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观察大鼠离体胃体环行肌和胃底环行肌不同的药理学特征,分析核苷及核苷酸类物质诱发胃体环行肌收缩反应的作用特点和受体机制。制备大鼠离体胃体环行肌和胃底环行肌标本,利用受体药理学技术观察药物诱发的收缩反应。在胃体环行肌KCl所致收缩反应与胃底环行肌无显著性差别;但是,CCh收缩胃体环行肌的EC50值[(0.45±0.15)μmol.L-1]显著高于胃底环行肌[(0.20±0.09)μmol.L-1,P<0.01]。5-HT和His收缩两种标本的EC50值无显著差异(P>0.05);但是,在胃体环行肌5-HT和His产生收缩反应的Emax值[(0.81±0.26)和(0.88±0.27)g]显著小于胃底环行肌[(2.67±0.61)和(1.90±0.68)g,P<0.01]。在预收缩胃体环行肌,ATP(0.1～3000μmol.L-1)诱发浓度依赖性收缩反应,未见舒张反应;在预收缩胃底环行肌标本,同浓度ATP诱发先舒张后收缩的双相反应,并呈浓度依赖性。ATP、UTP、ADP、2-MeSATP和α,β-MeATP浓度依赖性诱发大鼠胃体环行肌收缩反应,2-MeSATP的EC50值为(7.2±5.2)nmol.L-1比Ach[(3.47±1.20)μmol.L-1]低500倍;各药物产生收缩反应的效价序列为:2-MeSATP>>ADP>ATP=UTP>α,β-MeATP>>腺苷。酚妥拉明、普萘洛尔、阿托品及河豚毒素不影响ATP和UTP诱发的胃体环行肌收缩反应。研究结果表明,大鼠胃体环行肌的药理学特征明显不同于胃底环行肌;核苷酸类物质通过某种特殊的P2Y受体介导胃体环行肌收缩反应,是调节胃体环行肌收缩功能的重要介质。
To observe the different pharmacological characteristics of isolated gastric gastric muscle and gastric fundus muscle, and to analyze the role and mechanism of nucleoside and nucleotide-induced contractile response of gastric muscle. Preparation of isolated rat gastric corpus circular muscle and gastric fundus ring specimens, the use of receptor pharmacology to observe drug-induced contractile response. However, there was no significant difference in the contractile response of KCl between gastric herpetic muscle and gastric fundus. However, EC50 of CCh contracting gastric herpetic muscle [(0.45 ± 0.15) μmol.L-1] was significantly higher than that of gastric fundus [(0.20 ± 0.09) μmol.L-1, P <0.01]. There was no significant difference in EC50 values between 5-HT and His contraction (P> 0.05); however, the Emax values of contractile response to 5-HT and His in the gastric corpus myosphere [(0.81 ± 0.26) and (0.88 ± 0.27 ) g] was significantly less than that in the gastric fundus [(2.67 ± 0.61) and (1.90 ± 0.68) g, P <0.01]. In the pre-contracted gastrocnemius muscle, ATP (0.1 ~ 3000μmol.L-1) induced a concentration-dependent contractile response and no diastolic reaction. In the pre-contracted gastric fundus, ATP- Reaction, and in a concentration-dependent manner. The EC50 of 2-MeSATP was (7.2 ± 5.2) nmol.L-1, which was significantly higher than that of Ach [(3.47 ± 1.20) μmol.L-1]. The titer sequence of each drug that produced contractile response was: 2-MeSATP >> ADP> ATP = UTP> α, β-MeATP >> adenosine. Phentolamine, propranolol, atropine, and tetrodotoxin do not affect ATP and UTP-induced constriction responses in the gastrocnemius muscle. The results show that the pharmacological characteristics of the rat gastric circulatory muscle significantly different from the gastric fundus; nucleotide through a special P2Y receptor mediated gastric contractile response is to regulate the gastrocnemius muscle Important medium for systolic function.