Design and Optimization of Benzimidazole-Containing Transient Receptor Potential Melastatin 8 (TRPM8) Antagonists

Transient receptor potential melastatin 8 (TRPM8) is a nonselective cation channel that is thermoresponsive to cool to cold temperatures (8−28 °C) and also may be activated by chemical agonists such as menthol and icilin. Antagonism of TRPM8 activation is currently under investigation for the treatm...

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Veröffentlicht in:	Journal of medicinal chemistry 2011-01, Vol.54 (1), p.233-247
Hauptverfasser:	Parks, Daniel J, Parsons, William H, Colburn, Raymond W, Meegalla, Sanath K, Ballentine, Shelley K, Illig, Carl R, Qin, Ning, Liu, Yi, Hutchinson, Tasha L, Lubin, Mary Lou, Stone, Dennis J, Baker, Judith F, Schneider, Craig R, Ma, Jianya, Damiano, Bruce P, Flores, Christopher M, Player, Mark R
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Analgesics - chemical synthesis Analgesics - pharmacokinetics Analgesics - pharmacology Animals Benzimidazoles - chemical synthesis Benzimidazoles - pharmacokinetics Benzimidazoles - pharmacology Biological Availability Constriction, Pathologic - drug therapy Constriction, Pathologic - physiopathology Dogs HEK293 Cells Humans Hyperalgesia - drug therapy Hyperalgesia - physiopathology In Vitro Techniques Isoxazoles - chemical synthesis Isoxazoles - pharmacokinetics Isoxazoles - pharmacology Macaca fascicularis Microsomes, Liver - metabolism Neuralgia - drug therapy Neuralgia - physiopathology Rats Structure-Activity Relationship TRPM Cation Channels - antagonists & inhibitors
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