Long-lasting antagonistic effects of monatepil on Ca2+ current in guinea-pig ventricular cells.
Monatepil maleate (CAS 103377-41-9, AJ-2615), a new derivative of dihydrodibenzothiepins, showed dose-dependent inhibition of Ca2+ current (ICa) in single cardiac cells isolated from guinea-pig ventricle. ICa was elicited by depolarization from -40 mV to +10 mV at 0.2 Hz. IC50 value of monatepil for the peak ICa at +10 mV was 18.7 nmol/l. The ICa inhibition was still sustained 30 min after washout, indicating that monatepil had long lasting activity in the mammalian single muscle cell.
Nagata
S
S
Department of Pharmacology I, Dainippon Pharmaceutical Co., Ltd., Osaka, Japan.
Hosoki
K
K
Karasawa
T
T
D000818:Animals; D002121:Calcium Channel Blockers / Q000494:pharmacology*; D003988:Dibenzothiepins / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004594:Electrophysiology; D006168:Guinea Pigs; D006321:Heart / Q000187:drug effects*; D006352:Heart Ventricles / Q000166:cytology / Q000187:drug effects / Q000378:metabolism; D066298:In Vitro Techniques; D008297:Male; D009206:Myocardium / Q000166:cytology / Q000378:metabolism*; D018408:Patch-Clamp Techniques; D010879:Piperazines / Q000494:pharmacology
D002121:Calcium Channel Blockers; D003988:Dibenzothiepins; D010879:Piperazines; C067818:monatepil