Metoclopramide

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的多巴胺 D2 受体拮抗剂，Ki 为 28 nM；也是一种混合的 5-HT3 受体拮抗剂/5-HT4 受体激动剂。

A potent dopamine D2 receptor antagonist with Ki of 28 nM; also is a mixed 5-HT3 receptor antagonist/5-HT4 receptor agonist; commonly used to treat nausea and vomiting caused by chemotherapy.Chemotherapeutic Agents Phase 2 Discontinued(In Vitro):Metoclopramide (0.01-10 μM) stimulates aldosterone release in isolated perfused rat zona glomerulosa cells.Metoclopramide results in prokinesis by four mechanisms: inhibition of presynaptic D2 receptors and stimulation of presynaptic excitatory 5-HT4 receptors, thereby allowing acetylcholine (ACh) release from intrinsic cholinergic motor neurons; inhibition of D2 postsynaptic receptors; and antagonism of the presynaptic inhibition of muscarinic receptors, leading to further augmentation of ACh release.(In Vivo):Metoclopramide (6.7 μg/g; s.c. daily for 50 days) 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.) induces catalepsy and antagonizes Apomorphine induced cage climbing behaviour in mice.Metoclopramide (1.25-2.5 mg/kg; i.p.) induces stereotyped cage climbing behaviour in mice.

Metoclopramide (0.01-10 μM) stimulates aldosterone release in isolated perfused rat zona glomerulosa cells.Metoclopramide results in prokinesis by four mechanisms: inhibition of presynaptic D2 receptors and stimulation of presynaptic excitatory 5-HT4 receptors, thereby allowing acetylcholine (ACh) release from intrinsic cholinergic motor neurons; inhibition of D2 postsynaptic receptors; and antagonism of the presynaptic inhibition of muscarinic receptors, leading to further augmentation of ACh release.

Metoclopramide (6.7 μg/g; s.c. daily for 50 days) 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.) induces catalepsy and antagonizes Apomorphine induced cage climbing behaviour in mice.Metoclopramide (1.25-2.5 mg/kg; i.p.) induces stereotyped cage climbing behaviour in mice. Animal Model:Adult, virgin female mice of the Swiss EPM-1 strain Dosage:6.7 μg/g Administration:S.c. daily for 50 days Result:Increased the number but also stimulated the metabolic activity of lactotrophs.

Metoclopramide, Afipran, Maxolon, Reglan, Maxeran, Cerucal

GPCR/G Protein

Dopamine Receptor

dopamine D2

Cancer

Chemotherapeutic

364-62-5

299.7964

C14H22ClN3O2

>98% (HPLC)

DMSO: ≥ 41 mg/mL

O=C(NCCN(CC)CC)C1=CC(Cl)=C(N)C=C1OC

Benzamide, 4-amino-5-chloro-N-[2-(diethylamino)ethyl]-2-methoxy-

(-20℃)

With Ice Pack

≥ 2 years