Trapidil and other 5-triazolo-(1, 5-alpha)-pyrimidine derivatives as calcium channel blockers in 108CC5 cells.
The action of trapidil (RocornalR) and its derivatives AR 12-456 and AR 12-160 on the inward calcium current (ICa) was studied in mouse neuroblastoma x rat glioma hybrid cells of the line 108CC5 under voltage clamp conditions by means of a suction pipette method. A dissociation constant of the calcium channel-trapidil complex of 277 microM was estimated for the initial inhibition of ICa by trapidil. Half maximal block of ICa was produced by 80 +/- 20 microM AR 12-456 and 500 +/- 150 microM AR 12-160.
S
S
Hering
R
R
Bodewei
B
B
Schubert
E G
EG
Krause
A
A
Wollenberger
D000818:Animals; D002118:Calcium / Q000378:metabolism; D002121:Calcium Channel Blockers; D000697:Central Nervous System Stimulants / Q000494:pharmacology*; D006822:Hybrid Cells / Q000187:drug effects / Q000378:metabolism; D007473:Ion Channels / Q000187:drug effects / Q000378:metabolism; D051379:Mice; D011743:Pyrimidines / Q000494:pharmacology*; D051381:Rats; D014192:Trapidil / Q000031:analogs & derivatives / Q000378:metabolism / Q000494:pharmacology*
D002121:Calcium Channel Blockers; D000697:Central Nervous System Stimulants; D007473:Ion Channels; D011743:Pyrimidines; C046930:AR 12456; C046931:5,7-dimethyl-(1,2,4)triazolo(1,5-a)pyrimidine; D014192:Trapidil; D002118:Calcium