Home Neuronal Signaling Dopamine Receptor agonist Pramipexole 2HCl Monohydrate

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Pramipexole 2HCl Monohydrate Dopamine Receptor agonist

Cat.No.S2011

Pramipexole 2HCl Monohydrate is a novel non-ergoline dopamine (DA) agonist, used to treat Parkinson's disease.
Pramipexole 2HCl Monohydrate Dopamine Receptor agonist Chemical Structure

Chemical Structure

Molecular Weight: 302.26

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Chemical Information, Storage & Stability

Molecular Weight 302.26 Formula

C10H17N3S.2HCl.H2O

 Storage (From the date of receipt)
CAS No. 191217-81-9 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CCCNC1CCC2=C(C1)SC(=N2)N.O.Cl.Cl

Solubility

In vitro
Batch:

DMSO : 60 mg/mL ( (198.5 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 60 mg/mL

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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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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Mechanism of Action

Targets/IC50/Ki
D2S Receptor [1]
D2L Receptor [1]
D3 receptor [1]
D4 receptor [1]
In vitro
Pramipexole, a chemically novel dopamine agonist used for the treatment of Parkinson's disease symptoms, possesses antioxidant activity and is neuroprotective toward substantia nigral dopamine neurons in hypoxic-ischemic and methamphetamine models. Pramipexole reduces the levels of oxygen radicals produced by methylpyridinium ion (MPP+) both when incubated with SH-SY5Y cells and when perfused into rat striatum. Pramipexole also exhibits a concentration-dependent inhibition of opening of the mitochondrial transition pore induced by calcium and phosphate or MPP+. [1] Pramipexole decreases the levels of dopamine metabolites dose dependently, whereas striatal dopamine levels remains unchanged. [2] Pramipexole acts in both of these models to reduce the elevated dopamine turnover and the associated elevation in hydroxyl radical production secondary to increased MAO activity that could be responsible for oxidative damage to the nigrostriatal neurons. [3] Pramipexole (4-100 mM) significantly attenuates DA- or L-DOPA-induced cytotoxicity and apoptosis, an action which is not blocked by D3 antagonist U-99194 A or D2 antagonist raclopride. Pramipexole also protects MES 23.5 cells from hydrogen peroxide-induced cytotoxicity in a dose-dependent manner. Pramipexole can effectively inhibit the formation of melanin, an end product resulting from DA or L-DOPA oxidation in cell-free system. [4]
In vivo
Pramipexole (0.001-1 mg/kg s.c.) reduces exploratory locomotor activity in mice. [2] Pramipexole (1 mg/kg, p.o.) is able to significantly reduce the increased DA turnover, but by only 16%. [3]
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06269146 Not yet recruiting
Anxiety Disorders|Anxiety|Depression|Social Disconnection
University of California San Diego|National Institute of Mental Health (NIMH)|New York State Psychiatric Institute
 February 2024 Phase 2
NCT03683225 Active not recruiting
Idiopathic Parkinson Disease
Chase Therapeutics Corporation
 April 1 2019 Phase 2
NCT03642964 Active not recruiting
Major Depressive Disorder (MDD)
Chase Therapeutics Corporation
 September 10 2018 Phase 2
NCT02101138 Unknown status
Hypereosinophilic Syndrome
National Institute of Allergy and Infectious Diseases (NIAID)|Knopp Biosciences|National Institutes of Health Clinical Center (CC)
 March 14 2014 Phase 2
NCT01733199 Completed
Parkinson''s Disease|Secondary Behavioural Addiction
Nantes University Hospital
 October 2012 Phase 4
NCT01607034 Completed
Healthy Volunteers
Knopp Biosciences
 June 2012 Phase 1

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