| Identification | Back Directory | [Name]
SPIROXATRINE | [CAS]
1054-88-2 | [Synonyms]
R 5188
SPIROXATRINE
Spiroxatrine (R 5188)
SPIROXATRINE (R 5188) SELECTIVE SEROTONI N 5
8-(2,3-dihydro-1,4-benzodioxin-3-ylmethyl)-1-phenyl-1,3,8-triazaspiro[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
1,3,8-Triazaspiro[4.5]decan-4-one, 8-[(2,3-dihydro-1,4-benzodioxin-2-yl)methyl]-1-phenyl-
8-((2,3-Dihydrobenzo[b][1,4]dioxin-2-yl)methyl)-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one
(+/-)-8-[(2,3-DIHYDRO-1,4-BENZODIOXIN-2-YL)METHYL]-1-PHENYL-1,3,8-TRIAZA-SPIRO[4,5]DECAN-4-ONE
R 5188, (±)-8-[(2,3-Dihydro-1,4-benzodioxin-2-yl)methyl]-1-phenyl-1,3,8-triaza-spiro[4,5]decan-4-one | [Molecular Formula]
C22H25N3O3 | [MDL Number]
MFCD00055134 | [MOL File]
1054-88-2.mol | [Molecular Weight]
379.45 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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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| Company Name: |
BOC Sciences
|
| Tel: |
|
| Website: |
https://www.bocsci.com |
| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
|