research use only
Cat.No.S2011
| Related Targets | Adrenergic Receptor AChR 5-HT Receptor COX Calcium Channel Histamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE) GluR |
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| Other Dopamine Receptor Inhibitors | MPTP Hydrochloride Trifluoperazine Trifluoperazine 2HCl Penfluridol Sulpiride SCH-23390 hydrochloride SKF38393 HCl Levosulpiride Domperidone Rotundine |
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In vitro |
DMSO
: 60 mg/mL
(198.5 mM)
Water : 60 mg/mL Ethanol : Insoluble |
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In vivo |
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| Molecular Weight | 302.26 | Formula | C10H17N3S.2HCl.H2O |
Storage (From the date of receipt) | |
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| CAS No. | 191217-81-9 | Download SDF | Storage of Stock Solutions |
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| Synonyms | N/A | Smiles | CCCNC1CCC2=C(C1)SC(=N2)N.O.Cl.Cl | ||
| Targets/IC50/Ki |
D2S Receptor
D2L Receptor
D3 receptor
D4 receptor
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|---|---|
| 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+. Pramipexole decreases the levels of dopamine metabolites dose dependently, whereas striatal dopamine levels remains unchanged. 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. 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.
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| In vivo |
Pramipexole (0.001-1 mg/kg s.c.) reduces exploratory locomotor activity in mice. Pramipexole (1 mg/kg, p.o.) is able to significantly reduce the increased DA turnover, but by only 16%.
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References |
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(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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