HUMAN BRONCHUS;
BUTYRYLCHOLINESTERASE;
ACETYLCHOLINESTERASE;
ACETYLCHOLINE;
BUTYRYLCHOLINE;
TETRAISOPROPYLPYROPHOS-PHORAMIDE;
NEOSTIGMINE;
D O I:
10.1111/j.1476-5381.1993.tb13486.x
中图分类号:
R9 [药学];
学科分类号:
1007 ;
摘要:
1 Neostigmine and BW284C51 induced concentration-dependent contractions in human isolated bronchial preparations whereas tetraisopropylpyrophosphoramide (iso-OMPA) was inactive on airway resting tone. 2 Neostigmine (0. 1 mum) or iso-OMPA (I 00 mum) increased acetylcholine sensitivity in human isolated bronchial preparations but did not alter methacholine or carbachol concentration-effect curves. 3 In the presence of iso-OMPA (10 mum) the bronchial rings were more sensitive to neostigmine. The pD2 values were, control: 6.05 +/- 0.15 and treated: 6.91 +/- 0.14. 4 Neostigmine or iso-OMPA retarded the degradation of acetylcholine when this substrate was exogenously added to human isolated airways. A marked reduction of acetylcholine degradation was observed in the presence of both inhibitors. Exogenous butyrylcholine degradation was prevented by iso-OMPA (10 mum) but not by neostigmine (0. 1 mum). 5 These results suggest the presence of butyrylcholinesterase activity in human bronchial muscle and this enzyme may co-regulate the degradation of acetylcholine in this tissue.