Chemical Name:6,7-Dimethyl-2,4-di-1-pyrrolidinyl-7H-pyrrolo[2,3-d]pyr
imidine hydrochloride
Biological Activity:
Positive allosteric modulator of GABAA
receptors. Enhances GABA-induced Cl- currents in the α1β2γ2, α3β2γ2 and
α6β2γ2
subtypes. Causes sedation in vivo following i.v. administration without losing
"righting reflex". Also displays antioxidant activity.
Bundyet al
(1995) Synthesis of novel 2,4-diaminopyrrolo-[2,3-d]pyrimidines with
antioxidant, neuroprotective, and antiasthma activity. J.Med.Chem. 38
4161. Haesooket al (1995) U-89843A is a novel allosteric
modulator of γ-aminobutyric
acidA receptors. J.Pharmacol.Exp.Ther. 275 1390. Rohnet al (1996) Inhibition of Ca2+-pump ATPase and the Na+/K+-pump
ATPase by iron-generated free radicals. Biochem.Pharmacol. 51
471.
Selective antagonist of neuro-steroid potentiation and direct gating of GABAA receptors. Selectively reduces the effects of 5α-reduced steroids compared to 5β-reduced steroids & displays no effect on potentiation evoked by barbiturates & benzodiazepines. Attenuates 3α,5α-THP-induced loss of righting reflex and total sleep time following i.c.v administration in rats.