GR 125743

GR 125743 is a selective 5-HT1B/1D receptor antagonist, with pKis of 8.85 and 8.31 for wild-type h5-HT1B and wild-type h5-HT1D, respectively. GR 125743 is used for the research of Parkinson's disease and cardiovascular diseases[1][2].

Product Specifications

CAS Number

[148547-33-5]

UNSPSC

12352005

Target

5-HT Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neurodegeneration

Field of Research

Neurological Disease; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/gr-125743.html

Purity

99.77

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(C1=CC=C(C(C)=C1)C2=CC=NC=C2)NC3=CC=C(C(N4CCN(CC4)C)=C3)OC

Molecular Formula

C25H28N4O2

Molecular Weight

416.52

References & Citations

[1]T Wurch, et al. Induction of a high-affinity ketanserin binding site at the 5-Hydroxytryptamine (1B) receptor by modification of its carboxy-terminal intracellular portion. Characterization of human serotonin 1D and 1B receptors using [3H]-GR-125743, a novel radiolabelled serotonin 5HT1D/1B receptor antagonist. Biochem Pharmacol. 2000 May 1;59 (9) :1117-21.|[2]Roberts, C., et al. The role of 5-HT1B/1D receptors in the modulation of 5-hydroxytryptamine levels in the frontal cortex of the conscious guinea pig. European Journal of Pharmacology. 1997 May 12;326 (1) :23-30.