Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C19H20Br2N2O3 |
Molecular Weight | 484.182 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1(C)OC[C@H](NC(=O)NC2=CC=C(Br)C=C2Br)[C@@H](O1)C3=CC=CC=C3
InChI
InChIKey=RBKIJGLHFFQHBE-IRXDYDNUSA-N
InChI=1S/C19H20Br2N2O3/c1-19(2)25-11-16(17(26-19)12-6-4-3-5-7-12)23-18(24)22-15-9-8-13(20)10-14(15)21/h3-10,16-17H,11H2,1-2H3,(H2,22,23,24)/t16-,17-/m0/s1
Molecular Formula | C19H20Br2N2O3 |
Molecular Weight | 484.182 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/15261275Curator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/21181123 |
https://www.ncbi.nlm.nih.gov/pubmed/17638707 |
https://www.ncbi.nlm.nih.gov/pubmed/24592208 |
https://www.ncbi.nlm.nih.gov/pubmed/19363060 | https://www.ncbi.nlm.nih.gov/pubmed/17638707
Sources: https://www.ncbi.nlm.nih.gov/pubmed/15261275
Curator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/21181123 |
https://www.ncbi.nlm.nih.gov/pubmed/17638707 |
https://www.ncbi.nlm.nih.gov/pubmed/24592208 |
https://www.ncbi.nlm.nih.gov/pubmed/19363060 | https://www.ncbi.nlm.nih.gov/pubmed/17638707
JNJ-10397049 is a potent and selective antagonist of the orexin-2 receptor. JNJ-10397049 regulated ovulation, and sleep promotion. JNJ-10397049 was reported to be effective in reducing the reinforcing effects of ethanol.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL4792 |
8.3 null [pKi] | ||
Target ID: CHEMBL5113 Sources: https://www.ncbi.nlm.nih.gov/pubmed/22796453 |
5.18 null [pKi] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
PubMed
Title | Date | PubMed |
---|---|---|
Both orexin receptors are expressed in rat ovaries and fluctuate with the estrous cycle: effects of orexin receptor antagonists on gonadotropins and ovulation. | 2007 Oct |
|
Selective blockade of the orexin-2 receptor attenuates ethanol self-administration, place preference, and reinstatement. | 2011 May |
|
Effects of orexins A and B on expression of orexin receptors and progesterone release in luteal and granulosa ovarian cells. | 2012 Oct 10 |
|
Orexin-1 receptor blockade dysregulates REM sleep in the presence of orexin-2 receptor antagonism. | 2014 |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/21181123
JNJ-10397049 (1, 3, and 10 mg/kg, sc) dose-dependently reduced ethanol self-administration without changing saccharin self-administration, dopamine levels, or withdrawal signs in rats. Treatment with JNJ-10397049 (10 mg/kg, sc) attenuated the acquisition, expression, and reinstatement of ethanol conditioned place preference and ethanol-induced hyperactivity in mice.
Route of Administration:
Other
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/24333629
Curator's Comment: Both orexin A and orexin B increased FSH and LH secretion in vitro in anterior pituitary cells of proestrous rats; these effects was suppressed by the orexin 2 receptor antagonist JNJ-1039704
Unknown
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 08:36:14 GMT 2023
by
admin
on
Sat Dec 16 08:36:14 GMT 2023
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Record UNII |
1B419P24AV
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Record Status |
Validated (UNII)
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Record Version |
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DTXSID501336831
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JNJ-10397049
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1B419P24AV
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9869934
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admin on Sat Dec 16 08:36:14 GMT 2023 , Edited by admin on Sat Dec 16 08:36:14 GMT 2023
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Related Record | Type | Details | ||
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ACTIVE MOIETY |