Asenapine maleate

Multiple receptor antagonist. Anti-psychotic agent.

Pack Size

Biological Description Novel, multiple receptor antagonist. Displays activity at 5-HT, dopamine, adrenoceptors and histamine receptors. (pK_i values are 8.60 (5-HT_1A), 8.40 (5-HT_1B), 10.15 (5-HT_2A), 9.75 (5-HT_2B), 10.46 (5-HT_2C), 8.84 (5-HT_5A), 9.60 (5-HT₆), 9.94 (5-HT₇), 8.85 (D₁), 8.90 (D_2L), 8.84 (D_2S), 9.38 (D₃), 8.95 (D₄), 8.93 (α_1A), 8.9 (α_2A), 9.49 (α_2B), 8.91 (α_2C), 9.00 (H₁) and 8.21(H₂) receptors respectively). Increases dopamine, norepinephrine and acetylcholine efflux. Anti-psychotic in vivo.
Useful References
Asenapine increases dopamine, norepinephrine, and acetylcholine efflux in the rat medial prefrontal cortex and hippocampus. abstract Asenapine effects in animal models of psychosis and cognitive function. abstract Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. abstract
Chemical Information trans-5-Chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenzo[2,3:6,7]oxepino[4,5-c]pyrrole maleate
	Store at +4°C MW 401.85 Soluble in DMSO to 100 mM and in ethanol to 100 mM C₁₇H₁₆ClNO.C₄H₄O₄ 85650-56-2