Výsledky vyhledávání - "James C. Blosser"

Development of a pharmacological target profile for muscarinic agonists

Autor: Sally A. McCreedy, Kris E. Kucera, David J. Triggle, Matthew Marler, Roberta Mihut, E. S. C. Wu, Jack Gordon, Mary L. Stagnitto, Dan Widzowski, Andrew Howell, Anthony C. Machulskis, John Zongrone, Paul Bialobok, George B. Mullen, Marilyn K. Knowles, Shawn Sitar, James C. Blosser

Publikováno v: Drug Development Research. 40:117-132

The purpose of these studies was to determine the levels of intrinsic activity in vitro at muscarinic receptor pharmacological subtypes (M1, M2, and M3) that would optimize cognitive activity while minimizing acute adverse cholinergic effects in vivo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::7e8998ab434e05f533027b5fd6d29250
https://doi.org/10.1002/(sici)1098-2299(199702)40:2<117::aid-ddr3>3.0.co

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Acylhydrazones as M1/M3 selective muscarinic agonists

Autor: Alexander Rochester New York Us Kover, James T. Loch, L.Paul Rosenberg, Simon F. Semus, John Zongrone, Anthony C. Machulskis, James C. Blosser, John C. Gordon, Patrick R. Verhoest, Sally A. McCreedy, Edwin S. C. Wu

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 6:2525-2530

To improve receptor binding affinity and to investigate functional selectivity of 2,8-dimethyl-1-oxa-8-azaspiro[4.5]decan-3-one acetylhydrazone 2 at muscarinic receptor subtypes, a series of acylhydrazones A was synthesized. The SAR indicates that th

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::eb889704e941189ecb0b2cf85e52420e
https://doi.org/10.1016/0960-894x(96)00471-4

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Synthesis and biological activity of enantiomers of a conformationally restricted muscarone analog

Autor: Alex Kover, Robert J. Murray, James C. Blosser, R. A. Mack, George B. Mullen, Sally A. McCreedy, James T. Loch, Anthony C. Machulskis, E. S. C. Wu, John C. Gordon

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 5:1813-1818

A short and efficient synthesis of both enantiomers of 2,8-dimethyl-1-oxa-8-azaspiro[4.5]-decan-3-one is described. The biological activity of the racemate resides predominantly in the S-enantiomer. While the S-isomer is a full M2-agonist, the R-isom

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::c50a6e4b6d92b777f5974a05bc64291a
https://doi.org/10.1016/0960-894x(95)00301-9

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Preclinical profile of the anticonvulsant remacemide and its enantiomers in the rat

Autor: Louis R. Freedman, H. Steve White, Ranjit Ray, James C. Blosser, Sally A. McCreedy, Gene C. Palmer, George E. Garske, Ronald C. Griffith, Jose H. Woodhead, Eric W. Harris, Ewart A. Swinyard, Napier James J

Publikováno v: Epilepsy Research. 9:161-174

Studies conducted by Fisons Pharmaceuticals and the Antiepileptic Drug Development Program (ADD Program) of the Epilepsy Branch (NINDS, NIH) revealed that ‘remacemide’ (FPL 12924, formerly PR 934-423) was effective orally in the prevention of max

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c0bd859779c3b7061ffa97256599c495
https://doi.org/10.1016/0920-1211(91)90050-p

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In vitro muscarinic activity of spiromuscarones and related analogs

Autor: Ronald C. Griffith, Robert J. Murray, George B. Mullen, Anthony C. Machulskis, Sally A. McCreedy, James C. Blosser, Edwin S. C. Wu, James T. Loch, Alex Kover

Publikováno v: Journal of medicinal chemistry. 38(9)

The cholinergic hypothesis of Alzheimer's disease suggests that cholinergic agonists may have therapeutic potential for treating the attendant memory deficits of the disease. As part of a program aimed at preparing metabolically stable, nonquaternary

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::35650bf7e78dda40b75d090a1d855055
https://pubmed.ncbi.nlm.nih.gov/7739014

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Flavones. 2. Synthesis and structure-activity relationship of flavodilol and its analogs. A novel class of antihypertensive agents with catecholamine depleting properties

Autor: M. A. Dailey, T. L. Thomas, T. A. Davidson, T. E. Cole, A. R. Borrelli, M. Fedorchuk, E. S. C. Wu, James C. Blosser, K. G. Doring, J T Loch rd

Publikováno v: Journal of Medicinal Chemistry. 32:183-192

(3-Phenyl-7-flavonoxy)propanolamines have been shown to exhibit antihypertensive activity in spontaneously hypertensive rats. Although they are structurally similar to classical beta-adrenergic blocking compounds, their activity is not due to inhibit

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8c3a1d7538e1fe887a0eae23677babd8
https://doi.org/10.1021/jm00121a034

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Inhibitors of membrane depolarization regulate acetylcholine receptor synthesis by a calcium-dependent, cyclic nucleotide-independent mechanism

Autor: Stanley H. Appel, James C. Blosser, James L. McManaman

Publikováno v: Biochimica et Biophysica Acta (BBA) - Molecular Cell Research. 720:28-35

The inhibition of membrane depolarization by tetrodotoxin or the local anesthetic benzocaine elevates the acetylcholine receptor levels in cultured myotubes. The elevated acetylcholine receptor levels are due to increased receptor synthesis rather th

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dc8b3894a5d5918a104a2eb2647cb39a
https://doi.org/10.1016/0167-4889(82)90035-0

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