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Description: AZD-6280 is a novel, potent and selective GABAA(alpha2/3) receptor modulator, used for treatment of generalized anxiety disorder. Following administration of AZD6280 at 10?mg and 40?mg doses, prolactin levels increased significantly compared with placebo (difference 42.0%, 19.8%, and 32.8%, respectively), suggesting that the alpha2 and/or alpha3 receptor subtypes are involved in GABAergic modulation of prolactin secretion, although possible roles of the alpha1 and alpha5 receptor subtypes are not excluded. The increases in prolactin levels after administration of AZD7325 at 2?mg and 10?mg doses (difference 7.6% and 10.5%, respectively) did not reach statistical significance, suggesting that doses of AZD7325 or intrinsic efficacy at the alpha2 and alpha3 receptor subtypes may have been too low.
References: Clin Pharmacol Drug Dev. 2015 Mar; 4(2):149-54.
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