| Identification | Back Directory | [Name]
GR 125743 | [CAS]
148547-33-5 | [Synonyms]
GR 125743
Benzamide, N-[4-methoxy-3-(4-methyl-1-piperazinyl)phenyl]-3-methyl-4-(4-pyridinyl)- | [Molecular Formula]
C25H28N4O2 | [MDL Number]
MFCD00918566 | [MOL File]
148547-33-5.mol | [Molecular Weight]
416.52 |
| Hazard Information | Back Directory | [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) | [storage]
4°C, protect from light | [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 |
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