A 5-HT1B receptor agonist (IC50 = 51 nM); selective for 5-HT1B over 5-HT1A and 5-HT2 receptors (IC50s = 876 and 6

CGS 12066B – 25 mg

Brand:
Cayman
CAS:
109028-10-6
Storage:
-20
UN-No:
Non-Hazardous - /

CGS 12066B is an agonist of the serotonin (5-HT) receptor subtype 5-HT1B (IC50 = 51 nM).{53886} It is selective for 5-HT1B over 5-HT1A and 5-HT2 receptors (IC50s = 876 and 6,480 nM, respectively), as well as α1-, α2-, and β-adrenergic, and dopamine D1 and D2 receptors (IC50s = >6,000, >1,000, >1,000, >5,000, and >5,000 nM, respectively). CGS 12066B inhibits forskolin-induced cAMP accumulation in opossum kidney cells when used at concentrations ranging from 0.001 to 1 µM.{53887} In vivo, CGS 12066B reduces 5-hydroxy-L-tryptophan (5-HTP) accumulation in the fronto-parietal cortex (ED50 = 7.92 µmol/kg) and induces dorsal raphe cell firing in rats (ED50 = 358 nmol/kg).{53886} It decreases interfemale and intermale aggression in Syrian hamsters.{53888}  

 

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Description

A 5-HT1B receptor agonist (IC50 = 51 nM); selective for 5-HT1B over 5-HT1A and 5-HT2 receptors (IC50s = 876 and 6,480 nM, respectively), as well as α1-, α2-, and β-adrenergic and dopamine D1 and D2 receptors (IC50s = >6,000, >1,000, >1,000, >5,000, and >5,000 nM, respectively); inhibits forskolin-induced cAMP accumulation in opossum kidney cells from 0.001-1 µM; reduces 5-HTP accumulaiton in the the fronto-parietal cortex (ED50 = 7.92 µmol/kg) and induces dorsal raphe cell firing in rats (ED50 = 358 nmol/kg); decreases interfemale and intermale aggression in Syrian hamsters

Formal name: 4-(4-methyl-1-piperazinyl)-7-(trifluoromethyl)-pyrrolo[1,2-a]quinoxaline, (2Z)-2-butenedioate

Synonyms: 

Molecular weight: 566.5

CAS: 109028-10-6

Purity: ≥98%

Formulation: A solid

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