Title : Serotonin-induced hypersensitivity via inhibition of catechol O-methyltransferase activity.

Pub. Date : 2012 Apr 13

PMID : 22500608






5 Functional Relationships(s)
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1 Serotonin-induced hypersensitivity via inhibition of catechol O-methyltransferase activity. Serotonin catechol-O-methyltransferase Homo sapiens
2 Here we show that serotonin also inhibits catechol O-methyltransferase (COMT), an enzyme that contributes to modultion the perception of pain, via non-competitive binding to the site bound by catechol substrates with a binding affinity comparable to the binding affinity of catechol itself (K(i) = 44 muM). Serotonin catechol-O-methyltransferase Homo sapiens
3 Here we show that serotonin also inhibits catechol O-methyltransferase (COMT), an enzyme that contributes to modultion the perception of pain, via non-competitive binding to the site bound by catechol substrates with a binding affinity comparable to the binding affinity of catechol itself (K(i) = 44 muM). Serotonin catechol-O-methyltransferase Homo sapiens
4 Binding of serotonin to the catalytic site inhibits the access of SAM, thus preventing methylation of COMT substrates. Serotonin catechol-O-methyltransferase Homo sapiens
5 Our results suggest that inhibition of COMT via serotonin binding contributes to pain hypersensitivity, providing additional strategies for the treatment of clinical pain conditions. Serotonin catechol-O-methyltransferase Homo sapiens