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Spiroxatrine (R 5188) is a selective and potent 5-HT1α and α2-adrenergic dual antagonist with sedative activity, and inhibitory effects on 5-HT1α, 5-HT1β, 5-HT2, and dopamine receptors. Spiroxatrine may be used in the study of disorders related to the cardiovascular system.

| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 5 mg | $80 | In Stock | |
| 10 mg | $128 | In Stock | |
| 25 mg | $263 | In Stock | |
| 50 mg | $422 | In Stock | |
| 100 mg | $613 | In Stock |
| Description | Spiroxatrine (R 5188) is a selective and potent 5-HT1α and α2-adrenergic dual antagonist with sedative activity, and inhibitory effects on 5-HT1α, 5-HT1β, 5-HT2, and dopamine receptors. Spiroxatrine may be used in the study of disorders related to the cardiovascular system. |
| Targets&IC50 | 5-HT2 receptor:118.5 nM (Ki), 5-HT1B/D receptor:224000 nM (Ki), 5-HT1A receptor:3.94 nM (Ki) |
| In vitro | Sproxatrine (0.01-0.1 μM, 15 mins) enhances contraction in the vas deferens tissue of α2A/D-adrenergic receptor knockout mice[2]. |
| In vivo | Sproxatrine (1-25 μg, intraperitoneal injection, 5 days) increases withdrawal latency to thermal and mechanical stimuli in the hind paw of nerve-injured rats and carrageenan-induced inflammatory rats[3]. Sproxatrine (4 mg/kg/day, intraperitoneal injection, 5 minutes) enhances the effect of Fluoxetine in reducing selectively bred alcohol-preferring (P) rat's voluntary oral ethanol intake[3]. |
| Synonyms | R 5188 |
| Molecular Weight | 379.45 |
| Formula | C22H25N3O3 |
| Cas No. | 1054-88-2 |
| Smiles | O=C1C2(N(CN1)C3=CC=CC=C3)CCN(CC4OC=5C(OC4)=CC=CC5)CC2 |
| Relative Density. | 1.32 g/cm3 (Predicted) |
| Storage | store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO: < 1 mg/mL (insoluble or slightly soluble) |

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