Brexpiprazole

Brexpiprazole

CAT N°: 22906
Price:

From 66.00 56.10

Brexpiprazole is a serotonin (5-HT) and dopamine receptor modulator that has high affinity (Ki = 1A and 5-HT2A serotonin, dopamine D2L, and ?1B-, and ?2C-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 ?1B- and ?2C-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.

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • 7-[4-(4-benzo[b]thien-4-yl-1-piperazinyl)butoxy]-2(1H)-quinolinone
  • Correlated keywords
    • 5HT OPC34712
  • Product Overview:
    Brexpiprazole is a serotonin (5-HT) and dopamine receptor modulator that has high affinity (Ki = 1A and 5-HT2A serotonin, dopamine D2L, and ?1B-, and ?2C-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 ?1B- and ?2C-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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