A serotonin and dopamine receptor modulator; partial agonist of human 5-HT1A

Brexpiprazole – 50 mg

Brand:
Cayman
CAS:
913611-97-9
Storage:
-20
UN-No:
Non-Hazardous - /

Brexpiprazole is a serotonin (5-HT) and dopamine receptor modulator that has high affinity (Ki = 1A and 5-HT2A serotonin, dopamine D2L, and α1B-, and α2C-adrenergic receptors in CHO cell membranes expressing the human receptors.{39167} It acts as a partial agonist of 5-HT1A, D2L, and D3 receptors (EC50s = 0.49, 4.0, and 2.8 nM, respectively) and an antagonist of 5-HT2A, 5-HT2B, as well as α1B- and α2C-adrenergic receptors (IC50s = 6.5, 14, 0.66, and 63 nM, respectively) in vitro. In vivo, brexpiprazole dose-dependently reduces conditioned avoidance response (CAR) time, inhibits locomoter hyperactivity induced by apomorphine (Item No. 16094) and amphetamine, and reverses cognitive defects induced by subchronic PCP administration in rats.{39168} It also reduces apomorphine-induced eye blinking in cynomolgus monkeys. Formulations containing brexpiprazole have been used in the treatment of schizophrenia and major depressive disorder.  

 

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SKU: 22906 - 50 mg Category:

Description

A serotonin and dopamine receptor modulator; partial agonist of human 5-HT1A, D2L, and D3 receptors (EC50s = 0.49, 4.0, and 2.8 nM, respectively); antagonist of 5-HT2A, 5-HT2B, as well as α1B- and α2C-adrenergic receptors (IC50s = 6.5, 14, 0.66, and 63 nM, respectively); dose-dependently reduces conditioned avoidance response (CAR) time, inhibits apomorphine- and amphetamine-induced locomoter hyperactivity, and reverses cognitive defects in rats; antagonizes apomorphine-induced eye blinking in cynomolgus monkeys

Formal name: 7-[4-(4-benzo[b]thien-4-yl-1-piperazinyl)butoxy]-2(1H)-quinolinone

Synonyms:  OPC 34712

Molecular weight: 433.6

CAS: 913611-97-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Neuroscience|Behavioral Neuroscience|Depression||Research Area|Neuroscience|Behavioral Neuroscience|Learning & Memory||Research Area|Neuroscience|Behavioral Neuroscience|Schizophrenia & Psychosis

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