GR 125743( —— )

Catalog No. M22737 CAS No. 148547-33-5

GR 125743 is a novel antagonist of 5-HT1B/1D receptor.GR-125743, a new radiolabelled derivative of a compound that exhibits selective antagonistic properties with respect to the serotonin human (h5-HT1D) and human (h5-HT1B) receptors.?The compound has been characterized for its ability to label the cloned h5-HT1D and h5-HT1B receptors.?

Purity : >98% (HPLC)

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Biological Information

Product Name

GR 125743
Note

Research use only, not for human use.
Brief Description

GR 125743 is a novel antagonist of 5-HT1B/1D receptor.GR-125743, a new radiolabelled derivative of a compound that exhibits selective antagonistic properties with respect to the serotonin human (h5-HT1D) and human (h5-HT1B) receptors.?The compound has been characterized for its ability to label the cloned h5-HT1D and h5-HT1B receptors.?
Description

GR 125743 is a novel antagonist of 5-HT1B/1D receptor.GR-125743, a new radiolabelled derivative of a compound that exhibits selective antagonistic properties with respect to the serotonin human (h5-HT1D) and human (h5-HT1B) receptors.?The compound has been characterized for its ability to label the cloned h5-HT1D and h5-HT1B receptors.?
In Vitro

GR 125743 has a Kd of 0.61 nM for h5-HT1B.
In Vivo

GR 125743 (0.3 mg/kg; i.p.) produces significant decreases in extracellular 5-HT in the frontal cortex of the conscious guinea pig. Animal Model:Male Dunkin Hartley guinea-pigs (350-450 g)Dosage:0.3 mg/kg Administration:Intraperitoneal injection Result:Produced significant transient increases in extracellular 5-HT.
Synonyms

——
Pathway

Endocrinology/Hormones
Target

5-HT Receptor
Recptor

5-HT1B/1D
Research Area

——
Indication

——

Chemical Information

CAS Number

148547-33-5
Formula Weight

416.53
Molecular Formula

C25H28N4O2
Purity

>98% (HPLC)
Solubility

In Vitro:?DMSO : 100 mg/mL (240.08 mM)
SMILES

COc1ccc(NC(=O)c2ccc(c(C)c2)-c2ccncc2)cc1N1CCN(C)CC1
Chemical Name

——

Shipping & Storage Information

Storage

(-20℃)
Shipping

With Ice Pack
Stability

≥ 2 years

Reference

1. T Doménech, J Beleta, J M Palacios,et al.Characterization of human serotonin 1D and 1B receptors using [3H]-GR-125743, a novel radiolabelled serotonin 5HT1D/1B receptor antagonist.Naunyn Schmiedebergs Arch Pharmacol. 1997 Sep;356(3):328-34.

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