Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C19H21NO2 |
Molecular Weight | 295.3755 |
Optical Activity | ( - ) |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
[H][C@@]12CC3=CC=C(O)C(O)=C3C4=C1C(CCN2CCC)=CC=C4
InChI
InChIKey=BTGAJCKRXPNBFI-OAHLLOKOSA-N
InChI=1S/C19H21NO2/c1-2-9-20-10-8-12-4-3-5-14-17(12)15(20)11-13-6-7-16(21)19(22)18(13)14/h3-7,15,21-22H,2,8-11H2,1H3/t15-/m1/s1
Propylnorapomorphine is a potent and selective D2 receptor agonist. Propylnorapomorphine is used as a tool compound to label dopamine receptors in rodent brain, and elicits dopaminergic behavioural effects. It stimulates motor activity, induces stereotypic behaviour and sexual stimulation. Propylnorapomorphine was investigated in clinical trial against Parkinson's disease and schizophrenia
CNS Activity
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: CHEMBL217 |
10.12 null [pKi] | ||
Target ID: CHEMBL234 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24325578 |
8.74 null [pKi] | ||
Target ID: P14416 Gene ID: 1813.0 Gene Symbol: DRD2 Target Organism: Homo sapiens (Human) |
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Target ID: P35462 Gene ID: 1814.0 Gene Symbol: DRD3 Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/12831994 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
PubMed
Title | Date | PubMed |
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Aporphines. 15. Action of aporphine alkaloids on dopaminergic mechanisms in rat brain. | 1976 Jan |
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3H-N-n-propylnorapomorphine: a novel agonist ligand for central dopamine receptors. | 1979 Jul 1 |
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Kinetics of the uptake and distribution of the dopamine D(2,3) agonist (R)-N-[1-(11)C]n-propylnorapomorphine in brain of healthy and MPTP-treated Göttingen miniature pigs. | 2003 Jul |
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Effects of unilateral 6-OHDA lesions on [3H]-N-propylnorapomorphine binding in striatum ex vivo and vulnerability to amphetamine-evoked dopamine release in rat. | 2011 Feb |
Patents
Sample Use Guides
In a clinical study against Parkinson's disease, propylnorapomorphine was administered orally. The most effect was observed at doses of 10 to 15 mg six time per day. In rodents, propylnorapomorphine is administered intraperitoneally.
Route of Administration:
Other
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/24325578
Binding to dopamine D2 receptor was determined using [3H]spiperone as radioligand and HEK293 cells, expressing recombinant human D2. Dose-response curves were converted to Ki values. pKi for propylnorapomorphine is 10.12.
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18426-20-5
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NH381P1BR8
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167715
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ACTIVE MOIETY
SALT/SOLVATE (PARENT)