Methiothepin mesylate

Names

[ Name ]:
Methiothepin mesylate

[Synonym ]:
Methiothepin mesylate salt
Methiothepin methanesulfonate
Methiothepin mesylate
Metitepine mesylate salt
Piperazine,1-(10,11-dihydro-8-(methylthio)dibenzo(b,f)thiepin-10-yl)-4-methyl-,methanesulfonate
1-[10,11-Dihydro-8-(methylthio)dibenzo[b,f]thiepin-10-yl]-4-methylpiperazine mesylate salt

Biological Activity

[Description]:

Methiothepin mesylate 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).

[Related Catalog]:

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

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

Research Areas >> Neurological Disease

[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].

[References]

[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.

[Related Small Molecules]

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₁H₂₈N₂O₃S₃

[ Molecular Weight ]:
452.65400

[ Exact Mass ]:
452.12600

[ PSA ]:
119.83000

[ LogP ]:
4.86490

[ Storage condition ]:
2-8℃

MSDS

Click to get detail MSDS

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ RIDADR ]:
NONH for all modes of transport

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Chloroquine was a cheap, extremely effective drug against Plasmodium falciparum until resistance arose. One approach to reversing resistance is the inhibition of chloroquine efflux from its site of ac...

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Human uterine artery smooth muscle cells in culture were shown to express constitutively both 5-ht7 receptor mRNA and 5-ht7-like receptors functionally linked to cyclic AMP formation. 5-Carboxamidotry...

Characterisation of 5-HT receptors in human coronary arteries by molecular and pharmacological techniques.

Eur. J. Pharmacol. 372 , 49-56, (1999)

5-Hydroxytryptamine (5-HT) can produce both vasoconstrictor and vasorelaxant effects in human coronary arteries and the response to 5-HT can be influenced by the presence of disease. The aim of the pr...

Related Compounds

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