20229-30-5

5HT1&2 receptor antagonist

Methiothepin Maleate exhibits anticonvulsant property and it is able to suppress pentylenetetrazol induced fos expression in zebrafish. In addition, Methiothepin Maleate is a 5-HT antagonist.

ChEBI: 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+).

Potent 5-HT 2 antagonist, also active as 5-HT 1 antagonist. Differentiates 5-HT 1D sub-types. Also displays affinity for rodent 5-HT 5B , 5-HT 5A , 5-HT 7 and 5-HT 6 receptors (pK 1 values are 6.6, 7.0, 8.4 and 8.7 respectively).