| Identification | Back Directory | [Name]
Carbamic acid, N-[3-chloro-5-[1-[[6-[2-(5-ethyl-4-methyl-2-thiazolyl)ethyl]-4-(4-morpholinyl)-2-pyridinyl]amino]ethyl]phenyl]-, 1-methylethyl ester | [CAS]
329716-61-2 | [Synonyms]
J115814
J-115814
UNII-81DP93CF8M
J 115814J-115814
Carbamic acid, N-[3-chloro-5-[1-[[6-[2-(5-ethyl-4-methyl-2-thiazolyl)ethyl]-4-(4-morpholinyl)-2-pyridinyl]amino]ethyl]phenyl]-, 1-methylethyl ester | [Molecular Formula]
C29H38ClN5O3S | [MOL File]
329716-61-2.mol | [Molecular Weight]
572.16 |
| Hazard Information | Back Directory | [Uses]
J-115814 is a potent and selective neuropeptide Y1 antagonist with Ki values of 1.4, 1.8, 1.9, >10000, 620, 6000, >10000 nM for hY1, rY1, mY1, hY2, hY4, hY5, mY6, respectively. J-115814 inhibits feeding behaviors[1]. | [in vivo]
J-115814 (0.3, 1, 3, 10 mg/kg; i.v.) inhibits NPY-induced feeding in SD rats[1].
J-115814 (3, 10, 30 mg/kg; i.p.) shows anorexigenic effect in mice[1]. | Animal Model: | db/db and lean C57BL6 mice[1] | | Dosage: | 3, 10, 30 mg/kg | | Administration: | I.p. | | Result: | Decreasesd nocturnal food intake in a dose-dependent manner. |
| Animal Model: | SD rats[1] | | Dosage: | 0.3, 1, 3, 10 mg/kg | | Administration: | I.v.; 1 h before ICV NPY | | Result: | Inhibited NPY-induced feeding with significant responses at 3 and 10 mg/kg. |
| [IC 50]
hY1 receptor: 1.4 nM (Ki); rNPY Y1 receptor: 1.8 nM (Ki); mY1: 1.9 nM (Ki); hY4 receptor: 620 nM (Ki); hY5 receptor: 6000 nM (Ki); human Y2 receptor: >10000 nM (Ki); mY6: >10000 nM (Ki) | [References]
[1] Kanatani A, et al. A typical Y1 receptor regulates feeding behaviors: effects of a potent and selective Y1 antagonist, J-115814. Mol Pharmacol. 2001 Mar;59(3):501-5. DOI:10.1124/mol.59.3.501 |
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