Zobrazeno 1 - 10
of 83
pro vyhledávání: '"Stafford, McLean"'
Autor:
Michelle Vanase-Frawley, Diane Stephenson, Patrick Robert Verhoest, Mihály Hajós, Geralyn P. Kocan, William E. Hoffmann, Kari R. Fonseca, Douglas S. Chapin, Christopher J. Schmidt, Fredrick R. Nelson, Curt Christoffersen, Frank S. Menniti, Jody Freeman, Stafford McLean, Victor Guanowsky, Kieran F. Geoghegan, Mark J. Majchrzak, Christopher John Helal, Patricia A. Seymour, John F. Harms, Sarah Grimwood, Francis David Tingley, Robin J. Kleiman, Robin Roof, Anne W. Schmidt, Dina McGinnis
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 341:396-409
Cyclic nucleotides are critical regulators of synaptic plasticity and participate in requisite signaling cascades implicated across multiple neurotransmitter systems. Phosphodiesterase 9A (PDE9A) is a high-affinity, cGMP-specific enzyme widely expres
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e434253f25e37a0d7e9a05a69e8cdd81
https://doi.org/10.1124/jpet.111.191353
https://doi.org/10.1124/jpet.111.191353
Autor:
David E. Johnson, Rouba Kozak, Mark J. Majchrzak, Mihály Hajós, Kathryn E. Williams, William E. Hoffmann, Hans Rollema, Patricia A. Seymour, Doug S. Chapin, Stafford McLean, Victor Guanowsky, Weldon Horner, Jody Freeman
Publikováno v:
Biochemical Pharmacology. 78:813-824
The pharmacological properties and pharmacokinetic profile of the alpha4beta2 nicotinic acetylcholine receptor (nAChR) partial agonist varenicline provide an advantageous combination of free brain levels and functional potencies at the target recepto
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bc35e34c456e3d48f7c746cdd4c74149
https://doi.org/10.1016/j.bcp.2009.05.033
https://doi.org/10.1016/j.bcp.2009.05.033
Autor:
Dianne K. Bryce, Martin Patrick Allen, Spiros Liras, Stafford McLean, Mary E. Haggan, Barb E. Segelstein, James F. Blake
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 10:523-526
3-Amino-3-phenylpropionamide derivatives were produced as small molecule mimics of the cyclic octapeptide octreotide from readily available imine 1 Download : Download high-res image (51KB) Download : Download full-size image Scheme 1 . Preparation o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7b6523a05d5873681cffe2d88ffb6ff8
https://doi.org/10.1016/s0960-894x(00)00034-2
https://doi.org/10.1016/s0960-894x(00)00034-2
Autor:
Masami Nakane, Rosen T, Rosemary T. Crawford, Megumi Tsuchiya, Dianne K. Bryce, Stafford McLean, Yoshiko Gohda, Atsushi Nagahisa, Karen J. Coffman, John A. Lowe
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 8:281-284
The synthesis and SAR of benzylamine side chain analogs of the NK-1 receptor antagonist CP-99,994 are described. The 5-trifluoromethoxy analog, CP-122,721, shows superior in vivo blockade of NK-1 receptor mediated responses.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ae9ffaa651f461a8e49413beebc519d1
https://doi.org/10.1016/s0960-894x(98)00012-2
https://doi.org/10.1016/s0960-894x(98)00012-2
Publikováno v:
British Journal of Pharmacology. 120:116-120
The NK1 receptor antagonist CP-99994 has been shown to prevent vomiting elicited by both peripherally and centrally acting emetogens in ferrets and dogs. These results have now been extended to another stimulus, provocative motion, and another specie
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::3d5d1346d2295d811d15498c6e16facb
https://doi.org/10.1038/sj.bjp.0700888
https://doi.org/10.1038/sj.bjp.0700888
Autor:
John A. Lowe III, Stafford McLean
Publikováno v:
Current Pharmaceutical Design. 1:269-278
The discovery of nonpeptide antagonists of the tachykinin peptides substance P, neurokinin A, and neurokinin B has greatly accelerated pharmacological characterization of the role of these peptides and their receptors (NK-1, NK-2, and NK-3) in the ce
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::0f2611bd61a9f752f570c500dfdc7f61
https://doi.org/10.2174/1381612801666220918144023
https://doi.org/10.2174/1381612801666220918144023
Autor:
Stafford McLean, Rosemary T. Crawford, John A. Lowe, Appleton Troy A, Jean Morrone, Franco Lombardo, Dianne K. Bryce, Stevin H. Zorn, Susan E. Drozda
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 5:1933-1936
A series of 5-substituted-3-ureidobenzazepin-2-ones bearing ioizable functionality was synthesized as potential cholecystokinin-B (CCK-B) receptor antagonists. SAR of this series of compounds demonstrated the optimal combination of a carboxylic acid
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::10eb65fc8de4fa6753c0176ba4b0fedc
https://doi.org/10.1016/0960-894x(95)00327-p
https://doi.org/10.1016/0960-894x(95)00327-p
Autor:
A. A. Fossa, S. Obach, Paul L.R. Andrews, T. Seeger, S. F. Gonsalves, Stafford McLean, J. W. Watson
Publikováno v:
British Journal of Pharmacology. 115:84-94
1. The selective NK1 receptor antagonist, CP-99,994, produced dose-related (0.1-1.0 mg kg-1, s.c.) inhibition of vomiting and retching in ferrets challenged with central (loperamide and apomorphine), peripheral (CuSO4) and mixed central and periphera
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7536e5dd438499513766c28c28badced
https://doi.org/10.1111/j.1476-5381.1995.tb16324.x
https://doi.org/10.1111/j.1476-5381.1995.tb16324.x
Autor:
Howard Harry R, Stafford McLean, Karen C. Coffman, Kevin D. Shenk, Dianne K. Bryce, Rosemary T. Crawford
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 5:111-114
Reaction of CP-99,994 (1) with benzyl chloromethyl ether under basic conditions produced the novel 1,6-diazabicyclo[3.2.1]octane system in good yield; analogs containing this nucleus display high binding affinity for substance P receptors. The ethyle
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::a843df8646155f210816e2d29c81922a
https://doi.org/10.1016/0960-894x(94)00467-t
https://doi.org/10.1016/0960-894x(94)00467-t
Autor:
Dianne K. Bryce, Rosemary T. Crawford, Weimin Qian, Jon Bordner, Stafford McLean, John A. Lowe, Pamela J. Scott
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 4:2877-2882
A series of 5,7-diphenyl-3-ureidohexahydroazepin-2-one cholecystokinin-B (CCK-B) receptor antagonists was synthesized using Beckmann ring expansion of a suitable 2,4-diphenylcyclohexanone as a key step. SAR studies revealed the importance of the 5-ar
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::2e890efb517da144e8781974e09ddc11
https://doi.org/10.1016/s0960-894x(01)80832-5
https://doi.org/10.1016/s0960-894x(01)80832-5