GR 125743
- Product Name
- GR 125743
- CAS No.
- 148547-33-5
- Chemical Name
- GR 125743
- Synonyms
- GR 125743;GR 125743, 10 mM in DMSO;GR 125743, 5-HT1B/1D antagonist;N-(4-Methoxy-3-(4-methylpiperazin-1-yl)phenyl)-3-methyl-4-(pyridin-4-yl)benzamide;Benzamide, N-[4-methoxy-3-(4-methyl-1-piperazinyl)phenyl]-3-methyl-4-(4-pyridinyl)-;h5-HT1B,cognitive disorder,h5-HT1D,cardiovascular,GR-125743,GR125743,inhibit,Parkinson's disease,5-HT Receptor,GR 125743,5-hydroxytryptamine Receptor,receptor,Inhibitor,Serotonin Receptor
- CBNumber
- CB22487573
- Molecular Formula
- C25H28N4O2
- Formula Weight
- 416.52
- MOL File
- 148547-33-5.mol
GR 125743 Property
- storage temp.
- 4°C, protect from light
- solubility
- DMSO: 100 mg/mL (240.08 mM)
- form
- Solid
- color
- White to off-white
N-Bromosuccinimide Price
- Product number
- CS-0081850
- Product name
- GR125743
- Purity
- 99.78%
- Packaging
- 5mg
- Price
- $100
- Updated
- 2021/12/16
- Product number
- CS-0081850
- Product name
- GR125743
- Purity
- 99.78%
- Packaging
- 10mg
- Price
- $150
- Updated
- 2021/12/16
- Product number
- CS-0081850
- Product name
- GR125743
- Purity
- 99.78%
- Packaging
- 50mg
- Price
- $450
- Updated
- 2021/12/16
- Product number
- BRS0000377
- Product name
- GR-125,743
- Purity
- 95.00%
- Packaging
- 10MG
- Price
- $694.91
- Updated
- 2021/12/16
- Product number
- 025865
- Product name
- GR-125743
- Packaging
- 001
- Price
- $600
- Updated
- 2021/12/16
GR 125743 Chemical Properties,Usage,Production
Uses
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].
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[2].
| Animal Model: | Male Dunkin Hartley guinea-pigs (350-450 g)[2] |
| Dosage: | 0.3 mg/kg |
| Administration: | Intraperitoneal injection |
| Result: | Produced significant transient increases in extracellular 5-HT. |
IC 50
human 5-HT1B Receptor: 8.85 (pKi); human 5-HT1D Receptor: 8.31 (pKi)
References
[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. DOI:10.1016/s0006-2952(99)00416-5
[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. DOI:10.1016/s0014-2999(97)00156-8
GR 125743 Preparation Products And Raw materials
Raw materials
Preparation Products
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