An atypical antipsychotic; binds to dopamine D2L

Cariprazine – 10 mg

Brand:
Cayman
CAS:
839712-12-8
Storage:
-20
UN-No:
Non-Hazardous - /

Cariprazine is an atypical antipsychotic.{60050} It binds to dopamine D2L, D2S, and D3 receptors, the serotonin (5-HT) receptor subtypes 5-HT1A, 5-HT2A, and 5-HT2B, and histamine H1 and sigma-1 (σ1) receptors (Kis = 0.085-23.44 nM).{36514} Cariprazine is an antagonist of dopamine D2 and D3 receptors (Kbs = 0.759 and 0.316 nM, respectively, in dopamine-induced [35S]GTPγS binding assays). It is also a partial agonist at these receptors, stimulating inositol phosphate production in murine A9 cells expressing human D2L receptors (EC50 = 3.16 nM) and inhibiting forskolin-induced cAMP accumulation in CHO cells expressing human D3 receptors (EC50 = 2.63 nM). Cariprazine inhibits amphetamine-induced hyperactivity and the conditioned avoidance response in rats (ED50s = 0.12 and 0.84 mg/kg, respectively).{60051} It also inhibits scopolamine-induced learning deficits in a water labyrinth learning test in rats when administered at doses ranging from 0.02 to 0.08 mg/kg. Formulations containing cariprazine have been used in the treatment of schizophrenia, as well as manic, depressive, or mixed episodes associated with bipolar I disorder.  

 

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Description

An atypical antipsychotic; binds to dopamine D2L, D2S, and D3, 5-HT1A, 5-HT2A, 5-HT2B, histamine H1, and σ1 receptors (Kis = 0.085-23.44 nM); an antagonist of dopamine D2 and D3 receptors (Kbs = 0.759 and 0.316 nM, respectively); a partial agonist at dopamine D2 and D3 receptors; stimulates inositol phosphate production in murine A9 cells expressing human D2L receptors (EC50 = 3.16 nM); inhibits forskolin-induced cAMP accumulation in CHO cells expressing human D3 receptors (EC50 = 2.63 nM); inhibits amphetamine-induced hyperactivity and the conditioned avoidance response in rats (ED50s = 0.12 and 0.84 mg/kg, respectively); inhibits scopolamine-induced learning deficits in a water labyrinth learning test in rats from 0.02-0.08 mg/kg

Formal name: N′-[trans-4-[2-[4-(2,3-dichlorophenyl)-1-piperazinyl]ethyl]cyclohexyl]-N,N-dimethyl-urea

Synonyms:  RGH-188

Molecular weight: 427.4

CAS: 839712-12-8

Purity: ≥98%

Formulation: A crystalline solid

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