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Spiroxatrine

Catalog No. T23382 CAS 1054-88-2

Synonyms: R 5188

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-HT1 β, 5-HT2, and dopamine receptors.Spiroxatrine may be used in the study of disorders related to the cardiovascular system.

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Spiroxatrine, CAS 1054-88-2

Pack Size	Availability	Price/USD
5 mg	In stock	$ 80.00
10 mg	In stock	$ 128.00
25 mg	In stock	$ 263.00
50 mg	In stock	$ 422.00
100 mg	In stock	$ 613.00

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Purity: 99.83%

Biological Description

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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-HT1 β, 5-HT2, and dopamine receptors.Spiroxatrine may be used in the study of disorders related to the cardiovascular system.
Targets&IC50	5-HT1A receptor:3.94 nM (Ki), 5-HT1B/D receptor:224000 nM (Ki), 5-HT2 receptor:118.5 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

Storage

store at low temperature,keep away from direct sunlight

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. D L Nelson, et al. Spiroxatrine: a selective serotonin1A receptor antagonist. Eur J Pharmacol. 1986 May 13;124(1-2):207-8. 2. Linda Cleary, et al. Investigation of neurotransmission in vas deferens from alpha(2A/D)-adrenoceptor knockout mice. Br J Pharmacol. 2002 Jul;136(6):857-64. 3. W J McBride, et al. Spiroxatrine augments fluoxetine-induced reduction of ethanol intake by the P line of rats. Pharmacol Biochem Behav. 1989 Oct;34(2):381-6. 4. Z-Y Liu, et al. Involvement of 5-hydroxytryptamine(1A) receptors in the descending anti-nociceptive pathway from periaqueductal gray to the spinal dorsal horn in intact rats, rats with nerve injury and rats with inflammation. Neuroscience. 2002;112(2):399-407.

Related compound libraries

This product is contained In the following compound libraries：

GPCR Compound Library Membrane Protein-targeted Compound Library Anti-Neurodegenerative Disease Compound Library

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Related compounds with same targets

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Keywords

Spiroxatrine 1054-88-2 GPCR/G Protein Neuroscience Dopamine Receptor 5-HT Receptor Adrenergic Receptor R 5188 inhibitor inhibit

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