Diaryldiamines with Dual Inhibition of the Histamine H3 Receptor and the Norepinephrine Transporter and the Efficacy of 4-(3-(Methylamino)-1-phenylpropyl)-6-(2-( …
RJ Altenbach, LA Black, MI Strakhova…
文献索引:Altenbach, Robert J.; Black, Lawrence A.; Strakhova, Marina I.; Manelli, Arlene M.; Carr, Tracy L.; Marsh, Kennan C.; Wetter, Jill M.; Wensink, Erica J.; Hsieh, Gin C.; Honore, Prisca; Garrison, Tiffany Runyan; Brioni, Jorge D.; Cowart, Marlon D. Journal of Medicinal Chemistry, 2010 , vol. 53, # 21 p. 7869 - 7873
H 3 antagonists such as thioperamide have been reported to be active in models of pain.(5) More recently, the H 3 R antagonist GSK-189254 (1) was reported to be efficacious in preclinical models of neuropathic pain and was examined in a phase I electrical hyperalgesia model.(6, 7) The efficacy of histamine H 3 antagonists can be rationalized as likely due to increases in levels of monoamines that are recognized to modulate pain sensation, such as NE. ...