135938-17-9
Chemical Structure
SB-203186
- CAS No.: 135938-17-9
- Formula:C16H20N2O2
- Molecular Weight:272.34
IUPAC Name: 2-(piperidin-1-yl)ethyl 1H-indole-3-carboxylate
InChIKey: YGKPIROTKVQCCU-UHFFFAOYSA-N
SMILES: O=C(C1=CNC2=C1C=CC=C2)OCCN3CCCCC3
Biological Activity: SB-203186 is a highly selective 5-HT4 receptor antagonist. SB-203186 exhibits a potent competitive antagonistic effect, with its pKB value being 8.3 in the isolated right atrium model of piglets. SB-203186 can dose-dependently shift the 5-HT-induced tachycardia curve to the right, and does not inhibit the maximum response. SB-203186 is an efficient 5-HT₄ antagonist in pig and human atria, but has no significant inhibitory effect in rat atria. SB-203186 can be used for the study of diseases such as arrhythmias and abnormal myocardial contraction[1][2].
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SB-203186 | SB-203186 is a highly selective 5-HT4 receptor antagonist. SB-203186 exhibits a potent competitive antagonistic effect, with its pKB value being 8.3 in the isolated right atrium model of piglets. SB-203186 can dose-dependently shift the 5-HT-induced tachycardia curve to the right, and does not inhibit the maximum response. SB-203186 is an efficient 5-HT₄ antagonist in pig and human atria, but has no significant inhibitory effect in rat atria. SB-203186 can be used for the study of diseases such as arrhythmias and abnormal myocardial contraction. | |||||||||||||||||||||
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References
- [1]. Medhurst AD, Kaumann AJ. Characterization of the 5‐HT4 receptor mediating tachycardia in piglet isolated right atrium. British journal of pharmacology. 1993 Nov;110(3):1023-30. [Content Brief]
- [2]. Läer S, et al. Receptor mechanisms involved in the 5‐HT‐induced inotropic action in the rat isolated atrium. British journal of pharmacology. 1998 Mar;123(6):1182-8.
