Title : Probing α4βδ GABAA receptor heterogeneity: differential regional effects of a functionally selective α4β1δ/α4β3δ receptor agonist on tonic and phasic inhibition in rat brain.

Pub. Date : 2014 Dec 3

PMID : 25471566






1 Functional Relationships(s)
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1 Whereas Thio-THIP displayed weak antagonist activity at alpha1,2,5beta2,3gamma2S and rho1 GABAARs and partial agonism at alpha6beta2,3delta GABAARs expressed in Xenopus oocytes, the pronounced agonism exhibited by the compound at alpha4beta1delta and alpha4beta3delta GABAARs was contrasted by its negligible activity at the alpha4beta2delta subtype. Thio-THIP MGC75582, possible similarity to act2 S homeolog Xenopus laevis