Dihydropyridine and peripheral type benzodiazepine binding sites: subcellular distribution and molecular size determination.
Electrophysiological and pharmacological studies have shown that peripheral-type benzodiazepine receptors modulate voltage-sensitive calcium channels in the heart. We have compared these binding sites with binding sites for [3H]dihydropyridines, which are believed to label such channels. Although no direct or allosteric interaction could be demonstrated between the two sites, their subcellular distribution--sarcolemma and ryanodine-sensitive sarcoplasmic reticulum--was parallel. Size determination of the two sites suggests that the receptors for these two classes of compounds are separate molecules packaged in the same membrane compartment.
A
A
Doble
J
J
Benavides
O
O
Ferris
P
P
Bertrand
J
J
Menager
N
N
Vaucher
M C
MC
Burgevin
A
A
Uzan
C
C
Gueremy
G
G
Le Fur
D000818:Animals; D001570:Benzodiazepinones / Q000378:metabolism / Q000494:pharmacology; D001665:Binding Sites; D002118:Calcium / Q000378:metabolism; D002121:Calcium Channel Blockers / Q000378:metabolism*; D015220:Calcium Channels; D002458:Cell Fractionation; D004285:Dogs; D007473:Ion Channels; D007546:Isoquinolines / Q000378:metabolism / Q000494:pharmacology; D017275:Isradipine; D008297:Male; D008970:Molecular Weight; D009206:Myocardium / Q000378:metabolism / Q000648:ultrastructure*; D009543:Nifedipine / Q000031:analogs & derivatives / Q000378:metabolism / Q000494:pharmacology; D009568:Nitrendipine; D010069:Oxadiazoles / Q000378:metabolism; D051381:Rats; D011919:Rats, Inbred Strains; D011963:Receptors, GABA-A / Q000378:metabolism*; D011978:Receptors, Nicotinic / Q000378:metabolism*; D012508:Sarcolemma / Q000378:metabolism*; D012519:Sarcoplasmic Reticulum / Q000378:metabolism*; D014700:Verapamil / Q000378:metabolism / Q000494:pharmacology
D001570:Benzodiazepinones; D002121:Calcium Channel Blockers; D015220:Calcium Channels; D007473:Ion Channels; D007546:Isoquinolines; D010069:Oxadiazoles; D011963:Receptors, GABA-A; D011978:Receptors, Nicotinic; C028513:4'-chlorodiazepam; D009568:Nitrendipine; D014700:Verapamil; D009543:Nifedipine; D002118:Calcium; C037850:PK 11195; D017275:Isradipine