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Featured researches published by Michael K James.


Expert Opinion on Investigational Drugs | 1994

Section Review: Central & Peripheral Nervous System: Remifentanil and anaesthesia for the future

Michael K James

Current trends toward outpatient surgery have created a demand for shorter acting anaesthetic agents. Such agents not only provide the anaesthetist with rapid patient recovery after completion of the procedure, but also with almost immediate intra-operative control over the anaesthetic state of the patient. Shorter acting anaesthetic agents are being developed in several therapeutic areas: volatile anaesthetics, neuromuscular blockers and injectable anaesthetics. Desflurane (Anaquest) and sevoflurane (Maruishi) are short acting volatile anaesthetics under development. Short acting neuromuscular blockers currently under clinical investigation, or recently introduced, include mivacurium (Wellcome) and rocuronium (Organon/Akzo). In the injectable anaesthetic area, propofol (Zeneca) has been introduced and offers some significant advantages over the previously existing induction agents, such as thiopental and methohexital. Several 4-anilidopiperdine opioid analgesics/anaesthetics are also being investigated. ...


Bioorganic & Medicinal Chemistry Letters | 2001

1,4-Benzodiazepine peripheral cholecystokinin (CCK-A) receptor agonists.

Ronald G. Sherrill; Judd Berman; Lawrence Birkemo; Dallas K. Croom; Milana Dezube; Gregory N. Ervin; Mary K. Grizzle; Michael K James; Michael F. Johnson; Kennedy L. Queen; Thomas Rimele; Frank Vanmiddlesworth; Elizabeth Ellen Sugg

A series of 1,4-benzodiazepines, N-1-substituted with an N-isopropyl-N-phenylacetamide moiety, was synthesized and screened for CCK-A agonist activity. In vitro agonist activity on isolated guinea pig gallbladder along with in vivo induction of satiety following intraperitoneal administration in a rat feeding assay was demonstrated.


Journal of Medicinal Chemistry | 1991

Design, synthesis, and pharmacological evaluation of ultrashort- to long-acting opioid analgetics

Paul L. Feldman; Michael K James; M F Brackeen; J M Bilotta; Schuster Sv; Lahey Ap; Michael W. Lutz; Johnson Mr; Leighton Hj


Journal of Pharmacology and Experimental Therapeutics | 1991

Opioid receptor activity of GI 87084B, a novel ultra-short acting analgesic, in isolated tissues.

Michael K James; Paul L. Feldman; S V Schuster; J M Bilotta; M F Brackeen; H J Leighton


Journal of Medicinal Chemistry | 1996

Discovery of 1,5-Benzodiazepines with Peripheral Cholecystokinin (CCK-A) Receptor Agonist Activity. 1. Optimization of the Agonist "Trigger"

Christopher Joseph Aquino; Duncan R. Armour; Judd Berman; Larry S. Birkemo; Robin Arthur Ellis Carr; Dallas K. Croom; Milana Dezube; Robert W. Dougherty; Gregory N. Ervin; Mary K. Grizzle; Julie E. Head; Gavin Charles Hirst; Michael K James; Michael F. Johnson; Laurence J. Miller; Kennedy L. Queen; Thomas J. Rimele; David N. Smith; Elizabeth E. Sugg


Journal of Pharmacology and Experimental Therapeutics | 1992

Hemodynamic effects of GI 87084B, an ultra-short acting mu-opioid analgesic, in anesthetized dogs.

Michael K James; A Vuong; M K Grizzle; S V Schuster; J E Shaffer


Archive | 1990

N-phenyl-N-(4-piperidinyl)amides useful as analgesics

Paul L. Feldman; Michael K James; Marcus F. Brackeen; Michael Ross Johnson; Harry Jefferson Leighton


Journal of Pharmacology and Experimental Therapeutics | 1989

A new method for estimation of agonist dissociation constants (KA): directly fitting the postinactivation concentration-response curve to a nested hyperbolic equation.

Michael K James; P H Morgan; H J Leighton


Journal of Pharmacology and Experimental Therapeutics | 1994

A pharmacodynamic model to investigate the structure-activity profile of a series of novel opioid analgesics.

Michael W. Lutz; Paul H. Morgan; Michael K James; Paul L. Feldman; M F Brackeen; Lahey Ap; S V James; J M Bilotta; J C Pressley


Journal of Medicinal Chemistry | 1995

Modification of receptor selectivity and functional activity in cholecystokinin peptoid ligands.

Milana Dezube; Elizabeth E. Sugg; Larry S. Birkemo; Dallas K. Croom; Robert W. Dougherty; Gregory N. Ervin; Mary K. Grizzle; Michael K James; Michael F. Johnson

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Gregory N. Ervin

University of North Carolina at Chapel Hill

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Judd Berman

Research Triangle Park

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