SB 203186 hydrochloride

Names

[ CAS No. ]:
207572-69-8

[ Name ]:
SB 203186 hydrochloride

[Synonym ]:
2-(Piperidin-1-yl)ethyl 1H-indole-3-carboxylate hydrochloride (1:1)
2-(1-Piperidinyl)ethyl 1H-indole-3-carboxylate hydrochloride (1:1)
1H-Indole-3-carboxylic acid, 2-(1-piperidinyl)ethyl ester, hydrochloride (1:1)
SB-203186 hydrochloride

Biological Activity

[Description]:

SB-203186 hydrochloride is a potent and competitive 5-HT4 antagonist. SB-203186 hydrochloride antagonizes the 5-HT4 receptor-mediated relaxations of the carbachol-contracted rat isolated oesophagus against 5-HT with pKB values of 10.9 (rat oesophagus), 9.5 (guinea-pig ileum), and 9.0 (human colon) respectively[1][2][3].

[Related Catalog]:

Research Areas >> Cardiovascular Disease

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

[Target]

pKB: 10.9 (5-HT4 in rat oesophagus), 9.5 (5-HT4 in guinea-pig ileum), and 9.0 (5-HT4 in human colon)[3].

[In Vitro]

SB-203186 (0.1-3mg/kg, i.v.) surmountably antagonised 5-HT-evoked tachycardia in anaesthetized Yucatan minipigs or new-born Camborough piglets with similar potency[1]. Pretreatment with SB-203186 (10 μM) enhances the 5-HT-induced contractions of the antral strips[2].

[In Vivo]

Intraduodenally administered SB-203186 (0.3-3 mg/kg) to new-born Camborough piglets produced blockade of 5-HT-evoked tachycardia which was maximal after 20 min and lasted for more than 3 h with 0.3 mg/kg[1].

[References]

[1]. S G Parker, et al. Blockade of human and porcine myocardial 5-HT4 receptors by SB 203186. Naunyn Schmiedebergs Arch Pharmacol. 1995 Dec;353(1):28-35.

[2]. Tohru Komada, et al. Pharmacological characterization of 5-Hydroxytryptamine-receptor subtypes in circular muscle from the rat stomach. Biol Pharm Bull. 2007 Mar;30(3):508-13.

[3]. P G McLean, et al. 5-HT4 receptor antagonist affinities of SB207710, SB205008, and SB203186 in the human colon, rat oesophagus, and guinea-pig ileum peristaltic reflex. Naunyn Schmiedebergs Arch Pharmacol. 1995 Aug;352(2):132-40.