sb-705498 and Neuralgia

sb-705498 has been researched along with Neuralgia* in 1 studies

Other Studies

1 other study(ies) available for sb-705498 and Neuralgia

Article	Year
Design, synthesis, and biological evaluation of novel biphenyl-4-carboxamide derivatives as orally available TRPV1 antagonists. Bioorganic & medicinal chemistry, 2018, 07-23, Volume: 26, Issue:12 A new series of transient receptor potential vanilloid type 1 (TRPV1) antagonists were designed and synthesized from N-(3-hydroxyphenyl)-2-(piperidin-1-ylmethyl)biphenyl-4-carboxamide hydrochloride (8). SAR studies identified (R)-N-(1-methyl-2-oxo-1,2,3,4-tetrahydro-7-quinolyl)-2-[(2-methylpyrrolidin-1-yl)methyl]biphenyl-4-carboxamide hydrochloride (ASP8370, 7), as a compound with high aqueous solubility, satisfactory stability in human liver microsomes, and reduced CYP3A4 inhibition. ASP8370 was selected as a clinical development candidate with significant ameliorative effects on neuropathic pain. SAR studies also revealed the structural mechanisms underlying the switching between TRPV1 antagonism and agonism. Topics: Administration, Oral; Amides; Anticonvulsants; Biphenyl Compounds; Cytochrome P-450 CYP3A; Drug Design; HEK293 Cells; Humans; Inhibitory Concentration 50; Microsomes, Liver; Neuralgia; Solubility; Structure-Activity Relationship; TRPV Cation Channels	2018

Article

Year

Design, synthesis, and biological evaluation of novel biphenyl-4-carboxamide derivatives as orally available TRPV1 antagonists.

Bioorganic & medicinal chemistry, 2018, 07-23, Volume: 26, Issue:12

A new series of transient receptor potential vanilloid type 1 (TRPV1) antagonists were designed and synthesized from N-(3-hydroxyphenyl)-2-(piperidin-1-ylmethyl)biphenyl-4-carboxamide hydrochloride (8). SAR studies identified (R)-N-(1-methyl-2-oxo-1,2,3,4-tetrahydro-7-quinolyl)-2-[(2-methylpyrrolidin-1-yl)methyl]biphenyl-4-carboxamide hydrochloride (ASP8370, 7), as a compound with high aqueous solubility, satisfactory stability in human liver microsomes, and reduced CYP3A4 inhibition. ASP8370 was selected as a clinical development candidate with significant ameliorative effects on neuropathic pain. SAR studies also revealed the structural mechanisms underlying the switching between TRPV1 antagonism and agonism.

Topics: Administration, Oral; Amides; Anticonvulsants; Biphenyl Compounds; Cytochrome P-450 CYP3A; Drug Design; HEK293 Cells; Humans; Inhibitory Concentration 50; Microsomes, Liver; Neuralgia; Solubility; Structure-Activity Relationship; TRPV Cation Channels

2018