H-7, a protein kinase C inhibitor, inhibits spontaneous tone and spasmogenic responses in normal and sensitized guinea pig trachea.
1. H-7, a protein kinase C inhibitor, fully inhibited the spontaneous and stimulated (KCl 20 mM or histamine 0.5 mM) tone of trachea from normal and sensitized guinea pig. 2. H-7 depressed the concentration-contraction curves to KCl, histamine or 5-hydroxytryptamine in epithelium-denuded, indomethacin-treated, trachea from normal and sensitized guinea pigs while responses to CaCl2 (in Ca2+ -free, K+ -depolarized tissues) and acetylcholine were not affected. 3. H-7 (100 microM did not depress Ca2+ (20 microM-induced contraction of Triton X-100 skinned trachea. 4. These results suggest the involvement of PKC in the maintenance of spontaneous tone and spasmogenic responses of guinea pig trachea.
de Diego
A
A
Departament de Farmacologia, Facultat de Medicina i Odontologia, Universitat de Valencia, Spain.
Cortijo
J
J
Villagrasa
V
V
Perpina
M
M
Morcillo
E J
EJ
D019307:1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine; D000818:Animals; D002122:Calcium Chloride / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D006168:Guinea Pigs; D006632:Histamine / Q000494:pharmacology; D066298:In Vitro Techniques; D007546:Isoquinolines / Q000494:pharmacology*; D008297:Male; D009130:Muscle, Smooth / Q000187:drug effects / Q000502:physiology; D010879:Piperazines / Q000494:pharmacology*; D011189:Potassium Chloride / Q000494:pharmacology; D011493:Protein Kinase C / Q000037:antagonists & inhibitors*; D014132:Trachea / Q000187:drug effects* / Q000502:physiology
D004791:Enzyme Inhibitors; D007546:Isoquinolines; D010879:Piperazines; D011189:Potassium Chloride; D006632:Histamine; D019307:1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine; D011493:Protein Kinase C; D002122:Calcium Chloride