Stereoselective blockade at the 5-HT autoreceptor and inhibition of radioligand binding to central 5-HT recognition sites by the optical isomers of methiothepin

Add time:09/02/2019    Source:sciencedirect.com

The enantiomers of the 5-HT autoreceptor antagonist methiothepin have been prepared and their activity as antagonists of the 5-HT autoreceptor and at the 5-HT recognition sites present in the frontal cortex of the rat have been evaluated. At the 5-HT autoreceptor, the order of potency as antagonists of 5-HT was (+)methiothepin (apparent pA2 5.95) < (±)methiothepin (apparent pA2 6.62) ⩽(−)methiothepin (apparent pA2 6.81). At the 5-HT2 recognition site, the isomeric forms of methiothepin were potent (pIC50 ∼ 8.2) and equiactive. At the subtypes of the 5-HT, recognition sites, similar concentrations to those blocking the autoreceptor were effective and (+)methiothepin was less active than (−)methiothepin. It is concluded that the chiral association of methiothepin with the 5-HT autoreceptor provides further evidence for a pharmacological similarity between this receptor and the 5-HTB subtype of the 5-HT1 recognition site.

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