Effect of terodiline hydrochloride in isolated rabbit detrusor.

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Abstract
Effect of terodiline on isolated rabbit and guinea pig detrusor was investigated in comparison with that of flavoxate and oxybutynin. Terodiline (10-6M) parallelly shifted the dose-response curve for carbachol in rabbit detrusor to the right, and high doses of terodiline (3 .times. 10-6 .apprx. 3 .times. 10-5 M) inhibited the maximal contraction. Oxybutynin (10-8M or more) shifted the dose-response curve to the right, but did not affect the maximal contraction. At 3 .times. 10-6 M or more, terodiline dose-dependently inhibited the Ca-contraction of rabbit detrusor. While the contraction of rabbit detrusor induced by electrical field stimulation was inhibited by atropine (3 .times. 10-7 M) or nifedipine (3 .times. 10-6 M) by 35% or 73%, respectively, the combination of atropine (10-7 M) and nifedpine (10-6M) abolished it. Oxybutynin (3 .times. 10-7 M) inhibited it by about 30%; terodiline (10-6 M or more) and falvoxate (10-5M or more) dose-dependently inhibited it, and abolished at 10-4 M and 3 .times. 10-4 M, respectively. Terodiline inhibited the l-quinuclidinyl-[phenyl-4-3H]-benzilate binding to the microsomal fraction of guinea pig urinary bladder, brain, atria and ileum dose-dependently, and it had similar affinity among these fractions. Terodiline (3 .times. 10-6 M or more) inhibited the 45Ca uptake to minced guinea pig urinary bladder dose-dependently, but did not influence the 45Ca efflux even at 10-4 M. Flavoxate (10-4 M) only slightly inhibited the 45Ca uptake. The present result suggests that the inhibitory action of terodiline on the contraction of detrusor is attributable to the anti-muscarinic and Ca-antagonistic effect, and terodiline has a different pharmacological property from oxybutynin and flavoxate.