17-PA

Uses

17-PA is an antagonist of neurosteroid GABA potentiation.

Biological Activity

Selective antagonist of neurosteroid potentiation and direct gating of GABA A receptors. Selectively reduces the effects of 5 α -reduced steroids compared to 5 β -reduced steroids and displays no effect on potentiation evoked by barbiturates and benzodiazepines. Attenuates 3 α ,5 α -THP-induced loss of righting reflex and total sleep time following i.c.v administration in rats.

Enzyme inhibitor

This selective neurosteroid antagonist (FW = 350.54 g/mol; CAS 694438- 95-4; Soluble to 25 mM in DMSO and to 50 mM in ethanol), also known as 17-PA, targets neurosteroid potentiation and directly gates GABAA receptors. 17-PA inhibition was also useful in demonstrating that ethanol modulates the interaction of the endogenous neurosteroid allopregnanolone with the α1β2γ2L GABAA receptor. 17-PA selectively reduces the effects of 5α-reduced steroids compared to 5β-reduced steroids and displays no effect on potentiation evoked by barbiturates and benzodiazepines. It also attenuates 3α,5α-THP-induced loss of righting reflex and total sleep time, following intracerebroventricular administration in rats.