Výsledky vyhledávání

Synthesis and in vitro characterization of novel amino terminally modified oxotremorine derivatives for brain muscarinic receptors

Autor: D S, Garvey, J T, Wasicak, J Y, Chung, Y K, Shue, G M, Carrera, P D, May, M M, McKinney, D, Anderson, E, Cadman, L, Vella-Rountree

Publikováno v: Journal of Medicinal Chemistry. 35:1550-1557

A series of novel 2-substituted acetylenic pyrrolidines and piperidines related to oxotremorine (1) were prepared and evaluated in vitro as muscarinic cholinergic agents at brain M1 and M2 receptors. One analogue, 3-(2-oxo-1-pyrrolidinyl)-1-[2(R)-pyr

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8fa619542c4ac99cd95a8adbdada490c
https://doi.org/10.1021/jm00087a008

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Design and evaluation of nitrosylated alpha-adrenergic receptor antagonists as potential agents for the treatment of impotence

Autor: I S, de Tejada, D S, Garvey, J D, Schroeder, T, Shelekhin, L G, Letts, A, Fernández, B, Cuevas, S, Gabancho, V, Martínez, J, Angulo, M, Trocha, P, Marek, P, Cuevas, S W, Tam

Publikováno v: The Journal of pharmacology and experimental therapeutics. 290(1)

We designed and evaluated a new class of molecules, nitrosylated alpha-adrenergic receptor antagonists, as potential agents for the treatment of impotence. In in vitro studies with human and rabbit corpus cavernosum strips in organ chambers, the alph

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::b64cc58f2b2c7180b94952791b08a67d
https://pubmed.ncbi.nlm.nih.gov/10381767

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Nitrosylated bovine serum albumin derivatives as pharmacologically active nitric oxide congeners

Autor: J F, Ewing, D V, Young, D R, Janero, D S, Garvey, T A, Grinnell

Publikováno v: The Journal of pharmacology and experimental therapeutics. 283(2)

Although nitrosothiols have been suggested to act as regulators of cell (patho)physiology, little is known about the pharmacology of nitrosylated proteins as nitric oxide (NO.) congeners. We describe the molecular consequences of nitrosylating bovine

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::e7c7b036e36e0e3bd099ad57a8632efe
https://pubmed.ncbi.nlm.nih.gov/9353418

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S-nitrosylated tissue-type plasminogen activator protects against myocardial ischemia/reperfusion injury in cats: role of the endothelium

Autor: J A, Delyani, T O, Nossuli, R, Scalia, G, Thomas, D S, Garvey, A M, Lefer

Publikováno v: The Journal of pharmacology and experimental therapeutics. 279(3)

S-Nitrosylated tissue plasminogen activator (tPA) is formed by S-nitrosylation of the clinically important agent tPA by nitric oxide, thus conferring nitric oxide donor properties to the molecule. Cats were subjected to 90 min of myocardial ischemia

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::5223fb7b945f52339544c8686646ce43
https://pubmed.ncbi.nlm.nih.gov/8968338

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Ligands for brain cholinergic channel receptors: synthesis and in vitro characterization of novel isoxazoles and isothiazoles as bioisosteric replacements for the pyridine ring in nicotine

Autor: D. S. Garvey, James T. Wasicak, Suzanne A. Lebold, David J. Anderson, Nan-Horng Lin, Ann-Marie Hettinger, George M. Carrera, Yun He, Elliott Richard L, Mark W. Holladay

Publikováno v: Journal of medicinal chemistry. 37(26)

Ligands which activate neuronal nicotinic acetylcholine receptors (nAChRs) represent a potential approach for the palliative treatment for the symptoms of memory loss associated with Alzheimer's disease (AD). Based upon this approach, a series of nov

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::93772902c32435ded14a40b0c266da41
https://pubmed.ncbi.nlm.nih.gov/7799396

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The in vitro hepatic metabolism of ABT-418, a cholinergic channel activator, in rats, dogs, cynomolgus monkeys, and humans

Autor: A D, Rodrigues, J L, Ferrero, M T, Amann, G A, Rotert, S P, Cepa, B W, Surber, J M, Machinist, N R, Tich, J P, Sullivan, D S, Garvey

Publikováno v: Drug metabolism and disposition: the biological fate of chemicals. 22(5)

The metabolism of the cholinergic channel activator [3H]ABT-418 was studied in 9,000g supernatant (S-9) fractions and precision-cut tissue slices prepared from rat, dog, monkey, and human livers. In rat S-9 fractions and tissue slices, the lactam and

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::38c4cff4228f63c5dce6d357613143e6
https://pubmed.ncbi.nlm.nih.gov/7530622

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(S)-3-methyl-5-(1-methyl-2-pyrrolidinyl) isoxazole (ABT 418): a novel cholinergic ligand with cognition-enhancing and anxiolytic activities: I. In vitro characterization

Autor: S P, Arneric, J P, Sullivan, C A, Briggs, D, Donnelly-Roberts, D J, Anderson, J L, Raszkiewicz, M L, Hughes, E D, Cadman, P, Adams, D S, Garvey

Publikováno v: The Journal of pharmacology and experimental therapeutics. 270(1)

A diversity of nicotinic acetylcholine receptor (nAChR) subtypes has been identified in mammalian brain using recombinant DNA technology. Alterations in the activity of these acetylcholinegated ion channels have been implicated in a number of central

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::ca775e422e9ac407b509a3044fab7889
https://pubmed.ncbi.nlm.nih.gov/7518514

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