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牛气管平滑肌的衰老与胆碱能反应

Aging and cholinergic responses in bovine trachealis muscle.

作者信息

Wills M, Douglas J S

机构信息

John B. Pierce Foundation Laboratory, New Haven, Ct. 06519.

出版信息

Br J Pharmacol. 1988 Apr;93(4):918-24. doi: 10.1111/j.1476-5381.1988.tb11480.x.

Abstract
  1. The relative potencies of muscarinic agonists on bovine tracheal smooth muscle were unchanged as a consequence of aging and were carbachol greater than oxotremorine greater than muscarine greater than pilocarpine greater than McNeil A-343. 2. During aging, the potencies of carbachol, oxotremorine, McNeil A-343 and pilocarpine, but not muscarine, were reduced. 3. Maximal induced tensions to all the agents studied were reduced as a consequence of age. 4. Irreversible antagonism with benzilylcholine mustard showed that agonist efficacy was significantly reduced during aging. 5. Estimated receptor occupancy at the EC50 was significantly greater in tracheal tissues from the mature versus immature cows for every agonist studied. 6. The dissociation constants for full agonists (carbachol, oxotremorine and methacholine) were decreased with maturation while the converse was observed with partial agonists (McNeil A-343, pilocarpine). 7. We conclude that there are significant changes in the properties and coupling of muscarinic receptors during aging. These changes may contribute to the reduced airway reactivity seen in vivo.
摘要
  1. 毒蕈碱激动剂对牛气管平滑肌的相对效价不会因衰老而改变,且卡巴胆碱大于氧化震颤素大于毒蕈碱大于毛果芸香碱大于麦克尼尔A - 343。2. 在衰老过程中,卡巴胆碱、氧化震颤素、麦克尼尔A - 343和毛果芸香碱的效价降低,但毒蕈碱的效价未降低。3. 由于年龄增长,所有研究药物诱导的最大张力均降低。4. 用苯甲酰胆碱芥进行不可逆拮抗表明,衰老过程中激动剂效能显著降低。5. 对于所研究的每种激动剂,在成熟奶牛与未成熟奶牛的气管组织中,在半数有效浓度(EC50)时估计的受体占有率在成熟奶牛中显著更高。6. 完全激动剂(卡巴胆碱、氧化震颤素和乙酰甲胆碱)的解离常数随成熟而降低,而部分激动剂(麦克尼尔A - 343、毛果芸香碱)则相反。7. 我们得出结论,衰老过程中毒蕈碱受体的性质和偶联存在显著变化。这些变化可能导致体内气道反应性降低。

相似文献

1
Aging and cholinergic responses in bovine trachealis muscle.牛气管平滑肌的衰老与胆碱能反应
Br J Pharmacol. 1988 Apr;93(4):918-24. doi: 10.1111/j.1476-5381.1988.tb11480.x.
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Muscarinic receptors in rat sympathetic ganglia.大鼠交感神经节中的毒蕈碱受体。
Br J Pharmacol. 1980 Dec;70(4):577-92. doi: 10.1111/j.1476-5381.1980.tb09777.x.
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Cholinoreceptors in the isolated costo-uterine muscle of the rat.大鼠离体肋子宫肌中的胆碱能受体。
J Auton Pharmacol. 1987 Jun;7(2):165-74. doi: 10.1111/j.1474-8673.1987.tb00146.x.

本文引用的文献

7
Autonomic regulation of the airways.气道的自主调节
Annu Rev Med. 1984;35:451-67. doi: 10.1146/annurev.me.35.020184.002315.
8
The affinity and efficacy of onium salts on the frog rectus abdominis.鎓盐对青蛙腹直肌的亲和力和效能。
Br J Pharmacol Chemother. 1967 Sep;31(1):188-96. doi: 10.1111/j.1476-5381.1967.tb01989.x.
9
The significance of the age of onset of asthma.
Med J Aust. 1971 Jun 19;1(25):1317-9. doi: 10.5694/j.1326-5377.1971.tb88132.x.

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