Novel non-vanilloid VR1 antagonist of high analgesic effects and its structural requirement for VR1 antagonistic effects

• Published in: Bioorganic & medicinal chemistry letters Vol. 13; no. 24; pp. 4389 - 4393
• Main Authors: SUH, Young-Ger, LEE, Yong-Sil, OH, Uh-Taek, KOO, Jae-Yeon, JOO, Yung-Hyup, KIM, Sun-Young, JIN KWAN KIM, PARK, Young-Ho, MIN, Kyung-Hoon, PARK, Ok-Hui, SEUNG, Ho-Sun, KIM, Hee-Doo, PARK, Hyoung-Geun, CHOI, Ji-Yeon, JEEWOO LEE, KANG, Sang-Wook
• Format: Journal Article
• Language: English
• Published: Oxford Elsevier 15.12.2003
• Subjects: Analgesics; Analgesics - chemical synthesis; Analgesics - chemistry; Analgesics - pharmacology; Animals; Biological and medical sciences; Capsaicin - analogs & derivatives; Capsaicin - chemical synthesis; Capsaicin - chemistry; Capsaicin - pharmacology; Medical sciences; Mice; Models, Molecular; Molecular Conformation; Neuropharmacology; Pain - prevention & control; Pharmacology. Drug treatments; Receptors, Drug - antagonists & inhibitors; Structure-Activity Relationship; Sulfonamide; Rodentia; Thioureas; Dose activity relation; Vertebrata; VR1 vanilloid receptor; Mammalia; Analgesic; Structure activity relation; Mouse; Animal; Benzenic compound; Antagonist; Fluorine Organic compounds; Chemical synthesis
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2003.09.024

A novel non-vanilloid VR1 antagonist consisting of a new vanilloid equivalent exhibits excellent analgesic effects as well as highly potent antagonistic activities in both capsaicin single channel and calcium uptake assays. In addition, the structural requirement for the vanilloid equivalent of the potent VR1 antagonist has also been elucidated.