A 5-HT1B and 5-HT1D receptor antagonist
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GR127935 (hydrochloride)

Item No. 29651

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[4-methoxy-3-(4-methyl-1-piperazinyl)phenyl]-2′-methyl-4′-(5-methyl-1,2,4-oxadiazol-3-yl)-[1,1′-biphenyl]-4-carboxamide, monohydrochloride
CAS Number
148642-42-6
Molecular Formula
C29H31N5O3 • HCl
Formula Weight
534.1
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 1 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.25 mg/ml
λmax
291 nm
SMILES
CC1=CC(C2=NOC(C)=N2)=CC=C1C3=CC=C(C(NC4=CC(N5CCN(C)CC5)=C(OC)C=C4)=O)C=C3.Cl
InChi Code
InChI=1S/C29H31N5O3.ClH/c1-19-17-23(28-30-20(2)37-32-28)9-11-25(19)21-5-7-22(8-6-21)29(35)31-24-10-12-27(36-4)26(18-24)34-15-13-33(3)14-16-34;/h5-12,17-18H,13-16H2,1-4H3,(H,31,35);1H
InChi Key
SRVVUYIJVBLEJI-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $119

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    10 mg

    $213

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    25 mg

    $440

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    50 mg

    $822

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    Product Description

    GR127935 is an antagonist of the serotonin (5-HT) receptor subtypes 5-HT1B, 5-HT1Dα, and 5-HT1Dβ (IC50s = 3.16, 1.26, and 0.13 nM, respectively).1 It is selective for the 5-HT1B and 5-HT1D receptors over other 5-HT receptors (IC50s = 39.81->10,000 nM in radioligand binding assays). GR127935 increases extracellular 5-HT levels in the guinea pig frontal cortex and prevents increases in 5-HT in rat frontal cortex induced by the selective serotonin reuptake inhibitor paroxetine (Item No. 14998).2 It enhances memory consolidation in an autoshaping learning task in rats when administered post-training at a dose of 10 mg/kg.3 It has been used to elucidate the 5-HT receptor subtypes involved in the anti-inflammatory activity of sumatriptan (Item No. 14600) following myocardial ischemia-reperfusion injury and testicular torsion/detorsion.4,5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Skingle, M., Beattie, D.T., Scopes, D.I., et al. GR127935: A potent and selective 5-HT1D receptor antagonist. Behav. Brain Res. 73(1-2), 157-161 (1996).

    2. Sharp, T., Umbers, V., and Gartside, S.E. Effect of a selective 5-HT reuptake inhibitor in combination with 5-HT1A and 5-HT1B receptor antagonists on extracellular 5-HT in rat frontal cortex in vivo. Br. J. Pharmacol. 121(5), 941-946 (1997).

    3. Meneses, A., Terrón, J.A., and Hong, E. Effects of the 5-HT receptor antagonists GR127935 (5-HT1B/1D) and MDL100907 (5-HT2A) in the consolidation of learning. Behav. Brain Res. 89(1-2), 217-223 (1997).

    4. Sheibani, M., Faghir-Ghanesefat, H., Dehpour, S., et al. Sumatriptan protects against myocardial ischaemia-reperfusion injury by inhibition of inflammation in rat model. Inflammopharmacology 27(5), 1071-1080 (2019).

    5. Dejban, P., Rahimi, N., Takzare, N., et al. Protective effects of sumatriptan on ischaemia/reperfusion injury following torsion/detorsion in ipsilateral and contralateral testes of rat. Andrologia 51(9):e13358, (2019).