| Bioactivity | LY310762 is a selective 5-HT1D receptor antagonist (Ki=249 nM) with a weak affinity for 5-HT1B receptor. LY310762 effectively abolishes the renal vasodilatory effects of 5-HT |
| Invitro | LY310762 (0.01-1 µM) shows potentiation of potassium-induced [3H]5-HT outflow from guinea pig cortical slices with an EC50 value of 31 nM[1].LY310762 (10 µM) significantly but not completely blocks the extent of sumatriptan-induced decrease in EPSCs (excitatory postsynaptic potential)[3]. |
| In Vivo | LY310762 (10 mg/kg; i.p.; single) significantly increases the extracellular 5-HT concentration produced by Fluoxetine (selective serotonin re-uptake inhibitor) in vivo[1].LY310762 (1 mg/kg; i.v.; single) abolishes 5-HT vasodilator effects in phenylephrine-infusion rats model[2]. Animal Model: |
| Name | LY310762 |
| CAS | 192927-92-7 |
| Formula | C24H28ClFN2O2 |
| Molar Mass | 430.94 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [1]. Pullar IA, et al. The role of the 5-HT1D receptor as a presynaptic autoreceptor in the guinea pig. Eur J Pharmacol. 2004 Jun 16;493(1-3):85-93. [2]. García-Pedraza JÁ, et al. Pharmacological evidence that 5-HT1D activation induces renal vasodilation by NO pathway in rats. Clin Exp Pharmacol Physiol. 2015 Jun;42(6):640-7. [3]. Choi IS, Cho JH, An CH, Jung JK, Hur YK, Choi JK, Jang IS. 5-HT(1B) receptors inhibit glutamate release from primary afferent terminals in rat medullary dorsal horn neurons. Br J Pharmacol. 2012 Sep;167(2):356-67. |
LY310762
CAS: 192927-92-7 F: C24H28ClFN2O2 W: 430.94
LY310762 is a selective 5-HT1D receptor antagonist (Ki=249 nM) with a weak affinity for 5-HT1B receptor. LY310762 effect
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