Methiothepin

Methiothepin (Metitepine; Ro 8-6837) is a potent and non-selective 5-HT2 receptor antagonist, with pKds of 7.10 (5-HT1A), 7.28 (5HT1B), 7.56 (5HT1C), 6.99 (5HT1D), 7.0 (5-HT5A), 7.8 (5-HT5B), 8.74 (5-HT6), and 8.99 (5-HT7), and pKis of 8.50 (5HT2A), 8.68 (5HT2B), and 8.35 (5HT2C) .

Product Specifications

CAS Number

[20229-30-5]

Product Name Alternative

Metitepine; Ro 8-6837

UNSPSC

12352005

Hazard Statement

H302-H315-H319-H335

Target

5-HT Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/Methiothepin.html

Smiles

CN1CCN(C2CC3=CC=CC=C3SC4=CC=C(SC)C=C24)CC1

Molecular Formula

C20H24N2S2

Molecular Weight

356.55

Precautions

P261-P280-P302+P352

References & Citations

[1]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.|[2]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.|[3]Hoyer D, et al. International Union of Pharmacology classification of receptors for 5-hydroxytryptamine (Serotonin) . Pharmacol Rev. 1994 Jun;46 (2) :157-203.