A potent and selective dopamine D2 receptor agonist (Kis = 0.912 and 6

Cabergoline – 50 mg

Brand:
Cayman
CAS:
81409-90-7
Storage:
-20
UN-No:
Non-Hazardous - /

Cabergoline is a potent and selective dopamine D2 receptor agonist (Kis = 0.912 and 6,935 nM for D2 and D1 receptors, respectively, in rat striatum) that inhibits the secretion of prolactin (PRL) and growth hormone.{41336,41337} It inhibits PRL secretion in and growth of rat pituitary tumor cells in a concentration-dependent manner, an effect which can be reversed by the dopamine D2 receptor antagonist haloperidol (Item No. 12014).{41337} Cabergoline suppresses the mammalian target of rapamycin (mTOR) signaling pathway in a time-dependent manner and induces autophagy and cell death in MMQ and GH3 rat pituitary cells.{41338} In vivo, cabergoline (0.25 mg/kg) stimulates motor activity and decreases dyskinesias in a monkey model of Parkinson’s disease induced by MPTP.{41339} Formulations containing cabergoline have been used to treat prolactinomas.  

 

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Description

A potent and selective dopamine D2 receptor agonist (Kis = 0.912 and 6,935 nM for D2 and D1 receptors, respectively, in rat striatum); inhibits PRL secretion in and growth of rat pituitary tumor cells in a concentration-dependent manner; suppresses the mTOR signaling pathway in a time-dependent manner and induces autophagy and cell death in MMQ and GH3 rat pituitary cells; stimulates motor activity and decreases dyskinesias in a monkey model of MPTP-induced Parkinson’s disease when administered at a dose of 0.25 mg/kg

Formal name: N-[3-(dimethylamino)propyl]-N-[(ethylamino)carbonyl]-6-(2-propen-1-yl)-ergoline-8β-carboxamide

Synonyms:  FCE 21336

Molecular weight: 451.6

CAS: 81409-90-7

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Cancer||Research Area|Endocrinology & Metabolism|Reproductive Biology||Research Area|Neuroscience|Neurodegenerative Disorders|Parkinson’s Disease

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