1054-88-2

1054-88-2 structure

Name: Spiroxatrine
Chemical Name: 8-(2,3-dihydro-1,4-benzodioxin-3-ylmethyl)-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one
CAS Number: 1054-88-2
Molecular Formula: C₂₂H₂₅N₃O₃
Molecular Weight: 379.45
Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
Create Date: 2018-07-06 19:21:08
Modify Date: 2025-08-25 17:18:17
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].

Name	8-(2,3-dihydro-1,4-benzodioxin-3-ylmethyl)-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one
Synonyms	L-803,087 trifluoroacetate Espiroxatrina MFCD00055134 R 5188 spiroxatriene Spiroxatrinum Spiroxatrine

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.

WGK Germany	3