Capsazocaine: a capsaicin-sensitive functional antagonist displays an argument on sensory capsaicin receptor.
1. Intravenous infusion of capsazocaine (CAPBZ), a molecular fusion product of irritant synthetic capsaicin and local analgesic benzocaine, at 100 micrograms/kg/min for 15 min inhibited capsaicin (10 micrograms/kg, IV)-induced spinal release of substance P-like immunoreactivity and vagus reflex responses in blood pressure and heart rate changes in rats. 2. Intrathecal perfusion of CAPBZ (1.0 nM) also reversed retrograde epigastric intraarterial capsaicin (10 micrograms/kg)-induced hypotensive spinal reflex. 3. In isolated guinea pig tissues, CAPBZ (1.0-100.0 microM) inhibited capsaicin (1.0 microM)-sensitive sensory and functional activities, including cardiatonic, bronchial, tracheal and ileal contractilities. CAPBZ is suggested to be a capsaicin antagonist.
Chen
I J
IJ
Department of Pharmacology, Kaohsiung Medical College, Taiwan, Republic of China.
Lo
Y C
YC
Lo
W J
WJ
Yeh
J L
JL
Wu
B N
BN
D000818:Animals; D001565:Benzoates / Q000494:pharmacology*; D001794:Blood Pressure / Q000187:drug effects; D001980:Bronchi / Q000187:drug effects; D015740:Calcitonin Gene-Related Peptide / Q000494:pharmacology; D005260:Female; D006168:Guinea Pigs; D006339:Heart Rate / Q000187:drug effects; D007082:Ileum / Q000187:drug effects; D066298:In Vitro Techniques; D007278:Injections, Spinal; D008297:Male; D009200:Myocardial Contraction / Q000187:drug effects; D010080:Oxazoles / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D011955:Receptors, Drug / Q000037:antagonists & inhibitors*; D012018:Reflex / Q000187:drug effects; D011984:Sensory Receptor Cells / Q000187:drug effects*; D013116:Spinal Cord / Q000187:drug effects; D013373:Substance P / Q000008:administration & dosage / Q000494:pharmacology; D014132:Trachea / Q000187:drug effects; D014630:Vagus Nerve / Q000187:drug effects
D001565:Benzoates; D010080:Oxazoles; D011955:Receptors, Drug; C108689:capsazocaine; D013373:Substance P; D015740:Calcitonin Gene-Related Peptide