盐酸甲基黄酮醇胺对离体兔回肠收缩性的影响
[Effects of methylflavonolamine hydrochloride on contractility of isolated rabbit ileum].
作者信息
Long P, Yan C H, Zhang M S, Zhou E F
机构信息
Department of Pharmacology, Shanxi Medical College, Taiyuan, China.
出版信息
Zhongguo Yao Li Xue Bao. 1992 Jan;13(1):63-5.
Methylflavonolamine hydrochloride (MFA), verapamil (Ver), and trifluoperazine (Tri) inhibited the contractions induced by submaximal concentrations of acetylcholine (ACh) and serotonin (5-HT). IC50 values (mumol.L-1) were 33.2 +/- 0.7, 0.276 +/- 0.018, 3.83 +/- 0.23, and 15.31 +/- 0.10, 0.233 +/- 0.017, 2.33 +/- 0.20, respectively. MFA, Ver, and Tri inhibited the contractions induced by CaCl2 and pD'2 values were 4.3 +/- 0.3, 6.23 +/- 0.22, 4.99 +/- 0.24, respectively. MFA 3 mumol.L-1, Ver 0.03 mumol.L-1, and Tri 3 mumol.L-1 inhibited the contractions induced by ACh in Ca(2+)-free medium, while MFA 60 mumol.L-1, Tri 30 mumol.L-1, but not Ver 0.6 mumol.L-1, had pronounced inhibitions on extracellular calcium-dependent contractions induced by ACh. These results suggest that MFA has a calcium antagonistic effect and that MFA is similar to Tri, but not Ver, in mechanism.
盐酸甲基黄酮醇胺（MFA）、维拉帕米（Ver）和三氟拉嗪（Tri）抑制了由亚最大浓度的乙酰胆碱（ACh）和5-羟色胺（5-HT）诱导的收缩。半数抑制浓度（IC50值，μmol·L⁻¹）分别为33.2±0.7、0.276±0.018、3.83±0.23，以及15.31±0.10、0.233±0.017、2.33±0.20。MFA、Ver和Tri抑制了由氯化钙诱导的收缩，其解离常数负对数值（pD'2值）分别为4.3±0.3、6.23±0.22、4.99±0.24。3μmol·L⁻¹的MFA、0.03μmol·L⁻¹的Ver和3μmol·L⁻¹的Tri抑制了无钙培养基中由ACh诱导的收缩，而60μmol·L⁻¹的MFA、30μmol·L⁻¹的Tri，但0.6μmol·L⁻¹的Ver对由ACh诱导的细胞外钙依赖性收缩有显著抑制作用。这些结果表明MFA具有钙拮抗作用，且在作用机制上MFA与Tri相似，但与Ver不同。
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