Drugs online research references
Farmaco. 1991 Dec;46(12):1435-47.
Synthesis and 5-HT receptors binding studies of some 3-substituted-2-(4-methyl-1-piperazinyl)-4-phenylquinolines.
Anzini M, Cappelli A, Vomero S, Campiani G, Cagnotto A, Skorupska M.
Dipartimento Farmaco Chimico Tecnologico-Universita, Siena, Italy.
The syntheses of some 3-substituted-2-(4-methyl-1-piperazinyl)-4-phenylquinolines are reported. The title compounds were tested for their potential activities on 5-HT receptor subtypes and 5-HT uptake site; compounds 4b-d showed micromolar affinity for 5-HT3 and 5-HT uptake site.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=1668253&dopt=Abstract
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Eur J Pharmacol. 1991 Feb 7;193(2):145-52.
Methylenedioxymethamphetamine induces spontaneous tail-flicks in the rat via 5-HT1A receptors.
Millan MJ, Colpaert FC.
Neurobiology Division, Fondax-Groupe de Recherche Servier, Puteaux, France.
In rats lightly restrained in horizontal cylinders, (+/-)-3,4-methylenedioxymethamphetamine (MDMA) dose dependently (0.16-10.0 mg/kg, s.c.) elicited spontaneous tail-flicks; that is, tail-flicks in the absence of extraneous stimulation. In contrast, amphetamine over a similar dose-range was inactive. Selective inhibitors of 5-hydroxytryptamine (5-HT) uptake and carrier-mediated 5-HT release, paroxetine and citalopram, did not induce spontaneous tail-flicks themselves and blocked those induced by MDMA. In distinction, maprotiline and bupropion, selective inhibitors of noradrenaline and dopamine uptake, respectively, failed to modify the action of MDMA. Spontaneous tail-flicks elicited by MDMA were unaffected by the selective 5-HT3 receptor antagonists, ICS 205,930 and GR 38032F. They were attenuated by the mixed 5-HT1/5-HT2 receptor antagonist, methiotepin, the mixed 5-HT1A/5-HT1B receptor antagonist, (-)-alprenolol and the mixed 5-HT1A/5-HT2 receptor antagonist, spiperone, but not by the selective 5-HT1C/5-HT2 receptor antagonists, ritanserin, ICI 169,369 and ketanserin. The novel 5-HT1A receptor antagonists, BMY 7378 and NAN-190, each abolished MDMA-evoked spontaneous tail-flicks. Selective D1, D2, alpha 1, alpha 2, beta 1 and beta 2 antagonists had little influence upon induction of spontaneous tail-flicks by MDMA. These data indicate that MDMA evokes spontaneous tail-flicks in the rat via a release of 5-HT which acts at 5-HT1A receptors. Thus, 5-HT1A receptors appear to be involved in the acute functional actions of MDMA.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=1675609&dopt=Abstract
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Neuropharmacology. 1991 Jun;30(6):607-16.
Effect of paroxetine, a selective 5-hydroxytryptamine uptake inhibitor, on beta-adrenoceptors in rat brain: autoradiographic and functional studies.
Nelson DR, Pratt GD, Palmer KJ, Johnson AM, Bowery NG.
SmithKline Beecham Pharmaceuticals, Research and Development, Harlow, Essex.
Quantitative receptor autoradiography was used to investigate the effects of paroxetine (8.3 mg/kg), amitriptyline (26 mg/kg) and desipramine (17 mg/kg), administered daily in the drinking water for 21 days, on the number of beta 1- and beta 2-adrenoceptors in the cortex of the rat. In addition, the effect of these drugs on the function of beta-adrenoceptors was examined by measuring noradrenaline- and isoprenaline-stimulated production of cyclic AMP in slices of cortex. Paroxetine did not alter the number of cortical beta 1 or beta 2-adrenoceptors nor did it induce any functional changes in beta-adrenoceptor-linked adenylyl cyclase. In contrast, desipramine caused a significant reduction in the density of beta 1-adrenoceptors and in the sensitivity of both noradrenaline and isoprenaline-stimulated adenylyl cyclase. Although amitriptyline significantly reduced the number of beta 1-adrenoceptors in cortical membranes, no such changes could be detected by autoradiography. It is apparent from these and other studies, that the ability of antidepressants to down-regulate central beta-adrenoceptors is not a property shared by all antidepressants. In particular, the more potent and selective inhibitors of the uptake of 5-HT, such as paroxetine, appear to be devoid of effects on this receptor system.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=1681445&dopt=Abstract
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