A 5-HT1B receptor agonist
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CGS 12066B

Item No. 30623

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-(4-methyl-1-piperazinyl)-7-(trifluoromethyl)-pyrrolo[1,2-a]quinoxaline, (2Z)-2-butenedioate
CAS Number
109028-10-6
Molecular Formula
C17H17F3N4 • 2C4H4O4
Formula Weight
566.5
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 25 mg/ml
SMILES
FC(F)(F)C1=CC=C2C(N=C(N3CCN(C)CC3)C4=CC=CN42)=C1.OC(/C=C\C(O)=O)=O.OC(/C=C\C(O)=O)=O
InChi Code
InChI=1S/C17H17F3N4.2C4H4O4/c1-22-7-9-23(10-8-22)16-15-3-2-6-24(15)14-5-4-12(17(18,19)20)11-13(14)21-16;2*5-3(6)1-2-4(7)8/h2-6,11H,7-10H2,1H3;2*1-2H,(H,5,6)(H,7,8)/b;2*2-1-
InChi Key
HTEVMLYDEWVIQE-SPIKMXEPSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    CGS 12066B is an agonist of the serotonin (5-HT) receptor subtype 5-HT1B (IC50 = 51 nM).1 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.2 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).1 It decreases interfemale and intermale aggression in Syrian hamsters.3

    WARNING This product is not for human or veterinary use.