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噻吗洛尔作用机制的实验研究

Experimental studies on the mechanism of action of timolol.

作者信息

Neufeld A H

出版信息

Surv Ophthalmol. 1979 May-Jun;23(6):363-70. doi: 10.1016/0039-6257(79)90229-7.

DOI:10.1016/0039-6257(79)90229-7
PMID:223248
Abstract

Timolol, which binds to beta-adrenergic receptors, is a potent antagonist of the catecholamine-stimulated synthesis of cyclic AMP. However, the actual mechanism of action by which timolol reduces intraocular pressure is not readily apparent. Compared to its efficacy in human eyes, the drug is relatively ineffective in rabbit eyes. A reasonable postulate is that soon after administration, timolol blocks endogenous adrenergic stimulation contributing to the formation of aqueous humor by the ciliary processes. Nevertheless, the long-lasting reduction of intraocular pressure persists at a time when the drug is no longer bound to beta-adrenergic receptors.

摘要

噻吗洛尔可与β-肾上腺素能受体结合,是儿茶酚胺刺激的环磷酸腺苷合成的强效拮抗剂。然而,噻吗洛尔降低眼压的实际作用机制尚不清楚。与在人眼中的疗效相比,该药物在兔眼中相对无效。一个合理的推测是,给药后不久,噻吗洛尔会阻断内源性肾上腺素能刺激,而这种刺激有助于睫状体产生房水。然而,当药物不再与β-肾上腺素能受体结合时,眼压仍会持续长时间降低。

相似文献

1
Experimental studies on the mechanism of action of timolol.噻吗洛尔作用机制的实验研究
Surv Ophthalmol. 1979 May-Jun;23(6):363-70. doi: 10.1016/0039-6257(79)90229-7.
2
The effects of topically applied epinephrine and timolol on intraocular pressure and aqueous humor cyclic-AMP in the rabbit.局部应用肾上腺素和噻吗洛尔对兔眼压及房水环磷酸腺苷的影响。
Exp Eye Res. 1981 Jun;32(6):681-90. doi: 10.1016/0014-4835(81)90017-8.
3
Effects of l- and d-timolol on cyclic AMP synthesis and intraocular pressure in water-loaded, albino and pigmented rabbits.
Invest Ophthalmol Vis Sci. 1983 Sep;24(9):1276-82.
4
Pharmacological effects of topical timolol in the rabbit eye.噻吗洛尔滴眼液对兔眼的药理作用。
Invest Ophthalmol Vis Sci. 1980 Oct;19(10):1189-97.
5
Laboratory and clinical studies on the mechanism of action of timolol.
Surv Ophthalmol. 1983 Dec;28 Suppl:286-92. doi: 10.1016/0039-6257(83)90152-2.
6
Acute effect of epinephrine on aqueous humor formation in the timolol-treated normal eye as measured by fluorophotometry.通过荧光光度法测量肾上腺素对噻吗洛尔治疗的正常眼房水生成的急性作用。
Invest Ophthalmol Vis Sci. 1980 Apr;19(4):420-3.
7
[Experimental studies with timolol: a new ocular hypotensive agent (author's transl)].噻吗洛尔的实验研究:一种新型降眼压药物(作者译)
J Fr Ophtalmol. 1978 Dec;1(12):717-21.
8
[Preliminary study of acidification of the pH of the aqueous humor in rats treated with timolol maleate].[马来酸噻吗洛尔治疗大鼠房水pH值酸化的初步研究]
Boll Soc Ital Biol Sper. 1980 Oct 30;56(20):2071-5.
9
Comparison of the effects of timolol and other adrenergic agents on intraocular pressure in the rabbit.噻吗洛尔与其他肾上腺素能药物对兔眼压影响的比较。
Invest Ophthalmol Vis Sci. 1977 Nov;16(11):987-96.
10
In vivo cAMP level in rabbit iris-ciliary body after topical epinephrine treatment.
Curr Eye Res. 1996 Oct;15(10):1025-32. doi: 10.3109/02713689609017651.

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bioRxiv. 2025 Jan 27:2025.01.24.634771. doi: 10.1101/2025.01.24.634771.
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Adrenoceptors in the Eye - Physiological and Pathophysiological Relevance.眼部肾上腺素能受体——生理与病理生理学相关性。
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β-Adrenoreceptors as Therapeutic Targets for Ocular Tumors and Other Eye Diseases-Historical Aspects and Nowadays Understanding.β-肾上腺素能受体作为眼部肿瘤和其他眼病的治疗靶点:历史方面和现今的认识。
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Discovery of Molecular Therapeutics for Glaucoma: Challenges, Successes, and Promising Directions.青光眼分子疗法的发现:挑战、成功与前景方向
J Med Chem. 2016 Feb 11;59(3):788-809. doi: 10.1021/acs.jmedchem.5b00828. Epub 2015 Sep 25.
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VAV2 and VAV3 as candidate disease genes for spontaneous glaucoma in mice and humans.VAV2 和 VAV3 作为小鼠和人类自发性青光眼的候选疾病基因。
PLoS One. 2010 Feb 4;5(2):e9050. doi: 10.1371/journal.pone.0009050.
7
Study of the additive effect of timolol and epinephrine in lowering intraocular pressure.噻吗洛尔与肾上腺素降眼压相加作用的研究
Br J Ophthalmol. 1981 Sep;65(9):596-602. doi: 10.1136/bjo.65.9.596.
8
[The effect of timolol and dipivalyl-epinephrine in the treatment of the elevated intraocular pressure (author's transl)].噻吗洛尔与二特戊酰肾上腺素治疗眼压升高的效果(作者译)
Albrecht Von Graefes Arch Klin Exp Ophthalmol. 1980;213(4):273-81. doi: 10.1007/BF00417550.
9
Beta adrenergic receptors in pigmented ciliary processes.色素性睫状突中的β肾上腺素能受体。
Br J Ophthalmol. 1982 Dec;66(12):788-92. doi: 10.1136/bjo.66.12.788.
10
Adrenergic regulation of intraocular pressure: identification of beta 2-adrenergic-stimulated adenylate cyclase in ciliary process epithelium.眼内压的肾上腺素能调节:睫状体上皮细胞中β2-肾上腺素能刺激的腺苷酸环化酶的鉴定。
Proc Natl Acad Sci U S A. 1980 Dec;77(12):7420-4. doi: 10.1073/pnas.77.12.7420.