PNU 109291

PNU109291 is a potent and selective 5-HT1D agonist. PNU109291 reduces dural plasma extravasation evoked by trigeminal ganglion stimulation[1].

Research Areas >> Neurological Disease

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

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

PNU109291 (0.24、2.4、7.3、24.4、73.3 nmol/kg；皮下注射) 减少猪的三叉神经节刺激引起的硬脑膜血浆外渗[1]。 PNU109291 (3 µM) 抑制大鼠弗氏佐剂 (CFA) 诱发的 EPSC（兴奋性突触后电流），但不抑制注射盐水的处理组[2]。 Animal Model: 200-500g, male Hartley guinea pigs[1] Dosage: 0.24, 2.4, 7.3, 24.4, 73.3 nmol/kg Administration: S.c.; 60 min before electrical stimulation Result: Dose-dependently decreased plasma protein extravasation with an IC50 value of 4.2 nmol/kg.

[1]. Cutrer FM, et al. Effects of PNU-109,291, a selective 5-HT1D receptor agonist, on electrically induced dural plasma extravasation and capsaicin-evoked c-fos immunoreactivity within trigeminal nucleus caudalis. Neuropharmacology. 1999 Jul;38(7):1043-53.  

[2]. Winters BL, et al. Inflammation induces developmentally regulated sumatriptan inhibition of spinal synaptic transmission. Br J Pharmacol. 2020 Aug;177(16):3730-3743.