Uses
Spiroxatrine (R 5188) is a SR-1A antagonist.
Definition
ChEBI: 8-(2,3-dihydro-1,4-benzodioxin-3-ylmethyl)-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one is a member of imidazolidines.
Biological Activity
5-HT 1A antagonist. More active and selective than spiperone. Also a very potent α 2C adrenergic receptor antagonist.
in vivo
Spiroxatrine (1-25 ug for i.p., 5 days) increases hindpaw withdrawal latencies to thermal and mechanical stimulation in the nerve injury rat and Carrageenan (HY-125474)-induced rat inflammation model[3].
Spiroxatrine (4 mg/kg/day for i.p., 5 mins) increases the voluntary oral ethanol intake induced by Fluoxetine (HY-B0102) in the selectively bred alcohol-preferring P line of rats [4].
| Animal Model: | The nerve injury rat model and Carrageenan (HY-125474)-induced rat inflammation model[3] |
| Dosage: | 1, 10, 25 ug, 5 days |
| Administration: | Intraperitoneal injection (i.p.) |
| Result: | Increased hindpaw withdrawal latencies to thermal and mechanical stimulation. |
| Animal Model: | Fluoxetine (HY-B0102) -induced reduction of ethanol Intake by the P Line of rats[4] |
| Dosage: | 4 mg/kg/day, 5 mins |
| Administration: | Intraperitoneal injection (i.p.) |
| Result: | Increased the voluntary oral ethanol intake induced by Fluoxetine (HY-B0102) in the selectively bred alcohol-preferring P line of rats. |
IC 50
α2-adrenergic receptor; 5-HT
1A Receptor: 3.94 nM (Ki); 5-HT
1B/D Receptor: 224000 nM (Ki); 5-HT
2 Receptor: 118.5 nM (Ki)
