The effect of AL0671, a novel potassium channel opener, on potassium current in rat aortic smooth muscle cells.
1. We evaluated the mechanism of activation by AL0671, a novel potassium channel opener, of potassium current in rat aortic smooth muscle cells. 2. Under conditions of whole cell recording, AL0671 (1-1000 microM) markedly increased potassium current with a Hill coefficient of 2 and dissociation constant of 1.5 x 10(-4) M. This activation was completely inhibited by intracellular ATP. 3. Under inside-out patch conditions, the ATP-sensitive K+ channels (KATP) treated with AL0671 (100 microM) showed prolongation of the slower open time component and shortening of the slower closed time component without modification of channel conductance.
Matzno
S
S
Basic Research Laboratories, Green Cross Corporation, Osaka, Japan.
Sato
R
R
Takai
H
H
Aida
Y
Y
Karasaki
S
S
Oyaizu
M
M
Nakamura
N
N
Katori
R
R
D000818:Animals; D001011:Aorta / Q000187:drug effects*; D001643:Bridged Bicyclo Compounds / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D006146:Guanidines / Q000494:pharmacology*; D000960:Hypolipidemic Agents / Q000494:pharmacology*; D008297:Male; D008564:Membrane Potentials / Q000187:drug effects; D008958:Models, Molecular; D009131:Muscle, Smooth, Vascular / Q000187:drug effects*; D015221:Potassium Channels / Q000187:drug effects*; D051381:Rats; D017208:Rats, Wistar; D013997:Time Factors
C088267:AL 0670; D001643:Bridged Bicyclo Compounds; D006146:Guanidines; D000960:Hypolipidemic Agents; D015221:Potassium Channels