Methiothepin mesylate structure
|
Common Name | Methiothepin mesylate | ||
---|---|---|---|---|
CAS Number | 74611-28-2 | Molecular Weight | 452.65400 | |
Density | N/A | Boiling Point | N/A | |
Molecular Formula | C21H28N2O3S3 | Melting Point | N/A | |
MSDS | Chinese USA | Flash Point | N/A |
Use of Methiothepin mesylateMethiothepin 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). |
Name | methanesulfonic acid,1-methyl-4-(3-methylsulfanyl-5,6-dihydrobenzo[b][1]benzothiepin-5-yl)piperazine |
---|---|
Synonym | More Synonyms |
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 | |
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 |
Molecular Formula | C21H28N2O3S3 |
---|---|
Molecular Weight | 452.65400 |
Exact Mass | 452.12600 |
PSA | 119.83000 |
LogP | 4.86490 |
Storage condition | 2-8℃ |
Personal Protective Equipment | Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter |
---|---|
RIDADR | NONH for all modes of transport |
Characterization of the commercially-available fluorescent chloroquine-BODIPY conjugate, LynxTag-CQGREEN, as a marker for chloroquine resistance and uptake in a 96-well plate assay.
PLoS ONE 9(10) , e110800, (2014) 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... |
|
Functional, endogenously expressed 5-hydroxytryptamine 5-ht7 receptors in human vascular smooth muscle cells.
Br. J. Pharmacol. 117 , 993-994, (1996) 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... |
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 |