同义名 :	Isoguvacine (hydrochloride)
	CAS号 :	68547-97-7
	货号 :	A355363
	分子式 :	C6H10ClNO2
	纯度 :	95%
	分子量 :	163.6
	MDL号 :	-
	存储条件：	Pure form Inert atmosphere, 2-8°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

生物活性

描述

Isoguvacine HCl (1,2,3,6-tetrahydropyridine-4-carboxylic acid) is a GABA (gamma-aminobutyric acid) agonist with limited conformational flexibility. Isoguvacine binds to membrane preparations of rat forebrain with pharmacological characteristics similar to the post-synaptic GABA recognition site; that it is transported into synaptosomal preparations by an uptake system similar to the high-affinity GABA uptake system; and that recently accumulated isoguvacine is released in a Ca2+-dependent manner and by heteroexchange with external GABA[1]. Isoguvacine, a GABAA receptor agonist, enhances substance P (SP) release in the spinal cord[2]. Bilateral microinjection of the GABAA receptor agonist isoguvacine or the GABAB receptor agonist baclofen attenuated the AAR(adipose afferent reflex)[3]. Neurons in the pontine Kölliker-Fuse nucleus (KF) were inhibited with bilateral microinjections of isoguvacine (50-70 nl, 10 mm) to remove the post-inspiratory phase of respiration[4]. Isoguvacine at a concentration of 50 μM blocks the seizure like events in 2 out of 6 organotypic hippocampal slice cultures. Isoguvacine inhibits the low magnesium induced seizure like events dose dependently[5].

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	6.11mL 1.22mL 0.61mL	30.56mL 6.11mL 3.06mL	61.12mL 12.22mL 6.11mL

参考文献

[1]White WF, Snodgrass SR. Isoguvacine binding, uptake, and release: relation to the GABA system. J Neurochem. 1983 Jun;40(6):1701-8 [2]Xi ZX, Akasu T. Presynaptic GABAA receptors in vertebrate synapses. Kurume Med J. 1996;43(2):115-22 [3]Ding L, Gao R, Xiong XQ, Gao XY, Chen Q, Li YH, Kang YM, Zhu GQ. GABA in Paraventricular Nucleus Regulates Adipose Afferent Reflex in Rats. PLoS One. 2015 Aug 28;10(8):e0136983 [4]Farmer DG, Dutschmann M, Paton JF, Pickering AE, McAllen RM. Brainstem sources of cardiac vagal tone and respiratory sinus arrhythmia. J Physiol. 2016 Dec 15;594(24):7249-7265 [5]Wahab A, Heinemann U, Albus K. Effects of gamma-aminobutyric acid (GABA) agonists and a GABA uptake inhibitor on pharmacoresistant seizure like events in organotypic hippocampal slice cultures. Epilepsy Res. 2009 Oct;86(2-3):113-23