Cabergoline

Synonyms: FCE-21336

Cabergoline (FCE-21336), an ergot derivative, is a long-acting dopamine agonist and prolactin inhibitor.

Cabergoline Chemical Structure

Cabergoline Chemical Structure

CAS: 81409-90-7

Selleck's Cabergoline has been cited by 1 publication

Purity & Quality Control

Batch: Purity: 99.82%
99.82

Cabergoline Related Products

Choose Selective Dopamine Receptor Inhibitors

Biological Activity

Description Cabergoline (FCE-21336), an ergot derivative, is a long-acting dopamine agonist and prolactin inhibitor.
Targets
D2 receptor [1] 5-HT2 [1] 5-HT2B [1] D3 receptor [1] D4 receptor [1]
0.7 nM 1.2 nM 1.2 nM 1.5 nM 9 nM
In vitro
In vitro Cabergoline prevents the oxidative stress-induced cell death of cultured cortical neurons via a D2 receptor-mediated mechanism. Cabergoline suppresses the activation of ERK signaling, which might have a role in the neuroprotection. Cabergoline significantly represses extracellular glutamate accumulation triggered by oxidative stress, and increases the expression of glutamate transporters including EAAC1, which is known to be involved in the clearance of extracellular glutamate[1].
In Vivo
In vivo Cabergoline has a long elimination half-life (63 to 109 h). An in vivo study of neuronal damage induced by intracerebroventricular (icv) injection of 6-OHDA, a neurotoxic compound that selectively damages dopaminergic neurons in male ICR mice, demonstrates that intraperitoneal (ip) administration of cabergoline for 7 days prevented nigrostriatal region dopaminergic neurons from cell death. Cabergoline also protects SH-SY5Y neuroblastoma from cell death by oxygen-glucose deprivation even when cabergoline is administered after the induction of cell death. Cabergoline increases hippocampal brain-derived neurotrophic factor (BDNF, an important regulator in the synaptic plasticity) and exerts an antidepressant effect in rats[1].
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03965572 Unknown status
Lactation Suppressed|Cabergoline Adverse Reaction|Postpartum DVT|Postpartum Depression
Laniado Hospital
June 7 2019 --
NCT03457389 Recruiting
Pituitary Adenoma|Prolactinoma|Pituitary Tumor|Recurrence Tumor
Seoul National University Hospital
February 22 2018 Not Applicable
NCT01651364 Completed
Cocaine Dependence|Cocaine Abuse|Cocaine Addiction|Substance Abuse
Baylor College of Medicine|National Institute on Drug Abuse (NIDA)
July 2011 Phase 1
NCT01270711 Completed
Parkinson''s Disease|Hyperprolactinemia
Pfizer
November 2010 --
NCT01009567 Completed
Ovarian Hyperstimulation Syndrome
Royan Institute
June 2009 Phase 1|Phase 2
NCT00153972 Completed
Parkinson''s Disease
Technische Universität Dresden|Pfizer
February 2005 Phase 4

Chemical Information & Solubility

Molecular Weight 451.60 Formula

C26H37N5O2

CAS No. 81409-90-7 SDF --
Smiles CCNC(=O)N(CCCN(C)C)C(=O)C1CC2C(CC3=CNC4=CC=CC2=C34)N(C1)CC=C
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 90 mg/mL ( (199.29 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 90 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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