[Effect of terodiline hydrochloride in isolated rabbit detrusor].
Effect of terodiline on isolated rabbit and guinea pig detrusor was investigated in comparison with that of flavoxate and oxybutynin. Terodiline (10(-6) M) parallelly shifted the dose-response curve for carbachol in rabbit detrusor to the right, and high doses of terodiline (3 X 10(-6)-3 X 10(-5) M) inhibited the maximal contraction. Flavoxate (10(-5) M or more) also inhibited the maximal contraction. Oxybutynin (10(-8) M or more) shifted the dose-response curve to the right, but did not affect the maximal contraction. At 3 X 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 X 10(-7) M) or nifedipine (3 X 10(-6) M) by 35% or 73%, respectively, the combination of atropine (10(-7) M) and nifedipine (10(-6) M) abolished it. Oxybutynin (3 X 10(-7) M) inhibited it by about 30%; terodiline (10(-6) M or more) and flavoxate (10(-5) M or more) dose-dependently inhibited it, and abolished at 10(-4) M and 3 X 10(-4) M, respectively. Terodiline inhibited the 1-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 X 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.(ABSTRACT TRUNCATED AT 250 WORDS)
D000818:Animals; D002082:Butylamines / Q000494:pharmacology*; D002121:Calcium Channel Blockers / Q000494:pharmacology*; D003864:Depression, Chemical; D004305:Dose-Response Relationship, Drug; D005422:Flavoxate / Q000494:pharmacology; D006168:Guinea Pigs; D066298:In Vitro Techniques; D008297:Male; D008333:Mandelic Acids / Q000494:pharmacology; D009119:Muscle Contraction / Q000187:drug effects*; D009130:Muscle, Smooth / Q000187:drug effects*; D010276:Parasympatholytics / Q000494:pharmacology; D011817:Rabbits; D001743:Urinary Bladder / Q000187:drug effects
D002082:Butylamines; D002121:Calcium Channel Blockers; D008333:Mandelic Acids; D010276:Parasympatholytics; D005422:Flavoxate; C010637:terodiline; C005419:oxybutynin