Matusák O, Bauer V, Bezeková M
Institute of Experimental Pharmacology, Slovak Academy of Sciences, Bratislava, Czechoslovakia.
Drugs Exp Clin Res. 1987;13(7):381-7.
The newly synthesized carbamate local anaesthetics (heptacaine and BK-141) affected the NCNA responses of different segments of the guinea-pig small (jejunum, ileum) and large (colon, taenia coli) intestine in a similar manner to the classic local anaesthetics (procaine and trimecaine). The sensitivity of NCNA responses to the action of local anaesthetics was, in order: primary contraction greater than rebound contraction greater than primary relaxation. The action of the carbamate local anaesthetics resembled that of trimecaine more than that of procaine. The results presented suggest that different Ca2+ channels participate in primary and rebound contraction and that local anaesthetics affect the receptor-operated Ca2+ channels in lower concentrations than the voltage-dependent ones.
新合成的氨基甲酸酯类局部麻醉药(庚卡因和BK - 141)对豚鼠小肠(空肠、回肠)和大肠(结肠、结肠带)不同节段的非胆碱能非肾上腺素能(NCNA)反应的影响,与经典局部麻醉药(普鲁卡因和三甲卡因)相似。NCNA反应对局部麻醉药作用的敏感性依次为:原发性收缩>反跳性收缩>原发性舒张。氨基甲酸酯类局部麻醉药的作用与三甲卡因的相似性超过普鲁卡因。所呈现的结果表明,不同的Ca2+通道参与原发性和反跳性收缩,并且局部麻醉药以低于电压依赖性Ca2+通道的浓度影响受体操纵性Ca2+通道。