^ a b c d e f g h i j k l m n o p q r s t u v w x y z aa ab ac Lapin, I.^ a b c d e f g h i j k l m n o p q r s t u Ozon Pharm, Fenibut (PDF), retrieved 15 September 2017.The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. 'Phenibut (4-amino-3-phenyl-butyric acid): Availability, prevalence of use, desired effects and acute toxicity'. ^ a b c d e f g h i j k l m n o p q r s t u v w x y z Owen DR, Wood DM, Archer JR, Dargan PI (2016).Īs of 14 November 2018, Hungary added phenibut and 10 other items to its New Psychoactive Substances ban list.
For this reason, the actions of phenibut as a α 2δ subunit-containing voltage-gated calcium channel blocker or gabapentinoid may be its true primary mechanism of action, and this may explain the differences between phenibut and its close relative baclofen (which, in contrast, has essentially insignificant activity as a gabapentinoid K i = 6 μM for the GABA B receptor and K i = 156 μM for α 2δ subunit-containing VDCCs, or a 26-fold difference in affinity). As such, based on the results of this study, phenibut would appear to have much greater potency in its interactions with α 2δ subunit-containing VDCCs than with the GABA B receptor (between 5- to 10-fold). Moreover, ( R)-phenibut possesses 4-fold greater affinity for this site than for the GABA B receptor (K i = 92 μM), while ( S)-phenibut does not bind significantly to the GABA B receptor (K i > 1 mM). Both ( R)-phenibut and ( S)-phenibut display this action with similar affinity (K i = 23 and 39 μM, respectively). Phenibut also binds to and blocks α 2δ subunit-containing VDCCs, similarly to gabapentin and pregabalin, and hence is a gabapentinoid.
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