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LY310762 is a potent and selective 5-HT1D serotonin receptor antagonist with an EC50 of 31 nM for the guinea pig 5-HT1D receptor. LY310762 had a higher affinity for the guinea pig 5-HT1D receptor (Ki=31 nM) than for the 5-HT1B receptor (Ki>1000 nM). LY310762 exhibited no activity on 5-HT transport. In microdialysis studies, injection of either LY310762 at 10 mg/kg by the intraperitoneal (i.p.) route, potentiated the increase in extracellular 5-HT concentration produced by a maximally effective dose of the selective serotonin re-uptake inhibitor, fluoxetine (at 20 mg/kg i.p.).LY310762 potentiated the potassium-induced [3H]5-HT outflow from guinea pig cortical slices with an EC50 values of 31 nM.
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
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| Animal models | Dunkin Hartley guinea pigs weighting 350-400 g |
| Formulation | |
| Dosages | 10 mg/kg |
| Administration | Administered via i.p. |
| Molecular Weight | 430.94 |
| Formula | C24H27FN2O2.HCl |
| CAS Number | 192927-92-7 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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| RS 39604
RS 39604 is a potent, selective, and orally active 5-HT4 receptor antagonist with a pKi of 9.1 in guinea pig striatal membranes. |
| GR127935
GR127935 is a selective 5-HT1D receptor antagonist. |
| SB-699551
SB-699551 is a potent and selective 5-HT5A antagonist with a pKi of 8.3. |
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