BMY-14802 is a potent and selective sigma-1 (σ1) receptor antagonist with an IC50 value of approximately 100 nM. BMY-14802 shows low affinity at serotonin (5-HT) 1A and adrenergic σ1 receptors and minimal activity at dopamine receptors. BMY-14802 has exhibited antipsychotic activity in rodent models and anti-dyskinetic effects against L-DOPA with preservation of antiparkinsonian efficacy.
| Molecular Weight | 348.39 |
| Formula | C18H22F2N4O |
| CAS Number | 105565-56-8 |
| Solubility (25°C) | DMSO: 5 mg/mL (warmed) |
| 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.
[3] S A Vanecek, et al. Discriminative stimulus characteristics of BMY 14802 in the pigeon
[4] D P Taylor, et al. A role for sigma binding in the antipsychotic profile of BMY 14802?
[5] G R Gewirtz, et al. BMY 14802, a sigma receptor ligand for the treatment of schizophrenia
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