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Methiothepin

Methiothepin structure

Methiothepin 

structure
  • CAS No:

    20229-30-5

  • Formula:

    C20H24N2S2

  • Chemical Name:

    Methiothepin

  • Synonyms:

    Piperazine,1-[10,11-dihydro-8-(methylthio)dibenzo[b,f]thiepin-10-yl]-4-methyl-;Dibenzo[b,f]thiepin,piperazine deriv.;1-[10,11-Dihydro-8-(methylthio)dibenzo[b,f]thiepin-10-yl]-4-methylpiperazine;Methiothepine;Methiothepin;Ro 8-6837;Metitepine;Methiotepin;101395-30-6

Description

Methiothepin is a dibenzothiepine that is 10,11-dihydrodibenzo[b,f]thiepine bearing additional methylthio and 4-methylpiperazin-1-yl substituents at positions 8 and 10 respectively. Potent 5-HT2 antagonist, also active as 5-HT1 antagonist. Differentiates 5-HT1D sub-types. Also displays affinity for rodent 5-HT5B, 5-HT5A, 5-HT7 and 5-HT6 receptors (pK1 values are 6.6, 7.0, 8.4 and 8.7 respectively). It has a role as an antipsychotic agent, a dopaminergic antagonist, a serotonergic antagonist and a geroprotector. It is a N-alkylpiperazine, a dibenzothiepine, an aryl sulfide and a tertiary amino compound. It is a conjugate base of a methiothepin(2+).|A serotonin receptor antagonist in the CENTRAL NERVOUS SYSTEM used as an antipsychotic.

Methiothepin Basic Attributes

452.65400

356.55

DTXSID2044000

2934999090

Characteristics

119.83000

4.86490

1.25g/cm3

80-82 °C @ Solvent: Ethanol

462.9ºC at 760mmHg

233.8ºC

Safety Information

3

|Warning|H315 (100%): Causes skin irritation [Warning Skin corrosion/irritation]|P261, P264, P271, P280, P302+P352, P304+P340, P305+P351+P338, P312, P321, P332+P313, P337+P313, P362, P403+P233, P405, and P501|Aggregated GHS information provided by 90 companies from 2 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Drug Information

Agents that control agitated psychotic behavior, alleviate acute psychotic states, reduce psychotic symptoms, and exert a quieting effect. They are used in SCHIZOPHRENIA; senile dementia; transient psychosis following surgery; or MYOCARDIAL INFARCTION; etc. These drugs are often referred to as neuroleptics alluding to the tendency to produce neurological side effects, but not all antipsychotics are likely to produce such effects. Many of these drugs may also be effective against nausea, emesis, and pruritus. (See all compounds classified as Antipsychotic Agents.)|Drugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or SEROTONIN RECEPTOR AGONISTS. (See all compounds classified as Serotonin Antagonists.)

Maleate, Methiothepin

Methiothepin Use and Manufacturing

5HT1&2 receptor antagonist

Computed Properties

Molecular Weight:356.6
XLogP3:4.2
Hydrogen Bond Acceptor Count:4
Rotatable Bond Count:2
Exact Mass:356.13809112
Monoisotopic Mass:356.13809112
Topological Polar Surface Area:57.1
Heavy Atom Count:24
Complexity:410
Undefined Atom Stereocenter Count:1
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

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