Details
Stereochemistry | ACHIRAL |
Molecular Formula | C27H29N3O3 |
Molecular Weight | 443.5375 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
COC(=O)CN1CN(C2=CC=CC=C2)C3(CCN(CC4=C5C=CC=CC5=CC=C4)CC3)C1=O
InChI
InChIKey=AQMPIDSGLFVVPL-UHFFFAOYSA-N
InChI=1S/C27H29N3O3/c1-33-25(31)19-29-20-30(23-11-3-2-4-12-23)27(26(29)32)14-16-28(17-15-27)18-22-10-7-9-21-8-5-6-13-24(21)22/h2-13H,14-20H2,1H3
Molecular Formula | C27H29N3O3 |
Molecular Weight | 443.5375 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
CNS Activity
Curator's Comment: Initial
behavioural studies have shown that NNC 63-0532 induces
eects that are consistent with central ORL1 activation upon
peripheral (s.c.) administration (facilitation of lordosis
behaviour and depression of locomotor activity), indicating that the compound does
cross the blood brain barrier.
Originator
Sources: https://www.ncbi.nlm.nih.gov/pubmed/11053209
Curator's Comment: Novo Nordisk A/S, Department of Molecular Pharmacology, Novo Nordisk Park, Denmark.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL2014 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11053209 |
305.0 nM [EC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/28856406
Rats: NNC 63-0532 was microinjected at 2, 20, and
200 nmol. The blockade of GABAA receptors in the dlSC elicited defensive
alertness (Tukey’s post hoc test; p < 0.001) that was
increased by the SNpr pretreatment with NNC 63-0532 at
the highest dose (200 nmol)
Route of Administration:
Other
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/16407766
Curator's Comment: A series of nociceptin receptor ligands has been investigated in relationship to their capability to promote receptor endocytosis, desensitization (evaluated as inhibition of forskolin-stimulated cAMP production) and compensatory upregulation of adenylyl cyclase activity in CHO-K1 cells expressing the cloned human nociceptin receptor.
Nociceptin (NC), [Arg14, Lys15]NC-NH2 and NNC 63-0532 (0.01 nM-10 uM) induce a concentration-dependent endocytosis and recycling of the nociceptin receptor.
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 09:30:10 GMT 2023
by
admin
on
Sat Dec 16 09:30:10 GMT 2023
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Record UNII |
73663SY1DT
|
Record Status |
Validated (UNII)
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Record Version |
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-
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9803475
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NNC 63-0532
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250685-44-0
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73663SY1DT
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DTXSID40397885
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admin on Sat Dec 16 09:30:10 GMT 2023 , Edited by admin on Sat Dec 16 09:30:10 GMT 2023
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Related Record | Type | Details | ||
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ACTIVE MOIETY |