Zobrazeno 1 - 10
of 22
pro vyhledávání: '"Graham P. Jackman"'
Autor:
William J Louis, Simon N S Louis, Graham P Jackman, Linda A Rezmann-Vitti, Curtis A. Machida, Brian J Duke, Tracy L. Nero
Publikováno v:
Journal of Medicinal Chemistry. 49:3467-3477
Site-directed mutagenesis and photoaffinity labeling experiments suggest the existence of at least two distinct binding orientations for aryloxypropanolamine competitive antagonists in the beta-adrenergic receptor (beta-AR), one where the aryloxy moi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::da3ece1df11b9c0faa0b22edb0caba29
https://doi.org/10.1021/jm050624l
https://doi.org/10.1021/jm050624l
Autor:
William J. Louis, Linda A Rezmann-Vitti, Tracy L. Nero, Dimitri Iakovidis, Simon N S Louis, Graham P. Jackman, Curtis A. Machida
Publikováno v:
Biochemical Pharmacology. 68:675-688
We investigated the role of Trp(134(3.28)), Ser(190(4.57)) and Tyr(356(7.43)) in agonist binding to, and activation of, the rat beta(1)-adrenergic receptor by comparing pK(i)s and functional responses of W134A, S190A and Y356F mutant receptors to wil
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::66f364284f1174e13d7b5f7573045357
https://doi.org/10.1016/j.bcp.2004.04.021
https://doi.org/10.1016/j.bcp.2004.04.021
Autor:
Simon N S Louis, William J. Louis, Linda A Rezmann-Vitti, Dimitri Iakovidis, Tracy L. Nero, Graham P. Jackman
Publikováno v:
European Journal of Medicinal Chemistry. 37:111-125
A series of 36 phenoxypropanolamines was examined to determine the structure--activity relationships of beta-adrenoceptor (beta-AR) antagonists for the human beta(1)-AR. The binding affinities of all the compounds were determined for human beta(1)-AR
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a575a4b10b20a60fd2eea9bbe38464f9
https://doi.org/10.1016/s0223-5234(01)01315-0
https://doi.org/10.1016/s0223-5234(01)01315-0
Publikováno v:
Cardiovascular Drugs and Therapy. 14:565-577
In vitro lipolysis stimulated by low (-)-isoprenaline concentrations (< or =30 nM) in epididymal white adipocytes from Sprague-Dawley rats was inhibited at least 60-80% by the specific beta1-antagonists LK 204-545 and CGP 20712A (1 microM), suggestin
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::7ff01723da2e3f7e04b2278305fb993d
https://doi.org/10.1023/a:1007838125152
https://doi.org/10.1023/a:1007838125152
Autor:
Felicia M. Colagrande, Graham P. Jackman, Tracy L. Nero, Simon N S Louis, William J Louis, Dimitri Iakovidis
Publikováno v:
European Journal of Medicinal Chemistry. 34:919-937
To further explore the structure-activity relationships of beta-adrenoceptor (beta-AR) antagonists, a series of 25 para-substituted N-isopropylphenoxy-propanolamines were synthesised, nine of which are new compounds. All have been examined for their
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5d5f676dccc0435c8fea8a47e478535f
https://doi.org/10.1016/s0223-5234(99)00114-2
https://doi.org/10.1016/s0223-5234(99)00114-2
Autor:
Felicia M. Colagrande, Graham P. Jackman, Linda Adriana Rezmann, William J Louis, Dimitri Iakovidis, Simon N S Louis, Tracy L. Nero
Publikováno v:
European Journal of Medicinal Chemistry. 34:539-548
The synthesis of (±)-1-(3',4'-dihydroxyphenoxy)-3-(3",4"-dimethoxyphenyl)ethylamino-2-propanol hydrochloride, (±)-RO363.HCl, and the ( 2S )-(-)-isomer is described for the first time. The binding affinities for (±)-RO363.HCl, ( 2S )-(-)-RO363.HCl
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::a08caa5a1dabc99efbfc531cbf4deec2
https://doi.org/10.1016/s0223-5234(99)80103-2
https://doi.org/10.1016/s0223-5234(99)80103-2
Publikováno v:
European Journal of Pharmacology. 367:431-435
LK 204-545 ((+/-)-1-(2-(3-(2-cyano-4-(2-cyclopropyl-methoxy-ethoxy)phenoxy)-2-hydro xy-propyl-amino)-ethyl)-3-(4-hydrxy-phenyl) urea), an antagonist that possesses high beta1-/beta2-selectivity in the rat, and a range of cardio-selective and non-sele
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dcd7bef335d169866717fba3ec851d81
https://doi.org/10.1016/s0014-2999(99)00019-9
https://doi.org/10.1016/s0014-2999(99)00019-9
Publikováno v:
Journal of the Autonomic Nervous System. 72:129-136
We have previously reported that in rat brain membranes, [ 3 H ]rilmenidine, in addition to labelling α2-adrenoceptors and the I2B-subtype of imidazoline receptor binding site (I2B-RBS), may label an additional I-RBS population, distinct from previo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::296098ddbac79f379fae52a195b5fc10
https://doi.org/10.1016/s0165-1838(98)00097-6
https://doi.org/10.1016/s0165-1838(98)00097-6
Autor:
Andrew L. Gundlach, Satoshi Suzuki, Paul R. King, William J. Louis, AR Hosseini, Dimitri Iakovidis, Tracy L. Nero, Graham P. Jackman
Publikováno v:
Journal of the Autonomic Nervous System. 72:118-128
The distribution and relative densities of imidazoline-receptor binding sites (I-RBS) and monoamine oxidase (MAO)-A and -B enzyme(s) in rat and rabbit kidney were compared autoradiographically using fixed nanomolar concentrations of [3H]rilmenidine a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::c900bf9e521bebf50fe087d9017231f5
https://doi.org/10.1016/s0165-1838(98)00096-4
https://doi.org/10.1016/s0165-1838(98)00096-4
Autor:
Simon N S Louis, Linda Adriana Rezmann, Tracy L. Nero, Dimitri Iakovidis, William J Louis, Graham P. Jackman, Felicia M. Colagrande
Publikováno v:
ChemInform. 30
The synthesis of (±)-1-(3',4'-dihydroxyphenoxy)-3-(3",4"-dimethoxyphenyl)ethylamino-2-propanol hydrochloride, (±)-RO363.HCl, and the ( 2S )-(-)-isomer is described for the first time. The binding affinities for (±)-RO363.HCl, ( 2S )-(-)-RO363.HCl
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::fe938d4ecdf27c42905dcc2d6136abc6
https://doi.org/10.1002/chin.199948099
https://doi.org/10.1002/chin.199948099