Výsledky vyhledávání - "John M. Wetzel"

Synthesis and SAR Investigations for Novel Melanin-Concentrating Hormone 1 Receptor (MCH1) Antagonists Part 1. The Discovery of Arylacetamides as Viable Replacements for the Dihydropyrimidinone Moiety of an HTS Hit

Autor: Irena Daniewska, John De Leon, Carlos Forray, Kim Andersen, Douglas A. Craig, Laxminarayan G. Hegde, Toni D. Wolinsky, Jiang Yu, Mohammad R. Marzabadi, Ron Kong, Kai Lu, Chen Chien-An, Boshan Li, John M. Wetzel

Publikováno v: Journal of Medicinal Chemistry. 50:3870-3882

Melanin-concentrating hormone (MCH) is involved in the regulation of feeding, water balance, energy metabolism, general arousal and attention state, memory, cognitive functions, and psychiatric disorders. Herein, two new chemical series exemplified b

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3204d0c9c648d9eec3964449da2f9d19
https://doi.org/10.1021/jm060381c

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Identification and Characterization of Two G Protein-coupled Receptors for Neuropeptide FF

Publikováno v: Journal of Biological Chemistry. 275:39324-39331

The central nervous system octapeptide, neuropeptide FF (NPFF), is believed to play a role in pain modulation and opiate tolerance. Two G protein-coupled receptors, NPFF1 and NPFF2, were isolated from human and rat central nervous system tissues. NPF

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bb5a488ab332b9fe290d764d964bd5d1
https://doi.org/10.1074/jbc.m004385200

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Design and Synthesis of Novel α1a Adrenoceptor-Selective Antagonists. 4. Structure−Activity Relationship in the Dihydropyrimidine Series

Publikováno v: Journal of Medicinal Chemistry. 42:4804-4813

We have previously disclosed dihydropyridines such as 1a,b as selective alpha(1a) antagonists as a potential treatment for benign prostatic hyperplasia (BPH). The propensity of dihydropyridines toward an oxidation led us to find suitable replacements

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::644bb1e845f3476e1d3846442d956b07
https://doi.org/10.1021/jm9902032

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Design and Synthesis of Novel α1a Adrenoceptor-Selective Dihydropyridine Antagonists for the Treatment of Benign Prostatic Hyperplasia

Autor: Dhanapalan Nagarathnam, Terry W. Schorn, Wai C. Wong, John M. Wetzel, Carlos Forray, Raymond S.L. Chang, William E. Heydorn, George Chiu, Theodore P. Broten, C. Gluchowski, Xingfang Hong, T. A. Branchek, Shou Wu Miao, James Fang, Mohammad R. Marzabadi

Publikováno v: Journal of Medicinal Chemistry. 41:5320-5333

We report the synthesis and evaluation of novel alpha1a adrenoceptor subtype-selective antagonists. Systematic modification of the lipophilic 4,4-diphenylpiperidinyl moiety of the dihydropyridine derivatives 1 and 2 provided several highly selective

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2107805a48424aca74e2ba8260056335
https://doi.org/10.1021/jm980506g

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Identification of a Dihydropyridine as a Potent α1a Adrenoceptor-Selective Antagonist That Inhibits Phenylephrine-Induced Contraction of the Human Prostate

Autor: Charles Gluchowski, Dhanapalan Nagarathnam, Wai C. Wong, Carlos Forray, Pierre J.-J. Vaysse, Xingfang Hong, Rui Tang, Shou Wu Miao, Mohammad R. Marzabadi, John M. Wetzel, Theresa Branchek, Herbert Lepor, George Chiu, James Fang, Diana Wang

Publikováno v: Journal of Medicinal Chemistry. 41:2643-2650

A number of novel dihydropyridine derivatives based upon 1, 4-dihydro-3-(methoxycarbonyl)-2, 6-dimethyl-4-(4-nitrophenyl)-5-((3-(4, 4-diphenylpiperidin-1-yl)propyl)aminocarbonyl)pyridine (4) have been synthesized and tested at cloned human alpha adre

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6bad3dcef4af073bcdde4b1db5b07bfb
https://doi.org/10.1021/jm980077m

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Characterization of specific binding of L-762,459, a selective α1A-adrenoceptor radioligand to rat and human tissues

Autor: Dhanapalan Nagarathnam, Stacey O'Malley, Tsing B Chen, Charles Gluchowski, H. Donald Burns, Raymond E. Gibson, John M. Wetzel, Jerry DiSalvo, Raymond S.L. Chang, Barbara Francis, Mohammad R. Marzabadi, Marvin L. Bayne

Publikováno v: European Journal of Pharmacology. 348:287-295

L-762,459 ((±)1-(3-{[5-carbamoyl-2-{2-[(4-hydroxy-3-iodobenzimidoyl)-amino]-ethoxy-methyl}-6-methyl-4-(4-nitrophenyl)-1,4-dihydropyridine-3-carbonyl]-amino}-propyl)-4-phenyl-1-piperidine-4-carboxylic acid methyl ester), an analog of a series of dihy

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::eaf5e7de7f2ac6ae529120605aaa7655
https://doi.org/10.1016/s0014-2999(98)00149-6

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Localization of mRNA and Receptor Binding Sites for the alpha sub 1a-Adrenoceptor Subtype in the Rat, Monkey and Human Urinary Bladder and Prostate

Autor: Eric L. Gustafson, Charles Gluchowski, John M. Wetzel, Herbert Lepor, Paul D. Walden, Margaret M. Durkin

Publikováno v: Journal of Urology. 157:1032-1038

Purpose: To localize the mRNAs and receptor binding sites for the alpha sub 1a/A, alpha1b/B and alpha1d/D-adrenoceptor (AR) subtypes in the rat, monkey and human urinary bladder and prostate.Materials and Methods: alpha1-AR mRNAs were localized on sl

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5ab2e630841a3c56097179d59424fb1c
https://doi.org/10.1016/s0022-5347(01)65136-x

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Comparison of the electronic effect and the steric influence between the 1,1,2,2,2-pentamethyldisilanyl and the trimethylsilyl groups

Autor: John Lee, Jih Ru Hwu, Ray J. Butcher, John M. Wetzel

Publikováno v: Journal of Organometallic Chemistry. 453:21-28

A comparison of the electronic effects expressed by the Me 3 SiMe 2 Si-; and Me 3 Si- groups towards carbocationic intermediates was made by study of acid-catalyzed rearrangements of decalin epoxides 3 and 4 . Reaction of the Me 3 SiMe 2 Si-epoxide 3

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::d32aee5d07416bc83792ad28bb61a22b
https://doi.org/10.1016/0022-328x(93)80322-3

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