Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C12H14N2 |
Molecular Weight | 186.253 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CN1CCC[C@H]1C2=CN=CC(=C2)C#C
InChI
InChIKey=NUPUDYKEEJNZRG-LBPRGKRZSA-N
InChI=1S/C12H14N2/c1-3-10-7-11(9-13-8-10)12-5-4-6-14(12)2/h1,7-9,12H,4-6H2,2H3/t12-/m0/s1
Molecular Formula | C12H14N2 |
Molecular Weight | 186.253 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
DescriptionCurator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/10812948
https://www.ncbi.nlm.nih.gov/pubmed/18692487
Curator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/10812948
https://www.ncbi.nlm.nih.gov/pubmed/18692487
Altinicline (SIB-1508Y, SIB-1765F) is a drug which acts as an agonist at neural nicotinic acetylcholine receptors with high selectivity for the α4β2 subtype. It stimulates release of dopamine and acetylcholine in the brain in both rodent and primate models, and progressed as far as Phase II clinical trials for Parkinson's disease, where "no antiparkinsonian or cognitive-enhancing effects were demonstrated", although its current status is unclear.
CNS Activity
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL3301382 Sources: http://jpet.aspetjournals.org/content/280/1/373.full |
7.5 nM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
Doses
Dose | Population | Adverse events |
---|---|---|
40 mg 2 times / day multiple, oral (unknown) Highest studied dose Dose: 40 mg, 2 times / day Route: oral Route: multiple Dose: 40 mg, 2 times / day Sources: |
unhealthy, ADULT n = 16 Health Status: unhealthy Condition: Parkinson disease Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 16 Sources: |
Other AEs: Nausea and vomiting... |
10 mg 2 times / day multiple, oral (unknown) MTD Dose: 10 mg, 2 times / day Route: oral Route: multiple Dose: 10 mg, 2 times / day Sources: |
unhealthy, ADULT n = 16 Health Status: unhealthy Condition: Parkinson disease Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 16 Sources: |
Other AEs: Lightheadedness, Dizziness... |
20 mg 2 times / day multiple, oral (unknown) Studied dose Dose: 20 mg, 2 times / day Route: oral Route: multiple Dose: 20 mg, 2 times / day Sources: |
unhealthy, ADULT n = 16 Health Status: unhealthy Condition: Parkinson disease Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 16 Sources: |
Disc. AE: Thrombocytopenia... AEs leading to discontinuation/dose reduction: Thrombocytopenia (serious, 1 pt) Sources: |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Nausea and vomiting | 40 mg 2 times / day multiple, oral (unknown) Highest studied dose Dose: 40 mg, 2 times / day Route: oral Route: multiple Dose: 40 mg, 2 times / day Sources: |
unhealthy, ADULT n = 16 Health Status: unhealthy Condition: Parkinson disease Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 16 Sources: |
|
Dizziness | 10 mg 2 times / day multiple, oral (unknown) MTD Dose: 10 mg, 2 times / day Route: oral Route: multiple Dose: 10 mg, 2 times / day Sources: |
unhealthy, ADULT n = 16 Health Status: unhealthy Condition: Parkinson disease Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 16 Sources: |
|
Lightheadedness | 10 mg 2 times / day multiple, oral (unknown) MTD Dose: 10 mg, 2 times / day Route: oral Route: multiple Dose: 10 mg, 2 times / day Sources: |
unhealthy, ADULT n = 16 Health Status: unhealthy Condition: Parkinson disease Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 16 Sources: |
|
Thrombocytopenia | serious, 1 pt Disc. AE |
20 mg 2 times / day multiple, oral (unknown) Studied dose Dose: 20 mg, 2 times / day Route: oral Route: multiple Dose: 20 mg, 2 times / day Sources: |
unhealthy, ADULT n = 16 Health Status: unhealthy Condition: Parkinson disease Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 16 Sources: |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/16476941
10 mg daily
Route of Administration:
Oral
In Vitro Use Guide
Sources: http://jpet.aspetjournals.org/content/280/1/373.full
[3H]-DA uptake in rat striatal synaptosomes was conducted as described before: briefly, 100 μl of crude P2 synaptosomal fraction were preincubated in the presence of varying concentrations of test compounds (SIB-1765F) for 10 min before the addition of [3H]-DA final concentration of 10 nM
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 16:47:02 GMT 2023
by
admin
on
Sat Dec 16 16:47:02 GMT 2023
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Record UNII |
RJ9V9V09VM
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Record Status |
Validated (UNII)
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Record Version |
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-
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NCI_THESAURUS |
C73579
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7916
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179120-92-4
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ALTINICLINE
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DTXSID40870143
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CHEMBL111659
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3036156
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C77841
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300000037027
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RJ9V9V09VM
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Related Record | Type | Details | ||
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SALT/SOLVATE -> PARENT |
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TARGET -> AGONIST |
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
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