生物活性

• 靶点	Dopamine Receptor D2 EC50:13nM

• 描述Metoclopramide hydrochloride hydrate is a dopamine D2 antagonist that is used as an antiemetic. It can peripherally improvie gastric emptying, and centrally result in an anti-emetic effect. Metoclopramide side effects, mostly related to its ability to cross the blood-brain barrier, include drowsiness, restlessness, hyperprolactinemia, and tardive dyskinesia (TD), a movement disorder that may be irreversible^[3]. In a randomised crossover trial in 40 patients, intranasal metoclopramide or oral metoclopramide, both with dexamethasone, were equally effective in the control of delayed emesis induced by moderately-emetogenic chemotherapy. One 30 patient study suggests that intranasal metoclopramide has similar efficacy to oral metoclopramide in the treatment of functional dyspepsia. Intranasal metoclopramide caused minor irritation of the nasal membrane and unpleasant taste in some patients, but was otherwise well tolerated^[4]. Metoclopramide's gastrointestinal smooth muscle stimulatory effects are related to its ability to antagonize the inhibitory neurotransmitter, dopamine; to augment acetylcholine release and sensitize the muscarinic receptors of the gastrointestinal smooth muscle; and to coordinate gastric-pyloric-small intestinal motor function. Adverse effects, which may occur in up to 20% of patients, include drowsiness, lassitude, and akathisia; all are usually mild, transient, and reversible^[5].