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 | |
|---|---|
| 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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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