CAS NO: | 148547-33-5 |
包装 | 价格(元) |
10mM (in 1mL DMSO) | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
Cas No. | 148547-33-5 |
Canonical SMILES | O=C(C1=CC=C(C(C)=C1)C2=CC=NC=C2)NC3=CC=C(C(N4CCN(CC4)C)=C3)OC |
分子式 | C25H28N4O2 |
分子量 | 416.52 |
溶解度 | DMSO: 100 mg/mL (240.08 mM) |
储存条件 | 4°C, protect from light |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | 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]. GR 125743 has a Kd of 0.61 nM for h5-HT1B[1]. 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] [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. |