产品描述: | Metoclopramide hydrochloride hydrate is a potent antagonist of 5-HT3 and dopamine D2 receptor, with IC50s of 308 nM and 483 nM, respectively. Metoclopramide hydrochloride hydrate can be used for the research of nausea and vomiting, gastro-oesophageal reflux, and gastroparesis |
靶点: |
5-HT3 Receptor:308 nM (IC50);D2 Receptor:483 nM (IC50);DopamineReceptor;5-HTReceptor |
体内研究: |
Metoclopramide (6.7 µg/g; s.c. daily for 50 days) hydrochloride hydrate significantly increases the number and the volume of lactotroph cells of the pituitary gland during all phases of the estrous cycle. Metoclopramide (5-40 mg/kg; i.p.) hydrochloride hydrate induces catalepsy and antagonizes Apomorphine induced cage climbing behaviour in mice. Metoclopramide (1.25-2.5 mg/kg; i.p.) hydrochloride hydrate induces stereotyped cage climbing behaviour in mice. |
参考文献: |
1. Hirokawa Y, et, al. Synthesis and structure-activity relationships of 4-amino-5-chloro-N-(1,4-dialkylhexahydro-1,4-diazepin-6-yl)-2-methoxybenzamide derivatives, novel and potent serotonin 5-HT3 and dopamine D2 receptors dual antagonist. Chem Pharm Bull 2. Rao AS, et, al. Review article: metoclopramide and tardive dyskinesia. Aliment Pharmacol Ther. 2010 Jan;31(1):11-9. 3. Edwards CR, et, al. In vivo and in vitro studies on the effect of metoclopramide on aldosterone secretion. Clin Endocrinol (Oxf). 1980 Jul;13(1):45-50. 4. Bhosale KB, et, al. Dose-dependent response of central dopaminergic systems to metoclopramide in mice. Indian J Exp Biol. 1997 Jun;35(6):618-22. 5. Gomes RCT, et, al. Effects of metoclopramide on the mouse anterior pituitary during the estrous cycle. Clinics (Sao Paulo). 2011;66(6):1101-4. |
溶解性: |
DMSO : 50 mg/mL (141.14 mM; Need ultrasonic) H2O : 0.1 mg/mL (0.28 mM; Need ultrasonic) |
保存条件: |
RT |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
2.823 ml |
14.114 ml |
28.227 ml |
5 mM |
0.565 ml |
2.823 ml |
5.645 ml |
10 mM |
0.282 ml |
1.411 ml |
2.823 ml |
50 mM |
0.056 ml |
0.282 ml |
0.565 ml |
|
注意: |
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