[A study on the affinities of various muscarinic antagonists to the human detrusor muscle].
The affinities of various muscarinic antagonists to human detrusor muscle were determined using radioligand binding techniques. Saturation experiments with 3H-QNB revealed that there were significant amount of muscarinic cholinergic receptors in human detrusor muscle. Displacement of 3H-QNB binding by various muscarinic subtype selective drugs was studied in the inhibition experiment. Pirenzepine, AFDX-116 and 4-DAMP inhibited the 3H-QNB binding to human detrusor muscle with the Ki values (nM) (mean +/- S.D., n = 6) of 243 +/- 62.5, 59.7 +/- 15.3 and 2.69 +/- 0.96, respectively. These data indicate that M3-selective drug possesses the highest affinity to human detrusor muscle. The Ki values of oxybutynin and tiquizium bromide were similar to those of 4-DAMP, suggesting that these two drugs have strong affinities to human detrusor muscle.
Kondo
S
S
Second Department of Biochemistry, Akita University School of Medicine.
Morita
T
T
Hirano
S
S
D000218:Adamantane / Q000031:analogs & derivatives* / Q000378:metabolism / Q000494:pharmacology; D000368:Aged; D001667:Binding, Competitive; D005260:Female; D006801:Humans; D008297:Male; D008875:Middle Aged; D009130:Muscle, Smooth / Q000378:metabolism*; D010276:Parasympatholytics / Q000378:metabolism / Q000494:pharmacology*; D010890:Pirenzepine / Q000031:analogs & derivatives* / Q000378:metabolism / Q000494:pharmacology*; D011813:Quinuclidinyl Benzilate / Q000378:metabolism; D011869:Radioligand Assay; D011976:Receptors, Muscarinic / Q000145:classification / Q000378:metabolism*; D001743:Urinary Bladder / Q000378:metabolism*
D010276:Parasympatholytics; D011976:Receptors, Muscarinic; C016358:2,4-diamino-5-adamantyl-6-methylpyrimidine; D010890:Pirenzepine; D011813:Quinuclidinyl Benzilate; C048593:otenzepad; D000218:Adamantane