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| Content Provider | World Health Organization (WHO)-Global Index Medicus |
|---|---|
| Author | Walker, Mary W. Wolinsky, Toni D. Jubian, Vrej Chandrasena, Gamini Zhong, Huailing Huang, Xinyan Miller, Silke Hegde, Laxminarayan G. Marsteller, Douglas A. Marzabadi, Mohammad R. Papp, Mariusz Overstreet, David H. Gerald, Christophe P. G. Craig, Douglas A. |
| Description | Country affiliation: United States Author Affiliation: Walker MW ( Lundbeck Research USA, 215 College Road, Paramus, NJ 07652, USA. mmw@lundbeck.com) |
| Abstract | Neuropeptide Y (NPY) regulates physiological processes via receptor subtypes (Y(1), Y(2), Y(4), Y(5), and y(6)). The Y(5) receptor is well known for its role in appetite. Based on expression in the limbic system, we hypothesized that the Y(5) receptor might also modulate stress sensitivity. We identified a novel Y(5) receptor-selective antagonist, Lu AA33810 [N-[[trans-4-[(4,5-dihydro[1]-benzothiepino[5,4-d]thiazol-2-yl)amino]cyclohexyl]methyl]-methanesulfonamide], that bound to cloned rat Y(5) receptors (K(i) = 1.5 nM) and antagonized NPY-evoked cAMP and calcium mobilization in vitro. Lu AA33810 (3-30 mg/kg p.o.) blocked feeding elicited by intracerebroventricular injection of the Y(5) receptor-selective agonist [cPP(1-7),NPY(19-23),Ala(31),Aib(32),Gln(34)]-hPancreatic Polypeptide in Sprague-Dawley rats. In vivo effects of Lu AA33810 were correlated with brain exposure > or = 50 ng/g and ex vivo Y(5) receptor occupancy of 22 to 95%. Lu AA33810 was subsequently evaluated in models of stress sensitivity. In Fischer 344 rats, Lu AA33810 (30 mg/kg p.o.) attenuated increases in plasma ACTH and corticosterone elicited by intracerebroventricular injection of [cPP(1-7),NPY(19-23),Ala(31),Aib(32),Gln(34)]-hPancreatic Polypeptide. In Sprague-Dawley rats subjected to the social interaction test, Lu AA33810 (3-30 mg/kg p.o.) produced anxiolytic-like effects after acute or chronic treatment. In Flinders sensitive line rats, chronic dosing of Lu AA33810 (10 mg/kg/day i.p.) produced anxiolytic-like effects in the social interaction test, plus antidepressant-like effects in the forced swim test. In Wistar rats exposed to chronic mild stress, chronic dosing of Lu AA33810 (3 and 10 mg/kg/day i.p.) produced antidepressant-like activity, i.e., normalization of stress-induced decrease in sucrose consumption. We propose that Y(5) receptors may function as part of an endogenous stress-sensing system to mediate social anxiety and reward or motivational deficits in selected rodent models. |
| File Format | HTM / HTML |
| ISSN | 00223565 |
| Issue Number | 3 |
| Volume Number | 328 |
| e-ISSN | 15210103 |
| Journal | Journal of Pharmacology and Experimental Therapeutics |
| Language | English |
| Publisher | American Society for Pharmacology and Experimental Therapeutics |
| Publisher Date | 2009-03-01 |
| Publisher Place | United States |
| Access Restriction | Subscribed |
| Subject Keyword | Benzothiepins Receptors, Neuropeptide Y Rats, Wistar Rats, Inbred F344 Drug Therapy Models, Molecular Rats Male Antidepressive Agents Discipline Pharmacology Therapeutic Use Antagonists & Inhibitors Journal Article Animals Discipline Therapeutics Sulfonamides Thiazoles Stress, Psychological Anti-anxiety Agents Disease Models, Animal |
| Content Type | Text |
| Resource Type | Article |
| Subject | Molecular Medicine Pharmacology |
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