Asenapine is a novel psychopharmacologic agent under development for the treatment of schizophrenia and bipolar disorder. We determined and compared the human receptor binding affinities and functional characteristics of asenapine and several antipsychotic drugs. Compounds were tested under comparable assay conditions using cloned human receptors. In comparison with the antipsychotics, asenapine showed high affinity and a different rank order of binding affinities (p K i) for serotonin receptors (5-HT 1A [8.6], 5-HT 1B [8.4], 5-HT 2A [10.2], 5-HT 2B [9.8], 5-HT 2C [10.5], 5-HT 5 [8.8], 5-HT 6 [9.6] and 5-HT 7 [9.9]), adrenoceptors (α 1 [8.9], α 2A [8.9], α 2B [9.5] and α 2C [8.9]), dopamine receptors (D 1 [8.9], D 2 [8.9], D 3 [9.4] and D 4 [9.0]) and histamine receptors (H 1 [9.0] and H 2 [8.2]). It had much lower affinity (p K i ≤ 5) for muscarinic receptors and was the only agent with affinity for H 2 receptors. Relative to its D 2 receptor affinity, asenapine had a higher affinity for 5-HT 2C, 5-HT 2A, 5-HT 2B, 5-HT 7, 5-HT 6, α 2B and D 3 receptors, suggesting stronger engagement of these targets at therapeutic doses.

Nov 27, 2012. An agent that binds to but does not activate alpha -adrenergic receptors thereby blocking the actions of endogenous or exogenous alpha -adrenergic agonists. Alpha -Adrenergic antagonists are used in the. Asenapine: a review of its use in the management of mania in adults with bipolar I disorder. The results, recently obtained in coronary artery endothelial cells (CEC), have highlighted the role of asenapine on nitric oxide (NO) release and on different NO synthase (NOS) isoforms activation.[4] In particular, in physiological conditions, asenapine was found to increase NO production through the endothelial NOS.

Asenapine behaved as a potent antagonist (p K B) at 5-HT 1A (7.4), 5-HT 1B (8.1), 5-HT 2A (9.0), 5-HT 2B (9.3), 5-HT 2C (9.0), 5-HT 6 (8.0), 5-HT 7 (8.5), D 2 (9.1), D 3 (9.1), α 2A (7.3), α 2B (8.3), α 2C (6.8) and H 1 (8.4) receptors. These functional effects differed from those of risperidone (p K B.

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