Radiosynthesis and in Vivo Evaluation of Neuropeptide Y5 Receptor (NPY5R) PET Tracers

Autor: Gamini Chandrasena, J. John Mann, Jaya Prabhakaran, Mathivanan Packiarajan, Vrej Jubian, J. S. Dileep Kumar, Mali Pratap, Ramin V. Parsey, Mary W. Walker

Publikováno v: ACS chemical neuroscience. 7(5)

Neuropeptide Y receptor type 5 (NPY5R) is a G-protein coupled receptor (GPCR) that belongs to the subfamily of neuropeptide receptors (NPYR) that mediate the action of endogenous neuropeptide Y (NPY). Animal models and preclinical studies indicate a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5450a282121e7e2c6ba51dcc88d3df94
https://pubmed.ncbi.nlm.nih.gov/26886507

Metal templated receptors for the effective complexation of dicarboxylates

Autor: M. Scott Goodman, Andrew D. Hamilton, Vrej Jubian

Publikováno v: Tetrahedron Letters. 36:2551-2554

In this paper we show that a thiourea-functionalized terpyridine unit can be induced to form, in the presence of ruthenium (II), a well-ordered recognition site for dicarboxylate ions. Strong binding to the self-assembled receptor can be followed by

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::eb20a3794b9ca14a3d92df36f9c7678b
https://doi.org/10.1016/0040-4039(95)00337-c

5-(2'-Pyridyl)-2-aminothiazoles: alkyl amino sulfonamides and sulfamides as potent NPY(5) antagonists

Autor: Mathivanan Packiarajan, Hermogenes N. Jimenez, Mary W. Walker, Mohammad R. Marzabadi, Kim Andersen, Mahesh N. Desai, Toni C. Wolinski, Emily Reinhard, Vrej Jubian, Heather Coate, Gamini Chandrasena

Publikováno v: Bioorganicmedicinal chemistry letters. 21(21)

Synthesis, SAR and physico-chemical properties of an alkyl aminothiazole series 8 and 16 are described. 2-Pyridylaminothiazole based compounds such as 8c and 16a exhibit high affinity at the NPY(5) receptor with desirable cLogPs and solubilities. How

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::44107b81e368d97fb0a7f5bb5877e548
https://pubmed.ncbi.nlm.nih.gov/21924902

Discovery of Lu AA33810: a highly selective and potent NPY5 antagonist with in vivo efficacy in a model of mood disorder

Autor: Ove Wiborg, Mathivanan Packiarajan, Mohammad R. Marzabadi, Toni D. Wolinsky, Yalei Lu, Gamini Chandrasena, Hualing Zhong, Kim Andersen, Mary W. Walker, Wai C. Wong, Mahesh N. Desai, Vrej Jubian, Stewart A. Noble

Publikováno v: Packiarajan, M, Marzabadi, M R, Desai, M, Lu, Y, Noble, S A, Wong, W C, Jubian, V, Chandrasena, G, Wolinsky, T D, Zhong, H, Walker, M W, Wiborg, O & Andersen, K 2011, ' Discovery of Lu AA33810 : a highly selective and potent NPY5 antagonist with in vivo efficacy in a model of mood disorder ', Bioorganic & Medicinal Chemistry Letters, vol. 21, no. 18, pp. 5436-41 . https://doi.org/10.1016/j.bmcl.2011.06.124

The structure–activity relationship of a series of tricyclic-sulfonamide compounds 11 – 32 culminating in the discovery of N -[ trans -4-(4,5-dihydro-3,6-dithia-1-aza-benzo[e]azulen-2-ylamino)-cyclohexylmethyl]-methanesulfonamide ( 15 , Lu AA3381

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b7a28a777dee111d70ad35e0c6aa6572
https://pubmed.ncbi.nlm.nih.gov/21782428

The novel neuropeptide Y Y5 receptor antagonist Lu AA33810 [N-[[trans-4-[(4,5-dihydro[1]benzothiepino[5,4-d]thiazol-2-yl)amino]cyclohexyl]methyl]-methanesulfonamide] exerts anxiolytic- and antidepressant-like effects in rat models of stress sensitivity

Autor: Mary W, Walker, Toni D, Wolinsky, Vrej, Jubian, Gamini, Chandrasena, Huailing, Zhong, Xinyan, Huang, Silke, Miller, Laxminarayan G, Hegde, Douglas A, Marsteller, Mohammad R, Marzabadi, Mariusz, Papp, David H, Overstreet, Christophe P G, Gerald, Douglas A, Craig

Publikováno v: The Journal of pharmacology and experimental therapeutics. 328(3)

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) recepto

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::bfa69ad7a4e42927a9fa0893ce2c8929
https://pubmed.ncbi.nlm.nih.gov/19098165