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Guvacine is an amino acid found in A. catechu (Betel nut).1 It competitively inhibits GABA uptake (IC50 = 10 μM; Ki = 14 μM) in rat hippocampal brain slices.1,2 In vivo, guvacine, at doses ranging from 50-100 mg/kg, decreases spontaneous activity in mice.1 Administration of guvacine also decreases tail flick reaction time in a rat model of morphine analgesia.3
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1. Betel nut constituents as inhibitors of γ-
2. Structure-
3. Nipecotic acid and guvacine antagonism on morphine analgesia in rats. Pharmacol. Res. Commun. 11(8), 657-662 (1979).