Cabergoline

Catalog No.S5842 Synonyms: FCE-21336

Cabergoline Chemical Structure

Molecular Weight(MW): 451.60

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

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Biological Activity

Description Cabergoline, 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

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 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].

Protocol

Solubility (25°C)

In vitro DMSO 90 mg/mL (199.29 mM)
Ethanol 90 mg/mL (199.29 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 451.60
Formula

C26H37N5O2

CAS No. 81409-90-7
Storage powder
in solvent
Synonyms FCE-21336

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03965572 Recruiting -- Lactation Suppressed|Cabergoline Adverse Reaction|Postpartum DVT|Postpartum Depression Laniado Hospital June 7 2019 --
NCT03457389 Not yet recruiting Drug: Cabergoline Pituitary Adenoma|Prolactinoma|Pituitary Tumor|Recurrence Tumor Seoul National University Hospital October 1 2018 Not Applicable
NCT01915303 Active not recruiting Drug: Pasireotide with or without cabergoline Cushing''s Disease Novartis Pharmaceuticals|Novartis March 6 2014 Phase 2
NCT01651364 Completed Drug: Placebo|Drug: Cabergoline Cocaine Dependence|Cocaine Abuse|Cocaine Addiction|Substance Abuse Baylor College of Medicine|National Institute on Drug Abuse (NIDA) July 2011 Phase 1
NCT01270711 Completed Drug: Study Drug Parkinson''s Disease|Hyperprolactinemia Pfizer November 2010 --
NCT01009567 Completed Drug: Cabergoline|Drug: Control Ovarian Hyperstimulation Syndrome Royan Institute June 2009 Phase 1|Phase 2

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Dopamine Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID