Section Review—Central & Peripheral Nervous Systems: 5-HT₃ Receptor Antagonists in Development As-Anxiolytics

References

• HOYER D, CLARICE DE, FOZARD JR, HARTIG PR, MARTIN seGR, MYLECHARENE EJ, SAXENA PR, HUMPHREY PPA:International Union of Pharmacology classification of receptors for 5-hydroxytryptamine (serotonin). Phar-macol. Rev. (1994) 46:157-203. Recent review including the criteria of IUPHAR for classification of 5-HT receptor classes.
   Google Scholar
• BOESS FG, MARTIN IL: Molecular biology of 5-HT receptors. Neuropharmacology (1994) 33:275-317. Good review on the molecular biology of the different 5-FIT receptor subtypes.
   Google Scholar
• MARTIN GR, HUMPHREY PPA: Receptors for 5-hy-droxytryptamine: current perspectives on classifica-tion and nomenclature. Neuropbannacology (1994) 33:261–273.
   PubMed Web of Science ®Google Scholar
• PEROUTKA SJ, HOWELL TA: The molecular evolution of G protein-coupled receptors: focus on 5-hydroxytryp-tamine receptors. Neuropbarmacology (1994) 33:319–324.
   PubMed Web of Science ®Google Scholar
• IVERSEN SD: 5-HT and anxiety. Neuropharrnacology (1984) 23:1553–1560.
   PubMed Web of Science ®Google Scholar
• HANDLEY SL, MCBLANE JW: 5-HT drugs in animal models of anxiety. Psychopbarmacology 0993) 112:13-20.
   Google Scholar
• CHOPIN P, BRILEY M: Animal models of anxiety: theeffect of compounds that modify 5-HT neurotransmis-sion. TIPS (1987) 8:383–388.
   Web of Science ®Google Scholar
• BARRET JE, VANOVER KE: 5-HT receptors as targets for the development of novel anxiolytic drugs: models, mechanisms and future directions. Psychopharmacology (1993) 112:1–12.
   Google Scholar
• •• Review on the function of 5-HT in anxiety 00 GPO Review on the action of 5-HT-related drugs in animal models of anxiety.
   Google Scholar
• CHENG CHK, COSTALL B, KELLY ME, NAYLOR RJ: Actionsof 5-hydroxytryptophan to inhibit and disinhibit mouse behaviour in the light/dark test. Eur. J. Pharma-col. (1994) 255:39–49.
   PubMed Web of Science ®Google Scholar
• GLENNON RA: Serotonin receptor: Clinical implica-tions. Neurosci. Biobehav. Rev. (1990) 14:35–47.
   PubMed Web of Science ®Google Scholar
• DEL RIO J, LASHERAS B: The role of different serotoninreceptor subtypes in psychiatric syndromes. In: Strate-gies for studying brain disorders. Vol. I. Depressive, anxiety and drug abuse disorders. Palomo T, Archer T (Eds.). Farrand Press, London.(1994):239–250.
   Google Scholar
• HANDLEY SL, MCBLANEJW, CRITCHLEY MAE, NJUNG'E K: Multiple serotonin mechanisms in animal models of anxiety: environmental, emotional and cognitive fac-tors. Behav. Brain Res. (1993) 58:203-210. Interesting discussion on serotonergic fuction in anxiety.
   Google Scholar
• CEULEMANS DLS, HOPPENBROUWERS M-L, GELDERS YG, REYNTJENS AJM: The influence of ritanserin, a serotonin antagonist, in anxiety disorders: a double-blind pla-cebo-controlled study versus lorazepam. Pharmacopsy-chiaoy (1985) 18:303–305.
   PubMed Web of Science ®Google Scholar
• MITCHELL EA, PRATT JA, KILPATRICK GJ: Effects of the 5-HT3 receptor agonist mCPBG in the social interaction test of anxiety. Br. J. Pharmacol. (1991) 104:252P.
   Google Scholar
• HEN R, SAUDOU F, AMARA DA, BELZUNG C, DIERICH A, LEMEUR M, RAMBOZ S, SEGU L, MISSLIN R, BUHOT MC: Mice lacking 5-hydroxytryptamine 18 receptors display aggressive behavior. Soc. Neurosci. Abstr. (1994) 20:1266.
   Google Scholar
• MONSMA FJ, SHEN Y, WARD RP, HAMBLIN MW, SIBLEY • DR: Cloning and expression of a novel serotonin recep-tor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. (1993) 43:320-327. One example of the potential psychopharmacological interest of recently cloned 5-HT receptors.
   Google Scholar
• SHEN Y, MONSMA FJ, METCALF MA, JOSE PA, HAMBLINSMW, SIBLEY DR: Molecular cloning and expression of a 5-hydroxytryptamine7 serotonin receptor subtype. J. Biol. Chem. (1993) 268:18200–18204.
   PubMed Web of Science ®Google Scholar
• MARICQ AV, PE TERSON AS, BRAKE AJ, MYERS RM, JULIUS •D: Primary structure and functional expression of the5-HT3 receptor, a serotonin-gated ion channeL Science (1991) 254:432-437. Identification of rodent cDNA encoding the 5-HT3 receptor.
   Google Scholar
• APUD JA: The 5-HT3 receptor in mammalian brain: a new target for the development of psychotropic drugs? Neuropsychopharmacology (1993) 8:117-130. Good review on some basic aspects of 5-HT3 receptors of possible relevance in Psychiatry.
   Google Scholar
• BLANDINA P, GOLDFARB J, CRADDOCK-ROYAL B, GREEN JP: Release of endogenous dopamine by stimulation of 5-hydroxytryptamine3 receptors in rat striatum. J. Phar-macol. Exp. Ther. (1988) 251:803–809.
   Web of Science ®Google Scholar
• BARNES JM, BARNES NM, COSTALL B, NAYLOR RJ, TYERS MB: 5-HT3 receptors mediate inhibition of acetylcholine release in cortical tissue. Nature (1989) 338:762–763.
   PubMed Web of Science ®Google Scholar
• ZAZPE A, ARTAIZ I, DEL RIO J: Role of 5-HT3 receptors inbasal and Ktevoked dopamine release from rat olfac-tory tubercle and striatal slices. Br. J. Pharmacol. (1994) 113:968–972.
   PubMed Web of Science ®Google Scholar
• COSTALL B, DOMENEY AM, NAYLOR RJ, TYERS MB: Effectsof the 5-HT3 receptor antagonist, GR 38032F, on raised dopaininergic activity in the mesolimbic system of rat and marmoset brain. Br.J. Pharmacol. (1987) 92:881–894.
   PubMed Web of Science ®Google Scholar
• DOMENEY AM, COSTALL B, GERRARD PA, JONES DNC,NAYLOR RJ, TYERS MB: The effect of ondansetron on cognitive performance in the marmoset. Pharmacol. Bioc hem. Behav. (1991) 38: 169–175.
   PubMed Web of Science ®Google Scholar
• BARNES JM, BARNES NM, COOPER SJ: Behavioural phar-macology of 5-HT3 receptor ligands. Neurosci. Biobehav. Rev.. (1992) 16:107–113.
   PubMed Web of Science ®Google Scholar
• HOYER D: Serotonin 5-HT3, 5-HT4, and 5-HT-M recep- tors. Neuropsychopharrnacology (1990) 3:371-383. Historical account and features of 5-HT3 receptors.
   Google Scholar
• BONHAUS DW, WONG EHF, STEFANICH E, KUNYSZ EA, •EGLEN RM: Pharmacological characterization of 5-hy-droxytryptamine3 receptors in murine brain and ileum using the novel radioligand [311111S-42358-197: evidence for receptor heterogeneity. J. Neurochem (1993) 61:1927-1932. Evidence for 5-HT3 receptor heterogeneity in the same animal species.
   Google Scholar
• WONG EHF, BONHAUS DW, LEE JA, WU I, LOURY DN, EGLEN RM: Different densities of 5-HT3 receptors are labeled by [311]quipazine, [3111GR 65630 and [3II]granisetron. Neuropharmacology (1993) 32:869–875.
   PubMed Web of Science ®Google Scholar
• HIGGINS GA, JONES BJ, OAKLEY NR, TYERS MB: Evidence that the amygdala is involved in the disinhibitory ef-fects of 5-11T3 receptor antagonists. Psychopharmacology. (1991) 104:545-551. Relevance of 5-HT3 receptors located in limbic regions in the anxiolytic activity of 5-HT3 receptor antagonists.
   Google Scholar
• VOGEL JR, BEER B, CLODY DE: A simple and reliable conflict procedure for testing anti-anxiety agents. Psy-chopharmacologia (1971) 21:1–7.
   PubMed Web of Science ®Google Scholar
• COOK L, DAVIDSON AB: Effects of behaviorally active drugs in a conflict-punishment procedure in rats. In: The Benzodiazepines. Garattini S, Mussini E, Randall LO (Eds.). Raven Press, New York (1973):327–345.
   Google Scholar
• WITKIN JM, MANSBACH RS, BARRETT JE, BOLGER GT, SKOLNICK P, WEISSMAN B: Behavioural studies with anxiolytic drugs. N. Serotonergic involvement in the effects of buspirone on punished behaviour of pigeons. J. Pharmacol. Exp. Ther. (1987) 243:290–977.
   Google Scholar
• CRAWLEY JN, GOODWIN FK: Preliminary report of a simple animal behaviour model for the anxiolytic ef-fects of benzocliaaepines. Pharmacol. Biochem. Behav. (1980) 13:167–170.
   PubMed Web of Science ®Google Scholar
• RAHMAN SK, PIPER DC, KING FD: 5-HT3 receptor antagonists. E-r, opn Ther. Patents (1994) 4:669-680. Review on the structure-activity relationships of 5-HT3 receptor antagonists and their clinical possibilities.
   Google Scholar
• GAO B, CUTLER MG: Effects of acute administration ofthe 5-HT3 receptor antagonist, BRL 46470A, on the behaviour of mice in a two compartment light-dark box and during social interactions in their home cage and an unfamiliar neutral cage. Neuropharrnacology (1992) 31:743–748.
   PubMed Web of Science ®Google Scholar
• COSTALL B, NAYLOR RJ, TYERS MB: The psychopharmacology of 5-HT3 receptors. Pharmac. Ther. (1990)47:181-202. 27.
   Google Scholar
• •• OS A classic review by a pioneering group in behavioural studies with 5-HT3 receptor antagonists.
   Google Scholar
• ARTAIZ I, ROMERO G, ZAZPE A, MONGE A, CALDERO JM, ROCA J, LASHERAS B, DEL RIO J: The pharmacology of VA21B7: an atypical 5-HT3 receptor antagonist with anxiolytic-like properties in animal models. Psycho-pharmacology (1995) 117:137–148.
   PubMed Web of Science ®Google Scholar
• BORSINI F, BRAMBILLA R, CESANA R, DONE'rTI A: The effect of DAU 6215, a novel 5HT-3 antagonist, in animal models of anxiety. Pharmacol. Res. (1993) 27:151–164.
   PubMed Web of Science ®Google Scholar
• BILL DJ, FLETCHER A, GLENN BD, KNIGHT M: Behavioural studies on WAY 100289, a novel 5-HT3 receptor antago-nist, in two animal models of anxiety. Eur. J. Pharmacol. (1992) 218:327–334.
   PubMed Web of Science ®Google Scholar
• COSTALL B, DOMENEY AM, KELLY ME, TOMKINS DM, NAYLOR RJ, WONG ELIE, SMITH WL, WHITING RL, EGLEN EM: The effect of the 5-HT3 receptor antagonist, RS-42358-197, in animal models of anxiety. Eur. J. Pharma-col. (1993) 234:91–99.
   PubMed Web of Science ®Google Scholar
• YOUNG R, JOHNSON DN: Anxiolytic-like activity of R(+)-
   Google Scholar
• „and S(-)-zacopride in mice. Eur. J. Pharmacol. (1991)201:151-155. The antagonist potency of the two isomers at 5-HT3 receptors is not correlated with anxiolytic-like activity in rodents.
   Google Scholar
• BARNES NM, CHENG CHK, COSTALL B, GE J, KELLY ME, NAYLOR RJ: Profiles of interaction of R(+)/S(-) zacopride and anxiolytic agents in a mouse modeL Eur. J. Pharma-col. (1992) 218:91–100.
   Google Scholar
• KIDD E, BOUCHELET DE VENDEGIES I, LEVY JC, HAMON M, GOZLAN H: The potent 5-HT3 receptor antagonist (R)-zacopride labels an additional high affinity site in the central nervous system. Eur. J. Pharmacol. (1992) 211:133–136.
   PubMed Web of Science ®Google Scholar
• FILE SE: The use of social interaction as a method for detecting anxiolytic-activity of chlordiazepoxide-like drugs. J. Neurosci. Meth. (1980) 2:219–238.
   PubMed Web of Science ®Google Scholar
• PELLOW S, CHOPIN P, FILE SE, BRILEY M: Validation of open: closed arm entries in an elevated plus-maze as a measure of anxiety in the rat. J. Neurosci. Meth. (1985) 14:149–167.
   PubMed Web of Science ®Google Scholar
• FILE SE, JOHNSTON AL: Lack of effects of 5-HT3 receptorantagonists in the social interaction and elevated plus-maze tests of anxiety in the rat. Psychopharmacology (1989) 99:248–251.
   PubMed Web of Science ®Google Scholar
• BLACKBURN TP, BAXTER GS, KENNETT GA, KING FD, PIPER DC, SANGER GJ, THOMAS DR, UPTON N, WOOD MD: BRL 46470A: a lighly potent, selective and long acting 5-HT3 receptor antagonist with anxiolytic-like properties. Psychopharmacology (1993) 110:257–264
   PubMed Web of Science ®Google Scholar
• DUNN RW, CARLEZON WA, CORBE1 I R: Preclinical anx-iolytic versus antipsychotic profiles of the 5-HT3 an-tagonists ondansetron, zacopride, 3a-tropanyl -1H-indole-3-carboxylic acid ester, and laB, 3a, 5a11-tropan-3-y1-3,5-dichlorobenzoate. Drug Develop. Res. (1991) 23:289–300.
   Web of Science ®Google Scholar
• WRIGHT IK, HEATON M, UPTON N, MARSDEN CA: Com-parison of acute and chronic treatment of various serotonergic agents with those of diazepam and ida-zoxan in the rat elevated X-maze. Psychopharmacology. (1992) 113:405–414.
   Google Scholar
• PRATHER PL, REZAZADEH SM, LANE JD, ROWAN GA, HOOPER ML, LYTLE DA, EMMETT-OGLESBY MW, LAL H: Conflicting evidence regarding the efficacy of ondan-setron in benzodiazepine withdrawaLJ. Pharmacol. Exp. 7ber. (1993) 264:622–630.
   Google Scholar
• RODGERS RJ, COLE JC, TREDWELL JM: Ethological analy-sis fails to reveal anxiolytic effects of 5-HT3 receptor antagonists, ondansetron and WAY 100289, in the mur-ine plus-maze. Br. J. Pharmacol. (1993) 110:12P.
   Web of Science ®Google Scholar
• ACQUAS E, CARBONI E, GARAU L, DI CHIARA G: Blockade of acquisition of drug-conditioned place aversion by 5-HT3 antagonists. Psychopharmacology (1990) 100:459–463.
   PubMed Web of Science ®Google Scholar
• RODGERS RJ, SHEPHERD JK, RANDALL JI: Highly potent Inhibition effects of 5-HT3 receptor antagonist, GR 38032F, on non-opioid defeat analgesia in male mice. Neuropharmacology (1990) 29:17–23.
   PubMed Web of Science ®Google Scholar
• COSTALL B: The breadth of action of the 5-HT3 receptor antagonists. Int. Clin. Psychopharmacol. (1993) 8:3–9.
   PubMed Web of Science ®Google Scholar
• DE VRY J, BEZ U, SCHREIBER R, TRABER J: Shock induced ultrasonic vocalbation in young adult rats: a model for testing putative anti-anxiety drugs. Eur. I Pharmacol. (1993) 249:331–339.
   PubMed Web of Science ®Google Scholar
• GREENSHAW AJ: Behavioural pharmacology of 5-HT3 receptor antagonists: a critical update on therapeutic potential. TIPS (1993) 141:263–270.
   Google Scholar
• STEFANSKI R, PALEJKO W, BIDZINSKI A, KOSTOWSKI W, • PLAZNIK A: Serotonergic innervation of the hippocam-pus and nucleus accumbens septi and the anxiolytic-like actions of the 5-HT3 receptor antagonists. Neuropharmacology (1993) 32:987-993. One of the few studies showing anxiolytic-like activity of 5-HT3 antagonists in conflict paradigms in rodents.
   Google Scholar
• MENESES A, HONG E: Modification of the anxiolytic effects of 5-HT1A agonists by shock intensity. Pharmacol. Biochem. Behav. (1993) 46:569–573.
   PubMed Web of Science ®Google Scholar
• DAVIS M: Pharmacological and anatomical analysis of fear conditioning using the fear-potentiated startle paradigm. Behav. Neurosci. (1986) 100:814–824.
   PubMed Web of Science ®Google Scholar
• NEVINS ME, ANTHONY EW: Antagonists at the serotonin-3 receptor can reduce the fear-potentiated startle re-sponse in the rat: evidence for different types of anxiolytic activity? J Pharmacol. Exp. Ther. (1994) 268:248–268.
   PubMed Web of Science ®Google Scholar
• ANDREWS N, ME SE: Increased 5-HT release mediatesthe anxiogenic response during benzodiazepine with-drawal: a review of supporting neurochemical and behavioural evidence. Psychopharmacology. (1993) 112:21–25.
   PubMed Web of Science ®Google Scholar
• LEATHLEY MJ, GOLTDIE AJ: Effects of the 5-HT3 antagonistICS 205-930 on benzodiazepine withdrawal in rats. Behav. Pharmacol. (1992) 3:51–56.
   PubMed Web of Science ®Google Scholar
• GOUDIE AJ, LEATHLEY MJ: Effects of the 5-HT3 antagonistondansetron on benzodiazepine-induced operant be-havioural dependence in rats. Psychopharmacology (1992) 109:461–465.
   PubMed Web of Science ®Google Scholar
• LECRUBIER Y, PUECH AJ, AZCONA A, BAILEY PE, LATASTEX: A randomized double-blind placebo-controlled study of tropisetron in the treatment of outpatients with generalized anxiety disorder. Psychopharmacology(1993) 112:129-133. First full-length paper describing the efficacy of a 5-11T3 receptor antagonist in the treatment of anxiety disorders.
   Google Scholar
• ROTHE B, GLTLDNER J, HOHLFELDT E, LAUER CJ, POLL- MACHER T, HOLSBOE F, STEIGER A: Effects of 5-HT3 receptor antagonism by tropisetron on the sleep EEG and on nocturnal hormone secretion. Neuropsychophar-macology (1994) 11:101–106.
   PubMed Web of Science ®Google Scholar
• LADER M: (Reported in SCRIP (1991) 1626:24–25).
   Google Scholar
• VAN VEGGEL LMA, PRESTON C, O'HANLON JF: Ondan-setron and diazepam effects on actual driving and psychomotor performance. Neuropsychopharmacology (1994) 10:27S.
   Google Scholar
• BROOCKS A, PIGOTT T, CANTER S, HILL J, MURPHY DL: The highly-selective 5-HT3-antagonist, ondansetron, in-hibits GH secretion in healthy volunteers and patients with obsessive-compulsive disorder. Neuropsychophar-macology (1994) 10:151S.
   PubMedGoogle Scholar
• METZ A, EVONIUK G, DE VEAUGH-GEISS J: Multicenter trial of a 5-HT3 antagonist, ondansetron, in panic dis-order [Abstract]. American College of Neuropsychopharrna-cology Meeting. Puerto Rico, December 12–16 (1994).
   Google Scholar
• BELL J, DE VEAUGH-GEISS J: Multicenter trial of a 5-HT3antagonist, ondansetron, in social phobia [Abstract]. American College of Neuropsychopharmacology Meeting. Puerto Rico, December 12–16 (1994).
   Google Scholar
• PECKNOLD JC, LATHE L, INY L, MEANEY M: Platelet [31I]paroxetine and [31i]imipramine binding in zaco-pride treated patients with generalized anxiety disor-der: preliminary results. In: New concepts of anxiety. Briley M and File S (Eds), Macmillan, London (1991) 168–174.
   Google Scholar
• ANSSEAU M, PITCHOT W, GONZALEZ MORENO A: Pla-cebo-controlled study of the anxiolytic activity of single doses of zacopride among inpatients with genealized anxiety disorder. Neuropsychopharrnacology (1994) 10:260S.
   Google Scholar
• SmithKline Beecham Annual Report (1992).
   Google Scholar
• LINK CGG, LEIGH TJ, DENNISON JK: The effects of BRL 46470A, a novel 5-HT3 receptor antagonist, and lorazepam on psychometric performance and the EEG. Br. J. Clin. Pharrnacol. (1993) 35:395-399. At variance with benzodiazepines, a 5-HT3 receptor antagonist does not impair psychometric performance.
   Google Scholar
• LEIGH TJ, LINK CGG, FELL GL: Effects of granisetron and lorazeparn, alone and in combination, on psychometric performance. Br.J. Clin. Pbarrnacol. (1991) 31:333–336.
   PubMed Web of Science ®Google Scholar
• SEL'VERSTONE PH, COWEN PJ: The 5-HT3 antagonist BRL 46470 does not attenuate m-chlorophenylpiperazine (mCPP)-induced changes in human volunteers. Biol. Psychiat. (1994) 36:309–316.
   PubMed Web of Science ®Google Scholar