SPIROXATRINE
SPIROXATRINE Basic information
- Product Name:
- SPIROXATRINE
- Synonyms:
-
- SPIROXATRINE
- R 5188
- (+/-)-8-[(2,3-DIHYDRO-1,4-BENZODIOXIN-2-YL)METHYL]-1-PHENYL-1,3,8-TRIAZA-SPIRO[4,5]DECAN-4-ONE
- 8-[(2,3-DIHYDRO-1,4-BENZODIOXIN-2-YL)METHYL]-1-PHENYL-1,3,8-TRIAZASPIRO[4,5]DECAN-4-ONE
- SPIROXATRINE (R 5188) SELECTIVE SEROTONI N 5
- R 5188, (±)-8-[(2,3-Dihydro-1,4-benzodioxin-2-yl)methyl]-1-phenyl-1,3,8-triaza-spiro[4,5]decan-4-one
- Spiroxatrine (R 5188)
- 8-(2,3-dihydro-1,4-benzodioxin-3-ylmethyl)-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one
- CAS:
- 1054-88-2
- MF:
- C22H25N3O3
- MW:
- 379.45
- Product Categories:
-
- Serotonin receptor
- Mol File:
- 1054-88-2.mol
SPIROXATRINE Chemical Properties
- Melting point:
- 215.8-218.0 °C
- Boiling point:
- 602.8±55.0 °C(Predicted)
- Density
- 1.32±0.1 g/cm3(Predicted)
- storage temp.
- Store at RT
- solubility
- 0.1 M HCl: moderately soluble
- form
- powder
- pka
- 15.03±0.20(Predicted)
- color
- white
MSDS
- Language:English Provider:SigmaAldrich
SPIROXATRINE Usage And Synthesis
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-HT1A Receptor: 3.94 nM (Ki); 5-HT1B/D Receptor: 224000 nM (Ki); 5-HT2 Receptor: 118.5 nM (Ki)
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