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 (Request formulation change)
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
Certificates of Analysis & Batch Specific Data

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    5 mg

    $63

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    10 mg

    $110

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    25 mg

    $257

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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.

    References & Product Citations
    Product Description References

    1. Neale, R.F., Fallon, S.L., Boyar, W.C., et al. Biochemical and pharmacological characterization of CGS 12066B, a selective serotonin-1B agonist. Eur. J. Pharmacol. 136(1), 1-9 (1987).

    2. Unsworth, C.D., and Molinoff, P.B. Regulation of the 5-hydroxytryptamine1B receptor in opossum kidney cells after exposure to agonists. Mol. Pharmacol. 42(3), 464-470 (1992).

    3. Joppa, M.A., Rowe, R.K., and Meisel, R.L. Effects of serotonin 1A or 1B receptor agonists on social aggression in male and female Syrian hamsters. Pharmacol. Biochem. Behav. 58(2), 349-353 (1997).