An atypical antipsychotic; binds to dopamine D1-4

(±)-Asenapine – 10 mg

Brand:
Cayman
CAS:
65576-45-6
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

(±)-Asenapine is an atypical antipsychotic.{41915,41916} It binds to dopamine D1-4, α-adrenergic, and histamine receptors (Kis = 0.42-1.45, 0.32-1.26, and 1-6.17 nM, respectively), as well as the serotonin (5-HT) receptor subtypes 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT5A, 5-HT6, and 5-HT7 (Kis = 0.03-3.98 nM).{41916} (±)-Asenapine inhibits the suppression of neuron firing induced by the 5-HT2A, dopamine D2, and α2-adrenergic receptor agonists 2,5-dimethoxy-4-iodoamphetamine (DOI), apomorphine, and clonidine (Item No. 15949), respectively, in rat brain (ED50s = 75, 40, and 85 μg/kg, respectively).{41915} In vivo, (±)-asenapine (0.05-0.2 mg/kg, s.c.) increases extracellular dopamine levels in the medial prefrontal cortex (mPFC), nucleus accumbens (NAc), and lateral striatum and suppresses the conditioned avoidance response in rats.{41917} It prevents acute and chronic phencyclidine-induced deficits in cued reversal learning in rats when administered at a dose of 0.075 mg/kg.{41918} Formulations containing asenapine have been used in the treatment of schizophrenia and bipolar I disorder.  

 

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SKU: 9000496 - 10 mg Category:

Description

An atypical antipsychotic; binds to dopamine D1-4, α-adrenergic, and histamine receptors (Kis = 0.42-1.45, 0.32-1.26, and 1-6.17 nM, respectively), as well as various 5-HT receptors (Kis = 0.03-3.98 nM); inhibits DOI, apomorphine, or clonidine-induced neuron firing in rat brain (ED50s = 75, 40, and 85 μg/kg, respectively); increases mPFC, NAc, and lateral striatum extracellular dopamine and suppresses the conditioned avoidance response in rats from 0.05-0.2 mg/kg, s.c.; prevents acute and chronic phencyclidine-induced deficits in cued reversal learning in rats at 0.075 mg/kg

Formal name: rel-5-chloro-2,3,3aR,12bR-tetrahydro-2-methyl-1H-dibenz[2,3:6,7]oxepino[4,5-c]pyrrole

Synonyms: 

Molecular weight: 285.8

CAS: 65576-45-6

Purity: ≥95%

Formulation: A solid

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