Studies on the affinity and selectivity of tiquizium bromide (HSR-902), a novel spasmolytic agent, for muscarinic receptors.
The affinity and selectivity of a novel spasmolytic agent, tiquizium bromide (HSR-902), for muscarinic receptors were studied by the radioligand binding technique using 3H-quinuclidinyl benzilate. The parameters (Ki, nH) of HSR-902 obtained from competition experiments in cerebral cortex and heart muscarinic receptors showed that HSR-902 was an atropine-type, nonselective muscarinic antagonist. The affinity of HSR-902 toward the stomach and ileal muscarinic receptors was about 3-4 times more potent than atropine.
Oshita
M
M
Research Laboratories, Hokuriku Seiyaku Co., Ltd., Fukui, Japan.
Ohashi
T
T
Morikawa
K
K
Kato
H
H
Ito
Y
Y
Muramatsu
I
I
D000818:Animals; D001285:Atropine / Q000378:metabolism; D001667:Binding, Competitive; D002540:Cerebral Cortex / Q000378:metabolism; D005753:Gastric Mucosa / Q000378:metabolism; D007082:Ileum / Q000378:metabolism; D066298:In Vitro Techniques; D008297:Male; D009206:Myocardium / Q000378:metabolism; D010276:Parasympatholytics / Q000378:metabolism*; D010890:Pirenzepine / Q000378:metabolism; D011807:Quinolizines / Q000378:metabolism*; D051381:Rats; D011919:Rats, Inbred Strains; D011976:Receptors, Muscarinic / Q000378:metabolism*
D010276:Parasympatholytics; D011807:Quinolizines; D011976:Receptors, Muscarinic; D010890:Pirenzepine; C030950:thiaton; D001285:Atropine