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.
Shipping Conditions
Room Temperature
Storage Conditions
4°C (Powder, protect from light)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
5-HT1 Receptor; mLAG-3
Available Sizes
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