A 5-HT1B and 5-HT1D receptor antagonist
Technical Support & Resources

Visit our FAQ

Contact Us

Toll Free Phone (USA and Canada Only): (888) 526-5351
Direct Phone: (734) 975-3888

Request Technical Support

Technical Support Request

To streamline the process attach the appropriate questionnaire to your inquiry.

Download IHC QuestionnaireDownload WB Questionnaire

View Our Privacy Statement for details on how we use and protect your data. In addition, this site is protected by hCaptcha and its Privacy Policy and Terms of Service apply.

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
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
Recommended Products

Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

Download most recent Certificate of Analysis for this product

    5 mg

    $119

    Add

    10 mg

    $213

    Add

    25 mg

    $440

    Add

    50 mg

    $822

    Add
    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).