Spiroxatrine

Names

[ Name ]:
Spiroxatrine

[Synonym ]:
L-803,087 trifluoroacetate
Espiroxatrina
MFCD00055134
R 5188
spiroxatriene
Spiroxatrinum
Spiroxatrine

Biological Activity

[Description]:

Spiroxatrine (R 5188) is a selective, dual antagonist of 5-HT1α and α2-adrenergic, with the Ki values of 3.94, 224000, 118.5 nM for 5-HT1α，5-HT1β and 5-HT2，respectively. Spiroxatrine (R 5188) has a sedative effect[1][2][3][4].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor

Research Areas >> Inflammation/Immunology

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

[Target]

α2-adrenergic receptor

5-HT1A Receptor:3.94 nM (Ki)

5-HT1B/D Receptor:224000 nM (Ki)

5-HT2 Receptor:118.5 nM (Ki)

[References]

[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]. 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.

[4]. 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.

Chemical & Physical Properties

[ Density]:
1.32g/cm3

[ Boiling Point ]:
602.8ºC at 760mmHg

[ Molecular Formula ]:
C₂₂H₂₅N₃O₃

[ Molecular Weight ]:
379.45

[ Flash Point ]:
318.4ºC

[ Exact Mass ]:
379.19000

[ PSA ]:
54.04000

[ LogP ]:
2.58660

[ Vapour Pressure ]:
1.74E-14mmHg at 25°C

[ Index of Refraction ]:
1.665

MSDS

Click to get detail MSDS

Safety Information

[ WGK Germany ]:
3