Michael P. Neeper

Discovery and optimization of a novel series of pyrazolyltetrahydropyran N-type calcium channel (Cav 2.2) blockers for the treatment of pain

Mark John Wall, Nalin L. Subasinghe, Michael P. Winters, Mary Lou Lubin et autres

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Discovery and SAR of a novel series of 2,4,5,6-tetrahydrocyclopenta[c]pyrazoles as N-type calcium channel inhibitors

Michael P. Winters, Nalin L. Subasinghe, Mark John Wall, Edward J. Beck et autres

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Discovery and SAR of novel tetrahydropyrrolo[3,4-c]pyrazoles as inhibitors of the N-type calcium channel

Michael P. Winters, Nalin L. Subasinghe, Mark John Wall, Edward J. Beck et autres

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A novel series of pyrazolylpiperidine N-type calcium channel blockers

Nalin L. Subasinghe, Mark John Wall, Michael P. Winters, Na Qin et autres

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The design and synthesis of novel, phosphonate-containing transient receptor potential melastatin 8 (TRPM8) antagonists

Jay M. Matthews, Na Qin, Raymond W. Colburn, Scott L. Dax et autres

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An Integrated Multiassay Approach to the Discovery of Small-Molecule N-Type Voltage-Gated Calcium Channel Antagonists

Michael Finley, Mary Lou Lubin, Michael P. Neeper, Edward J. Beck et autres

Abstract The N-type voltage-gated calcium channel (Cav2.2) has been intensively explored as a target for novel, small-molecule analgesic drugs because of its distribution in the pain pathway and its role in nociceptive processing. For example, Cav2.2 is localized at presynaptic terminals of …

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4-Amino-6-arylamino-pyrimidine-5-carbaldehyde hydrazones as potent ErbB-2/EGFR dual kinase inhibitors

Guozhang Xu, Marta C. Abad, Peter J. Connolly, Michael P. Neeper et autres

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TRPV2 Is Activated by Cannabidiol and Mediates CGRP Release in Cultured Rat Dorsal Root Ganglion Neurons

Na Qin, Michael P. Neeper, Yi Liu, Tasha L. Hutchinson et autres

Transient receptor potential V2 (TRPV2) has been proposed to be a high-threshold thermosensor. However, further elucidation of the channel properties and physiological role of TRPV2 have been hindered by the lack of selective pharmacological tools as well as by the species-dependent differences …

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Discovery of novel 4-amino-6-arylaminopyrimidine-5-carbaldehyde oximes as dual inhibitors of EGFR and ErbB-2 protein tyrosine kinases

Guozhang Xu, Lily L. Searle, Terry V. Hughes, Amanda K. Beck et autres

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X-ray structure of EGFR in complex with oxime inhibitor

Marta C. Abad, Gen-Yang Xu, Michael P. Neeper, G.T. Struble et autres

Activation Properties of Heterologously Expressed Mammalian TRPV2

Michael P. Neeper, Yi Liu, Tasha L. Hutchinson, Yan Wang et autres

TRPV2 has been proposed as a potential pain target, in part due to its relatedness to the nociceptor TRPV1 and to its reported activation by noxious high temperatures (>52 degrees C). However, TRPV2 responses to heat as well as to the nonselective …

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X-ray Structure of Novel Biaryl-Based Dipeptidyl peptidase IV inhibitor

Lei Qiao, Carsten Baumann, Carl S. Crysler, Nisha S. Ninan et autres