An GABAB receptor-selective antagonist (3-aminopropyl)(diethoxymethyl)phosphinic acid (CGP35348) inhibited the antidepressant and antinociceptive effects of R-phenibut, as well as locomotor depressing activity of R-phenibut in open field test in vivo. Both R-phenibut and racemic phenibut showed analgesic activity in the tail-flick test with R-phenibut being slightly more active. In the forced swimming test, at a dose of 100 mg/kg only R-phenibut significantly decreased immobility time. In contrast, R-phenibut turned out to be two times more potent than racemic phenibut in most of the tests. In pharmacological tests of locomotor activity, antidepressant and pain effects, S-phenibut was inactive in doses up to 500 mg/kg. The aim of the present study was to compare the effects of racemic phenibut and its optical isomers in pharmacological tests and GABAB receptor binding studies. Received 12 June 2007 received in revised form 14 December 2007 accepted 14 January 2008 Available online 26 January 2008Ībstract Phenibut (3-phenyl-4-aminobutyric acid) is a GABA (γ-aminobutyric acid)-mimetic psychotropic drug which is clinically used in its racemic form. 21, Riga, LV-1006, Latvia b University of Latvia, Sarlotes St. Latvian Institute of Organic Synthesis, Aizkraukles St. Available online at European Journal of Pharmacology 583 (2008) 128 – 134 Comparative pharmacological activity of optical isomers of phenibut Maija Dambrova a,⁎, Liga Zvejniece a,b, Edgars Liepinsh a,b, Helena Cirule a, Olga Zharkova a, Grigory Veinberg a, Ivars Kalvinsh a a
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