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Bioactivity 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].
Invitro Spiroxatrine (0.01-0.1 μM, 15 mins) 使 α2A/D-肾上腺素受体敲除小鼠输精管组织收缩增强[2]。 0 --> Spiroxatrine 相关抗体:
In Vivo Spiroxatrine (1-25 ug, 腹腔注射, 5 天) 增加神经损伤大鼠和 Carrageenan (HY-125474) 诱导的炎症大鼠后爪对热刺激和机械刺激的戒断潜伏期[3]。Spiroxatrine (4 mg/kg/每天, 腹腔注射, 5 分钟) 增强 Fluoxetine (HY-B0102) 减少选择性繁殖的嗜醇性 P系大鼠自愿口服乙醇摄入的效果[4]。 Animal Model:
Name Spiroxatrine
CAS 1054-88-2
Formula C22H25N3O3
Molar Mass 379.45
Appearance Solid
Transport Room temperature in continental US; may vary elsewhere.
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Reference [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.

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