Methiothepin mesylate
CAS No. : 74611-28-2

Methiothepin mesylate
Cat. No. : CS-0030713
M. Wt. : 452.65
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  • Data Sheet

  • Introduction

  • SDS

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Name: Methiothepin mesylate; Metitepine mesylate; Ro 8-6837 mesylate
Cat. No. : CS-0030713
CAS No. : 74611-28-2
Formula: C21H28N2O3S3
M. Wt. : 452.65
Solubility: DMSO: ≥ 125 mg/mL

Activity:

Methiothepin mesylate is a potent and non-selective 5-HT2 receptor antagonist, and also acts as an antagonist at 5-HT1, 5-HT5A, 5-HT5B, 5-HT6, and 5-HT7, with pKds of 7.10, 7.28, 7.56, 6.99, 7.0, 7.8, 8.74, and 8.99 for 5-HT1A, 5HT1B, 5HT1C, 5HT1D, 5-HT5A, 5-HT5B, 5-HT6, and 5-HT7 and pKis of 8.50, 8.68, and 8.35 for 5HT2A, 5HT2B, 5HT2C. IC50 & Target: pKd: 7.10 (5-HT1A), 7.28 (5HT1B), 7.56 (5HT1C), 6.99 (5HT1D)[1], 7.0 (5-HT5A), 7.8 (5-HT5B), 8.74 (5-HT6), 8.99 (5-HT7)[3]
pKi: 8.50 (5-HT2A), 8.68 (5-HT2B), 8.35 (5-HT2C)[2] In Vitro: Methiothepin mesylate is a 5-HT receptor antagonist, with pKds of 7.10, 7.28, 7.56, and 6.99 for 5-HT1A, 5HT1B, 5HT1C, 5HT1D[1]. Methiothepin mesylate also shows pKds of 7.0, 7.8, 8.74, and 8.99 for 5-HT5A, 5-HT5B, 5-HT6, and 5-HT7, respectively[2]. Methiothepin exhibits high affinity at 5-HT2A, 5HT2B, and 5HT2C with pKis of 8.50, 8.68, and 8.35, respectively[3].

Protocol:

References:

Hoyer D, et al. International Union of Pharmacology classification of receptors for 5-hydroxytryptamine (Serotonin). Pharmacol Rev. 1994 Jun;46(2):157-203.

Schoeffter P, et al. 5-Hydroxytryptamine (5-HT)-induced endothelium-dependent relaxation of pig coronary arteries is mediated by 5-HT receptors similar to the 5-HT1D receptor subtype. J Pharmacol Exp Ther. 1990 Jan;252(1):387-95.

Knight AR, et al. Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors. Naunyn Schmiedebergs Arch Pharmacol. 2004 Aug;370(2):114-23. Epub 2004 Jul 30.

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