stimulus Properties to Narcotic Analgesics I. D. HIRSCHHORN* and J. A. ROSECRANS Department of Pharmacology, Medical College of Virginia, Richmond, Virginia 23298, U.S.A. Abstract. The present investigation sought to deter- Physical dependence is not always associated with drug mine whether the stimulus properties of morphine craving and a high abuse liability. Some narcotic- and lysergic acid diethylamide (LSD) would gener- antagonist analgesics, such as cyclazocine and nalor- alize to several narcotic analgesics which vary in their phine, produce physical dependence with chronic subjective effects. Morphine and saline served as administration, but withdrawal does not result in drug discriminative stimuli for one group of rats in a 2-1ever seeking behavior (Martin et al., 1965; Martin and discrimination task. LSD and saline were discrimina- Gorodetzky, 1965). However, both cyclazocine and tive stimuli for a second group. Depression of one nalorphine have subjective side effects characterized lever in an operant chamber resulted in reinforcement by dysphoria and hallucinations (Haertzen, 1970) following the administration of morphine or LSD which render them unsuitable for therapeutic use. and the opposite lever was reinforced after saline. Pentazocine, a less potent antagonist of morphine After discriminated responding was stable, stimulus than cyclazocine and nalorphine, more closely resem- generalization tests with narcotic analgesics and bles morphine in its pharmacological effects and has antagonists showed that the stimulus properties of a somewhat greater incidence of non-medical use morphine generalized to methadone and meperidine, than antagonists of the nalorphine type (Paddock and partially to pentazocine, all of which produce etal., 1969).
    [Show full text]
  • Symposium Iv. Discriminative Stimulus Effects
    Life Sciences, Vol. 28, pp. 1571-1584 Pergamon Press Printed in the U.S.A. MINI - SYMPOSIUM IV. DISCRIMINATIVE STIMULUS EFFECTS OF NARCOTICS: EVIDENCE FOR MULTIPLE RECEPTOR-MEDIATED ACTIONS Seymore Herling and James H. Woods Departments of Pharmacology and Psychology University of Michigan Ann Arbor, Michigan q8109 The different pharmacological syndromes produced by morphine and related drugs in the chronic spinal dog led Martin and his colleagues (1,2) to suggest that these drugs exert their agonist actions 0y interacting with three distinct receptors (~,K, and e). Morphine was hypothesized to be an agonist for the p receptor, ketazocine (ketocyclazocine) was an agonist for the K receptor, and SKF-10,0q7 was an agonist for the ~ receptor. The effects of these three drugs in the chronic spinal dog were reversed by the narcotic antagonist, naltrexone, indicating that the effects of these drugs are narcotic agonist effects (I). In additlon to the different effects of these narcotics in the non- dependent chronic spinal dog, the effects of morphine, ketazocine, and SKF-IO,047 in several other behavioral and physiological preparations are consistent with the concept of multiple receptors. For example, while ketazocine and ethylketazocine, like morphine, produce analgesia, these compounds, unlike morphine, do not suppress signs of narcotic abstinence in the morphine-dependent rhesus monkey or morphine-dependent chronic spinal dog (1-5). Further, the characteristics of ketazocine withdrawal and antagonist- precipitated abstinence syndromes, although similar to those of cyclazocine, are quailtativeiy different from those of morphine (1,2). In rhesus monkeys, ketazocine, ethylketazocine, and SKF-10,047 maintain lever pressing at rates comparable to or below those maintained by saline, and well below response rates maintained by codeine or morphine (5,6), suggesting that the former set of drugs have limited reinforcing effect.
    [Show full text]
  • (19) United States (12) Patent Application Publication (10) Pub
    US 20030077300A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2003/0077300 A1 Wermeling (43) Pub. Date: Apr. 24, 2003 (54) SYSTEM AND METHOD FOR INTRANASAL Publication Classi?cation ADMINISTRATION OF OPIOIDS (51) Int. Cl.7 ........................ ..A61K 31/485; A61L 9/04; (76) Inventor: Daniel P. Wermeling, Lexington, KY A61K 9/00 (US) (52) US. Cl. ........................... .. 424/400; 424/45; 514/282 Corres ondence Address: Kalowp& Springut LLP (57) ABSTRACT 19th Floor . 488 Madison Avenue The invention relates to pharmaceutical drug compositions New York, NY 10022 (Us) and preparations that are narcotic antagonists and analge sics, speci?cally opioids, more speci?cally morphine and its (21) APPL NO: 10/155’624 pharmaceutically active derivatives, analogues, homo logues, and metabolites, and still more speci?cally hydro (22) Filed; May 24, 2002 morphone and butorphanol. This invention also relates to pharmaceutical drug delivery devices, speci?cally to devices for the intranasal administration of drugs classi?ed as con Related US, Application Data trolled substances. The invention also relates to the ?eld of acute pain management through pharmaceutical interven (63) Continuation of application No. 09/569,125, ?led on tion, particularly as practiced in an institutional setting, such May 10, 2000. as a hospital. Patent Application Publication Apr. 24, 2003 Sheet 1 0f 5 US 2003/0077300 A1 Patent Application Publication Apr. 24, 2003 Sheet 2 0f 5 US 2003/0077300 A1 m2:@505 ooow Sow wllooow coo?ll (1w/6d) 'ONOO vwsvw Patent Application Publication Apr. 24, 2003 Sheet 4 0f 5 US 2003/0077300 A1 .@Iw oooi ooowv 0002 ooow ooow Sow Patent Application Publication Apr.
    [Show full text]
  • The Respiratory, Circulatory, and Narcotic Antagonistic Effects of Nalorphine, Levallorphan, and Naloxone in Anaesthetized Subjects
    THE RESPIRATORY, CIRCULATORY, AND NARCOTIC ANTAGONISTIC EFFECTS OF NALORPHINE, LEVALLORPHAN, AND NALOXONE IN ANAESTHETIZED SUBJECTS FRANCIS F. FOLDES, M.D., DERYCK DUNCALF, M.B., F.F.A.R.C.$., AND SHIGEO KUWABARA, M.D. e IT HAS BEEN XaEt'ORTED that, when administered alone, the hvo clinically available narcotic antagonists, nalorphine hydrochloride (Nalline) 1-7 and levallorphan tar- trate, 8-1~ have respiratory and circulatory effects similar to those of narcotics. When a third potent narcotic antagonist, naloxone hydrochloride, became avail- able for experimental use, it seemed worthwhile to compare the respiratory and circulatory effects of equipotent doses 11,1~ of these three compounds under identi- cal conditions in man. While it obtained information of pharmacological interest, the main goal of this study was to determine which of these three compounds has the least liability to respiratory and circulatory side effects and is therefore preferable for clinical use. METHOD The observations to be reported were made on 50 patients without respiratory disease, who were anaesthetized for elective surgical procedures. The patients, ranging in age from 18 to 60 years, were divided at random into five groups of ten each. They received intramuscularly 100 mg pentobarbital sodium (Nembu- tal) and 0.4 mg scopolamine hydrobromide 90 and 45 minutes respectively before the start of the observation period. On arrival in the operating room, an intra- venous infusion of 5 per cent dextrose containing 0.2 per cent sodium chloride was started. The patients' mouths and pharynges were topically anaesthetized with a 1 per cent tetracaine hydrochloride (Pontocaine) spray. Subsequently, all drugs were administered through the rubber sleeve of the intravenous infusion.
    [Show full text]
  • Behavioral Interactions of Opioid Agonists and Antagonists with Serotonergic Systems David J
    University of New England DUNE: DigitalUNE Biomedical Sciences Faculty Publications Biomedical Sciences Faculty Works 1984 Behavioral Interactions Of Opioid Agonists And Antagonists With Serotonergic Systems David J. Mokler University of New England, [email protected] Richard H. Rech Randall L. Commissaris Judith W. Henck Follow this and additional works at: http://dune.une.edu/biomed_facpubs Part of the Chemicals and Drugs Commons, and the Medical Sciences Commons Recommended Citation Mokler, David J.; Rech, Richard H.; Commissaris, Randall L.; and Henck, Judith W., "Behavioral Interactions Of Opioid Agonists And Antagonists With Serotonergic Systems" (1984). Biomedical Sciences Faculty Publications. 4. http://dune.une.edu/biomed_facpubs/4 This Article is brought to you for free and open access by the Biomedical Sciences Faculty Works at DUNE: DigitalUNE. It has been accepted for inclusion in Biomedical Sciences Faculty Publications by an authorized administrator of DUNE: DigitalUNE. For more information, please contact [email protected]. Behavioral Interactions of Opioid Agonists and Antagonists With Serotonergic Systems Richard H. Rech, David J. Mokler, Randall L. Commissaris, and Judith W. Henck Morphine interacts with brain serotonergic (5-HT) systems; these systems have been implicated in morphine analgesia and dependence see Cervo et al., 1981). The 5-HT agonist quipazine induces analgesia in rats that is attenuated by naloxone and 5-HT antagonists (Minnema et al., 1980; Samanin et al., 1976). Behavioral disruption by the hallucinogens LSD, DMT and mescaline, mediated primarily through brain 5-HT effects (Rech and Commissaris, 1982), is potentiated by naloxone and naltrexone (Com- missaris et al., 1980; Ruffing and Domino, 1981) and is variably antago- nized or potentiated by morphine and methadone (Ruffing and Domino, 1981).
    [Show full text]
  • Agonist and Antagonist Actions of Morphine- Like Drugs on the Guinea-Pig Isolated Ileum by E
    Br. J. Pharmac. Chemother. (1966), 27, 514-527. AGONIST AND ANTAGONIST ACTIONS OF MORPHINE- LIKE DRUGS ON THE GUINEA-PIG ISOLATED ILEUM BY E. A. GYANG* AND H. W. KOSTERLITZ From the Department of Physiology, University of A berdeen (Received June 14, 1966) Substitution of the side-chain attached to the N atom of narcotic analgesic drugs of the morphine, morphinan and benzomorphan series leads to compounds which antagonize the action of the parent compounds; nalorphine and levallorphan, the allyl analogues of morphine and levorphanol, are widely used as " narcotic antagonists." However, these and other analogues also exhibit agonist properties; for example, they may act as analgesics and depress respiration (Eddy, Halbach & Braenden, 1957; Lasagna, De Kornfeld & Pearson, 1964). This dual action of the "narcotic antagonists " has also been observed in isolated tissues. Paton (1957a) showed that morphine and nalorphine are equally effective in depressing the electrically induced contraction of the longitudinal muscle of the guinea- pig ileum, and Gyang, Kosterlitz & Lees (1964) found that the same holds for their inhibitory actions on the peristaltic reflex or the graded reflex contraction of the longitudinal muscle. The experiments presented in this paper were planned to analyse more fully the actions of " narcotic agonists " and " narcotic antagonists " on the guinea-pig ileum. METHODS Experimental procedure. All experiments were performed on the guinea-pig isolated ileum; the terminal portion was used after discarding the 10 cm nearest to the ileo-caecal junction. In the first set of experiments, the depressant action of morphine-like drugs was tested on the contraction.of the longitudinal muscle induced by coaxial electrical stimulation (Paton, 1955).
    [Show full text]
  • Stembook 2018.Pdf
    The use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances FORMER DOCUMENT NUMBER: WHO/PHARM S/NOM 15 WHO/EMP/RHT/TSN/2018.1 © World Health Organization 2018 Some rights reserved. This work is available under the Creative Commons Attribution-NonCommercial-ShareAlike 3.0 IGO licence (CC BY-NC-SA 3.0 IGO; https://creativecommons.org/licenses/by-nc-sa/3.0/igo). Under the terms of this licence, you may copy, redistribute and adapt the work for non-commercial purposes, provided the work is appropriately cited, as indicated below. In any use of this work, there should be no suggestion that WHO endorses any specific organization, products or services. The use of the WHO logo is not permitted. If you adapt the work, then you must license your work under the same or equivalent Creative Commons licence. If you create a translation of this work, you should add the following disclaimer along with the suggested citation: “This translation was not created by the World Health Organization (WHO). WHO is not responsible for the content or accuracy of this translation. The original English edition shall be the binding and authentic edition”. Any mediation relating to disputes arising under the licence shall be conducted in accordance with the mediation rules of the World Intellectual Property Organization. Suggested citation. The use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances. Geneva: World Health Organization; 2018 (WHO/EMP/RHT/TSN/2018.1). Licence: CC BY-NC-SA 3.0 IGO. Cataloguing-in-Publication (CIP) data.
    [Show full text]
  • Salvinorin A: a Potent Naturally Occurring Nonnitrogenous Opioid Selective Agonist
    Salvinorin A: A potent naturally occurring nonnitrogenous ␬ opioid selective agonist Bryan L. Roth*†‡§¶, Karen Baner*, Richard Westkaemperሻ, Daniel Siebert**, Kenner C. Rice††, SeAnna Steinberg*, Paul Ernsberger*‡‡, and Richard B. Rothman§§ *National Institute of Mental Health Psychoactive Drug Screening Program, and Departments of †Biochemistry, ‡Psychiatry, §Neurosciences, and ‡‡Pharmacology and Nutrition, Case Western Reserve University Medical School, Cleveland, OH 44106; §§Clinical Psychopharmacology Section, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, Baltimore, MD 21224; ࿣Department of Medicinal Chemistry, Medical College of Virginia, Richmond, VA 23298; **The Salvia divinorum Research and Information Center, Malibu, CA 90263; and ††Laboratory of Medicinal Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892 Edited by Erminio Costa, University of Illinois, Chicago, IL, and approved July 9, 2002 (received for review April 18, 2002) Salvia divinorum, whose main active ingredient is the neoclero- pharmacological properties of rodent and human molecular dane diterpene Salvinorin A, is a hallucinogenic plant in the mint targets are frequently distinct (7), and that tissue-based radio- family that has been used in traditional spiritual practices for its ligand binding assays frequently yield inaccurate estimates of psychoactive properties by the Mazatecs of Oaxaca, Mexico. More drug potency and selectivity. Accordingly, we reexamined the recently, S. divinorum extracts and Salvinorin A have become more molecular pharmacological profile of the novel diterpene Salvi- widely used in the U.S. as legal hallucinogens. We discovered that norin A at a large number of cloned human G protein-coupled Salvinorin A potently and selectively inhibited 3H-bremazocine receptors (GPCRs), channels, and transporters.
    [Show full text]
  • Truncated G Protein-Coupled Mu Opioid Receptor MOR-1 Splice Variants Are Targets for Highly Potent Opioid Analgesics Lacking Side Effects
    Truncated G protein-coupled mu opioid receptor MOR-1 splice variants are targets for highly potent opioid analgesics lacking side effects Susruta Majumdara, Steven Grinnella, Valerie Le Rouzica, Maxim Burgmana, Lisa Polikara, Michael Ansonoffb, John Pintarb, Ying-Xian Pana, and Gavril W. Pasternaka,1 aMolecular Pharmacology and Chemistry Program and Department of Neurology, Memorial Sloan-Kettering Cancer Center, New York, NY 10065; and bDepartment of Neuroscience and Cell Biology, Robert Wood Johnson Medical School, Piscataway, NJ 08854 Edited by Solomon H. Snyder, Johns Hopkins University School of Medicine, Baltimore, MD, and approved October 21, 2011 (received for review September 17, 2011) Pain remains a pervasive problem throughout medicine, transcend- administration. In addition to its high potency, IBNtxA also ing all specialty boundaries. Despite the extraordinary insights into displayed full efficacy, as indicated by most mice reaching cutoff pain and its mechanisms over the past few decades, few advances values at higher doses. We also assessed IBNtxA analgesia by have been made with analgesics. Most pain remains treated by using a graded response [percentage maximal possible effect (% opiates, which have significant side effects that limit their utility. MPE)] (Fig. S2). Its ED50 value (0.34 mg/kg; 95% confidence We now describe a potent opiate analgesic lacking the traditional limits: 0.23, 0.52) was very close to that with quantal responses side effects associated with classical opiates, including respiratory (Fig. 3A). Furthermore, IBNtxA analgesia was not limited to the fi depression, signi cant constipation, physical dependence, and, radiant heat tail-flick assay. IBNtxA was a potent analgesic in the perhaps most important, reinforcing behavior, demonstrating that hot plate assay (ED50 = 0.6 mg/kg) as well (Fig.
    [Show full text]
  • Harmonized Tariff Schedule of the United States (2004) -- Supplement 1 Annotated for Statistical Reporting Purposes
    Harmonized Tariff Schedule of the United States (2004) -- Supplement 1 Annotated for Statistical Reporting Purposes PHARMACEUTICAL APPENDIX TO THE HARMONIZED TARIFF SCHEDULE Harmonized Tariff Schedule of the United States (2004) -- Supplement 1 Annotated for Statistical Reporting Purposes PHARMACEUTICAL APPENDIX TO THE TARIFF SCHEDULE 2 Table 1. This table enumerates products described by International Non-proprietary Names (INN) which shall be entered free of duty under general note 13 to the tariff schedule. The Chemical Abstracts Service (CAS) registry numbers also set forth in this table are included to assist in the identification of the products concerned. For purposes of the tariff schedule, any references to a product enumerated in this table includes such product by whatever name known. Product CAS No. Product CAS No. ABACAVIR 136470-78-5 ACEXAMIC ACID 57-08-9 ABAFUNGIN 129639-79-8 ACICLOVIR 59277-89-3 ABAMECTIN 65195-55-3 ACIFRAN 72420-38-3 ABANOQUIL 90402-40-7 ACIPIMOX 51037-30-0 ABARELIX 183552-38-7 ACITAZANOLAST 114607-46-4 ABCIXIMAB 143653-53-6 ACITEMATE 101197-99-3 ABECARNIL 111841-85-1 ACITRETIN 55079-83-9 ABIRATERONE 154229-19-3 ACIVICIN 42228-92-2 ABITESARTAN 137882-98-5 ACLANTATE 39633-62-0 ABLUKAST 96566-25-5 ACLARUBICIN 57576-44-0 ABUNIDAZOLE 91017-58-2 ACLATONIUM NAPADISILATE 55077-30-0 ACADESINE 2627-69-2 ACODAZOLE 79152-85-5 ACAMPROSATE 77337-76-9 ACONIAZIDE 13410-86-1 ACAPRAZINE 55485-20-6 ACOXATRINE 748-44-7 ACARBOSE 56180-94-0 ACREOZAST 123548-56-1 ACEBROCHOL 514-50-1 ACRIDOREX 47487-22-9 ACEBURIC ACID 26976-72-7
    [Show full text]
  • Discovery of Novel Opioid Medications
    National Institute on Drug Abuse RESEARCH MONOGRAPH SERIES Discovery of Novel Opioid Medications 147 U.S. Department of Health and Human Services • Public Health Service • National Institutes of Health Discovery of Novel Opioid Medications Editors: Rao S. Rapaka, Ph.D. Heinz Sorer, Ph.D. NIDA Research Monograph 147 1995 U.S. DEPARTMENT OF HEALTH AND HUMAN SERVICES Public Health Service National Institutes of Health National Institute on Drug Abuse 5600 Fishers Lane Rockville, MD 20857 ACKNOWLEDGEMENT This monograph is based on the papers from a technical review on “Discovery of Novel Opioid Medications” held on July 28-29, 1993. The review meeting was sponsored by the National Institute on Drug Abuse. COPYRIGHT STATUS The National Institute on Drug Abuse has obtained permission from the copyright holders to reproduce certain previously published material as noted in the text. Further reproduction of this copyrighted material is permitted only as part of a reprinting of the entire publication or chapter. For any other use, the copyright holder’s permission is required. All other material in this volume except quoted passages from copyrighted sources is in the public domain and may be used or reproduced without permission from the Institute or the authors. Citation of the source is appreciated. Opinions expressed in this volume are those of the authors and do not necessarily reflect the opinions or official policy of the National Institute on Drug Abuse or any other part of the U.S. Department of Health and Human Services. The U.S. Government does not endorse or favor any specific commercial product or company.
    [Show full text]