BW 723C86 hydrochloride - CAS 160521-72-2
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
Molecular Weight:
5-HT Receptor
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
≥99% by HPLC
BW723C86; BW-723-C-86; BW 723 C 86; BW-723C86; BW 723C86; α-methyl-5-(2-thienylmethoxy)-1H-indole-3-ethanamine hydrochloride
the treatment of CNS disorders as epilepsy, migraine and feeding disorders
Canonical SMILES:
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.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related 5-HT Receptor Products

CAS 299433-10-6 NPS ALX Compound 4a dihydrochloride

NPS ALX Compound 4a dihydrochloride
(CAS: 299433-10-6)

NPS ALX Compound 4a dihydrochloride is a 5-HT6 antagonist with IC50 value of 7.2 nM.

CAS 1977-08-8 Isoclozapine

(CAS: 1977-08-8)

Isoclozapine is a 2-Cl analogue of clozapine as a typical antipsychotic.

Elzasonan hydrochloride
(CAS: 220322-05-4)

Elzasonan, also called as CP 448187, exhibits potent and selective antagonism of 5-HT1B receptors in vitro, and preclinical in vivo studies demonstrate enhanced...

CAS 1217474-40-2 NAS-181

(CAS: 1217474-40-2)

NAS-181 is a 5-HT1B receptor antagonist with Ki value of 47 nM. It can increase synthesis and metabolism of 5-HT in the brain following systemic administration ...

Iloperidone hydrochloride
(CAS: 1299470-39-5)

The hydrochloride salt form of Iloperidone which is a antagonist of both D2 and 5-HT2 receptor and has been commonly used against schizophrenia. IC50: 10-100 nm...

CAS 1135280-78-2 Altanserin hydrochloride

Altanserin hydrochloride
(CAS: 1135280-78-2)

Altanserin hydrochloride is the hydrochloride salt of altanserin, which is a selective and potent 5-HT2A receptor antagonist with Ki value of 0.13 nM. It is cen...

CAS 154323-57-6 Almotriptan

(CAS: 154323-57-6)

Almotriptan, also called as Almogran, is a agonist with high and specific affinity for 5-HT1B/1D receptors. developed by Almirall Prodesfarma for the acute trea...

CAS 1217756-94-9 LY 344864 hydrochloride

LY 344864 hydrochloride
(CAS: 1217756-94-9)

LY 344864 hydrochloride is a 5-HT1F receptor agonist with EC50 value of 3 nM.

Chemical Structure

CAS 160521-72-2 BW 723C86 hydrochloride

Quick Inquiry

Verification code

Featured Items