CAS |
No.4205-91-8 |
中文名称 |
盐酸可乐定(10mM in DMSO,无菌) |
英文名称 |
Clonidine Hydrochloride(10mM in DMSO,Sterile) |
分子式 |
C9H9Cl2N3·HCl |
分子量 |
266.55 |
溶解性 |
请根据自己的实验要求使用。 |
外观(性状) |
无菌溶液 |
储存条件 |
Stroe at -20℃,6 months. |
运输条件 |
冷冻运输 |
靶点 |
Adrenergic Receptor |
通路 |
Endocrinology & Hormones;GPCR & G Protein;Neuronal Signaling |
背景说明 |
Clonidine hydrochloride 是 α2-adrenoceptor 激动剂。 |
生物活性 |
Clonidine hydrochloride is an agonist of α2-adrenoceptor and potent antihypertensive agent.[1-4] |
In Vitro |
Clonidine (0.01, 0.1 or 1 μM) significantly induces CGRP (α and β) mRNA expression in a dose-dependent manner in endothelial cells. Clonidine treatment (1 μM) for 24 h significantly increases the NO level in endothelial cells. NO pathway modulates CGRP production induced by clonidine[2]. |
In Vivo |
Clonidine (50 μg/kg, i.p.) induces a significant decrease in body temperature of rat lasting 3 hr, with the maximum at 1 hr after administration. An intracerebroventricular pretreatment of rats with neutral doses of phentolamine 15 min before clonidine considerably antagonizes the clonidine-induced hypothermia[1]. Clonidine (0.003-0.05 mg/kg, i.p.) potently suppresses dopamine efflux in the prefrontal cortex induced by PCP. Pretreatment with the alpha-2A receptor antagonist (BRL-44408) prevents clonidine from suppressing PCP-induced dopamine overflow in the prefrontal cortex[3]. In DMSO-pretreated SO rats, clonidine (0.6 μg i.c.) has no effect on blood pressure. However, after central adenosine A1R blockade (DPCPX) in SO rats, clonidine significantly (P 0.05, one-way ANOVA) clonidine-evoked reduction in blood pressure in ABD rats. In DPCPX-pretreated SO rats and along with the appearance of the hypotensive response, clonidine causes a significant (P [4]. |
动物实验 |
On the day of the experiment, the flow rate is increased to 2 μL/min approximately 2 h before beginning the collection of baseline samples. Dialysates are collected every 20 min; after 4 baseline samples are collected, animals are pretreated with an intra-peritoneal (i.p.) injection of either 0.9% saline (the vehicle), clonidine (0.0033, 0.01 or 0.05 mg/kg) or guanfacine (0.05 or 0.5 mg/kg), before receiving an injection of PCP (2.5 mg/kg, i.p.) 20 min later. In a separate study, BRL (1.0 mg/kg) is administered 20 min prior to clonidine. In addition, for some control experiments, the animals only receive one injection of saline, clonidine (0.01 or 0.05 mg/kg), guanfacine (0.5 mg/kg) or BRL (1.0 mg/kg). |
数据来源文献 |
[1]. Bugajski J, et al. The involvement of central alpha-adrenergic and histamine H2-receptors in the hypothermia induced by clonidine in the rat. Neuropharmacology. 1980 Jan;19(1):9-15. [2]. Nassar N, et al. Brainstem adenosine A1 receptor signaling masks phosphorylated extracellular signal-regulated kinase 1/2-dependent hypotensive action of clonidine in conscious normotensive rats. J Pharmacol Exp Ther. 2009 Jan;328(1):83-9. [3]. Zhang YM, et al. Clonidine induces calcitonin gene-related peptide expression via nitric oxide pathway in endothelial cells. Peptides. 2009 Sep;30(9):1746-52. [4]. Jentsch JD, et al. Clonidine and guanfacine attenuate phencyclidine-induced dopamine overflow in rat prefrontal cortex: mediating influence of the alpha-2A adrenoceptor subtype. Brain Res. 2008 Dec 30;1246:41-6. |
规格 |
0.1ml 0.3ml 0.5ml 1ml 1.5ml |
单位 |
瓶 |