Törneke K, Larsson C I, Appelgren L E
Swedish University of Agricultural Sciences, Faculty of Veterinary Medicine, Department of Pharmacology and Toxicology, Uppsala, Sweden.
J Vet Pharmacol Ther. 1997 Jun;20(3):216-9. doi: 10.1111/j.1365-2885.1997.tb00098.x.
Strips of tracheal smooth muscle from 12 horses were contracted by carbachol in tissue baths under isometric conditions. This contraction (approximately 50% of maximum: EC50) was relaxed completely with adrenoceptor drugs. The only exception was clenbuterol, where the degree of relaxation was approximately 90%. In all horses the EC50-value for isoprenaline (mean 1.6 x 10(-8) M) was less than that for adrenaline (mean 9.6 x 10(-8) M) and noradrenaline (mean 1.8 x 10(-6) M). The potency ratio was 1 < 6 < 110 which indicates that the beta 2-subtype dominates among the beta-adrenoceptors of equine airways. All preparations were also very sensitive to the specific and potent beta 2-receptor agonists clenbuterol (mean 5.7 x 10(-9) M) and procaterol (mean 3.6 x 10(-10) M). No differences in EC50-values due to age, sex and breed were observed in this material. The standard deviation of the mean EC50-values seems to be larger for the specific beta 2-adrenoceptor agonists than for the unspecific. A reason for this could be differences in the pattern of the beta-adrenoceptor population.
在等长条件下,将来自12匹马的气管平滑肌条在组织浴中用卡巴胆碱收缩。这种收缩(约为最大收缩的50%:半数有效浓度)可被肾上腺素能药物完全松弛。唯一的例外是克伦特罗,其松弛程度约为90%。在所有马匹中,异丙肾上腺素的半数有效浓度值(平均1.6×10⁻⁸ M)低于肾上腺素(平均9.6×10⁻⁸ M)和去甲肾上腺素(平均1.8×10⁻⁶ M)。效价比为1<6<110,这表明β₂亚型在马气道的β肾上腺素能受体中占主导地位。所有制剂对特异性强效β₂受体激动剂克伦特罗(平均5.7×10⁻⁹ M)和丙卡特罗(平均3.6×10⁻¹⁰ M)也非常敏感。在该材料中未观察到因年龄、性别和品种导致的半数有效浓度值差异。特异性β₂肾上腺素能受体激动剂的平均半数有效浓度值的标准差似乎比非特异性激动剂的标准差更大。其原因可能是β肾上腺素能受体群体模式的差异。