Chemistry:Cicloprolol
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Cicloprolol (INN; developmental code name SL-75177), or cycloprolol (BAN), is a β-adrenergic receptor antagonist (beta blocker) described as an antihypertensive agent which was never marketed.[1][2][3][4][5] It has weak partial agonist or intrinsic sympathomimetic activity (30%) at the β-adrenergic receptors.[4][2] This is higher than that of many other beta blockers but is lower than that of xamoterol (45%).[4] The drug is selective for the β1-adrenergic receptor.[3] It has been studied in the treatment of heart failure.[3]
Chemistry
The chemical structure of cicloprolol is very similar to that of betaxolol.
Synthesis
Cicloprolol can be synthesized starting from 4-benzyloxyphenol.[6][7]
References
- ↑ The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer US. 2014. p. 272. ISBN 978-1-4757-2085-3. https://books.google.com/books?id=0vXTBwAAQBAJ&pg=PA272. Retrieved 29 August 2024.
- ↑ 2.0 2.1 Concise Dictionary of Pharmacological Agents: Properties and Synonyms. Springer Netherlands. 2012. p. 88. ISBN 978-94-011-4439-1. https://books.google.com/books?id=tsjrCAAAQBAJ&pg=PA88. Retrieved 2024-08-29.
- ↑ 3.0 3.1 3.2 "Beta receptor antagonists in the treatment of heart failure". Cardiovascular Drugs and Therapy 5 (3): 589–604. June 1991. doi:10.1007/BF03029728. PMID 1678962.
- ↑ 4.0 4.1 4.2 "Beta-adrenoceptor partial agonists: a renaissance in cardiovascular therapy?". British Journal of Clinical Pharmacology 30 (2): 157–171. August 1990. doi:10.1111/j.1365-2125.1990.tb03760.x. PMID 1976342.
- ↑ "An evaluation of the safety of the beta-modulator cicloprolol in chronic heart failure". Clinical Cardiology 15 (1): 38–42. January 1992. doi:10.1002/clc.4960150109. PMID 1347258.
- ↑ Manoury PM, Cavero IA, Majer H, Giudicelli DP, "Phenoläther, Verfahren zu ihrer Herstellung und sie enthaltende Arzneimttel [Phenol ethers, processes for their preparation and medicinal products containing them]", DE patent 2649605, published 1977-05-18
- ↑ P. M. J. Manouri, I. A. G. Carero, H. Majer, and P. R. L. Giudicelli, (1977) Chem. Abstr., 87:134,543j (1977). eidem U.S. Patent 4,311,708
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