特異的および非特異的刺激物質に対するモルモット摘出胆のう収縮反応に及ぼすButoxybenzyl hyoscyamine bromideの影響
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Effects of butoxybenzyl hyoscyamine bromide (BBHB) on contractile response of isolated guinea-pig gallbladder to specific and non-specific stimulants were examined. Results are as follows: 1) BBHB, in low concentrations (10-9_??_10-6M), exerted an atropine-like competitive blocking action against the acetylcholine (ACh)-induced contraction. The affinity to muscarinic receptor of BBHB (pA2=8.79±0.08, molar unit) was greater than that of atropine (pA2=7.64±0.12, molar unit). 2) BBHB, in high concentrations (5×10-6_??_4×10-4M), showed non-competivity blocking action against the KCl-induced contraction (pD2=3.30±0.06) and the BaCl2-induced contraction (pD2=3.12±0.15). The affinity of BBHB was somewhat less than that of papaverine (pD2=4.80±0.11 to BaCl2 and 4.81±0.05 to KCl). 3) In the Ca++-free medium, high concentrations of BBHB inhibited noncompetitively the BaCl2-induced contraction, the pD2 value being 3.05±0.12, however BBHB, even in a high concentration, did not affect the Ca++-induced contraction of K+-depolarized preparation in Ca++-free medium. On the other hand, papaverine antagonized noncompetitively the Ba++-induced contraction (pD2=4.56±0.21) and the Ca++-induced contraction (pD2 =4.75 ±0.03). These results suggest that BBHB, in low concentrations, antagonizes competitively the ACh-induced contraction at muscarinic receptors, whereas in gigh concentrations reduced K+-induced and Ba++-induced contractions, presumably by interfering with the K+- and Ba++-induced inward release of membrane-bound calcium, by decreasing the Ba++-influx and/or by preventing the barium ion from being utilized by the contractile proteins.
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