BW 723C86 hydrochloride - CAS 160521-72-2
Category: Inhibitor
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Molecular Formula:
C16H18N2OS.HCl
Molecular Weight:
322.85
COA:
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Targets:
5-HT Receptor
Description:
BW 723C86 hydrochloride is a selective 5-HT2B receptor agonist used for the treatment of certain CNS disorders, such as epilepsy, migraine and feeding disorders.
Brife Description:
5-HT2B receptor agonist
Purity:
≥99% by HPLC
Synonyms:
BW723C86; BW-723-C-86; BW 723 C 86; BW-723C86; BW 723C86; α-methyl-5-(2-thienylmethoxy)-1H-indole-3-ethanamine hydrochloride
MSDS:
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Application:
the treatment of CNS disorders as epilepsy, migraine and feeding disorders
InChIKey:
PYJBJMIBANAOFJ-UHFFFAOYSA-N
InChI:
InChI=1S/C16H18N2OS.ClH/c1-11(17)7-12-9-18-16-5-4-13(8-15(12)16)19-10-14-3-2-6-20-14;/h2-6,8-9,11,18H,7,10,17H2,1H3;1H
Canonical SMILES:
CC(CC1=CNC2=C1C=C(C=C2)OCC3=CC=CS3)N.Cl
1.Characterization of phospholipase C activity at h5-HT2C compared with h5-HT2B receptors: influence of novel ligands upon membrane-bound levels of [3H]phosphatidylinositols.
Cussac D;Newman-Tancredi A;Quentric Y;Carpentier N;Poissonnet G;Parmentier JG;Goldstein S;Millan MJ Naunyn Schmiedebergs Arch Pharmacol. 2002 Mar;365(3):242-52. Epub 2002 Jan 16.
Employing a novel, rapid and sensitive method for evaluation of phospholipase C (PLC) activity, the present study characterized the actions of diverse agonists and antagonists at human (h)5-HT2C receptors expressed in Chinese Hamster Ovary (CHO) cells. In addition, affinities and efficacies at these sites were compared with those obtained at h5-HT2B receptors.5-HT elicited a robust and rapid reduction in levels of the pre-labelled, membrane-bound substrate of PLC, [3H]phosphatidylinositols ([3H]PI). The time-course of [3H]PI depletion paralleled that of [3H]inositol phosphate ([3H]IP) accumulation, as determined by conventional anion exchange chromatography. Inactivation of h5-HT2C receptors with the alkylating agent, N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline (EEDQ), revealed a large receptor reserve, with half-maximal PLC activation induced by a concentration of 5-HT occupying only 5% of sites. In analogy to 5-HT ( Emax=100%), DOI, MK212 and mCPP, as well as the novel ligands, Ro600332, Ro600175 and BW723C86, showed "full" efficacy at h5-HT2C sites. Their efficacies were similar at h5-HT2B sites, with the exception of mCPP and MK212, which acted as partial agonists. Further, lisuride and Ro600869 behaved as partial agonists and antagonists at h5-HT2C and h5-HT2B receptors, respectively.
2.Stimulation of growth hormone release by 5-hydroxytryptamine (5-HT) in cultured rat anterior pituitary cell aggregates: evidence for mediation by 5-HT2B, 5-HT7, 5-HT1B, and ketanserin-sensitive receptors.
Papageorgiou A;Denef C Endocrinology. 2007 Sep;148(9):4509-22. Epub 2007 Jun 21.
5-Hydroxytryptamine (5-HT) promotes the release of GH by a hypothalamic site of action. The present study explores a putative pituitary action in a perifused rat anterior pituitary aggregate cell culture system. In aggregates cultured with 1 nM estradiol for expression of the 5-HT4, -5, and -6 receptor (R), 5-HT promptly stimulated GH secretion with a dose dependency between 1 and 10 nM. The effect of 5-HT was partially blocked by methiothepin and methysergide; by SB-206553, a 5-HTR2B/C antagonist; SB-269970, a 5-HTR7/5A antagonist; and SB-224289, a 5-HTR1B antagonist. The GH response was fully blocked by combined administration of SB-206553+SB-269970 and SB-206553+ketanserin but not by SB-206553+spiperone. Culturing the aggregates without estradiol diminished the magnitude of the GH response to 5-HT as well as the impact of 5-HTR7/5 blockade on the response. Basal GH release was stimulated by the 5-HTR2 agonists 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane, m-chlorophenyl piperazine, and alpha-methyl 5-HT; 5-carboxytryptamine (agonist at 5-HTR1, -5, and -7); tryptamine (preferential 5-HTR7 agonist); and the selective 5-HTR1B agonist CP93129 but not the 5-HTR1A agonists 7-(dipropylamino)tetralin-1-ol-8-hydroxy-2-(di-n-propylamino)tetralin and the 5-HTR1B/D agonist sumatriptan.
3.Vasoconstrictor responses to 5-hydroxytryptamine in the autoperfused hindquarters of spontaneously hypertensive rats.
Calama E;Morán A;Ortiz de Urbina AV;Martín ML;San Román L Pharmacology. 2004 Jun;71(2):66-72.
In this work we studied the responses and receptors involved in the effects of intra-arterial 5-hydroxytryptamine (5-HT) in the in situ autoperfused hindquarters of spontaneously hypertensive rats (SHR). Intra-arterial administration of the highest doses (50-1,000 ng/kg) produced a vasoconstrictor effect that was inhibited by ritanserin (a selective 5-HT2 receptor antagonist), SB 206553 (a selective 5-HT(2B/2C) receptor antagonist) and spiperone (a nonspecific 5-HT(1/2A) receptor antagonist), and was mimicked by alpha-methyl-5-HT (a selective 5-HT2 receptor agonist) and m-CPP (a selective 5-HT2C receptor agonist), but not by the intra-arterial administration of BW 723C86, a selective 5HT2B receptor agonist. SB 206553 and spiperone inhibited alpha-methyl-5HT-induced vasoconstriction in the hindquarters of SHR. Our data suggest that the vasoconstrictor response induced by 5-HT in the autoperfused hindquarters of SHR is mainly mediated by the activation of 5-HT2A and 5-HT2C receptors.
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CAS 160521-72-2 BW 723C86 hydrochloride

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