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207572-69-8

207572-69-8 structure
207572-69-8 structure
  • Name: SB 203186 hydrochloride
  • Chemical Name: 2-(1-Piperidinyl)ethyl 1H-indole-3-carboxylate hydrochloride (1:1)
  • CAS Number: 207572-69-8
  • Molecular Formula: C16H21ClN2O2
  • Molecular Weight: 308.803
  • Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
  • Create Date: 2018-06-30 03:40:08
  • Modify Date: 2024-01-02 21:52:02
  • 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].

Name 2-(1-Piperidinyl)ethyl 1H-indole-3-carboxylate hydrochloride (1:1)
Synonyms 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
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
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.

Molecular Formula C16H21ClN2O2
Molecular Weight 308.803
Exact Mass 308.129150
Hazard Codes Xi
Risk Phrases 36/37/38
Safety Phrases 26-36