Burger's Medicinal Chemistry and Drug Discovery, by Donald A. Abraham

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By Donald A. Abraham

His is quantity three: Cardiovascular brokers and Endocrines, of Burger's Medicinal Chemistry and Drug Discovery, sixth variation. This new quantity comprises severe new chapters on Endogenous Vasoactive Peptides, Iron Chelators and healing makes use of, and basics of Steroid Chemistry and Biochemistry.

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Extra info for Burger's Medicinal Chemistry and Drug Discovery, Cardiovascular Agents and Endocrines, Edition: Sixth Edition

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3): Cilnidipine is a unique calcium antagonist that has both L-type and N-type voltage-dependent calcium channel blocking activity (125-129). Cilnidipine is under investigation for the treatment of hypertension in Europe. Recently, cilnidipine, its analogs, and other dihydropyridine derivatives were evaluated for their state dependent inhibition of L-type Ca2+channels, and revealed that structurally related DHPs act in distinct ways to inhibit the L-type channel in the resting, open, and inactivated states.

A list of compounds in the class, along with uses and side effects are shown in With the exception of sotalol (2321, the compounds in this class are all structurally similar agents known as aryloxypropanolamines (Fig. 14). This name originates from the presence of an --OCH,- group located between a substituted benzene ring and an ethylamino side-chain. The aromatic ring and substituents are the primary determinants . Substitution of the para position of the benzene ring, in tandem with the absence of meta position substitution, seems to confer selectivity for p l cardiac receptors.

Such drugs include propranolol (Inderal), a and P blockers labetalol (Normdyne, Trandate), acebutolol (Sectral), atenolol (Tenormin), metopro101 (Toprol), and bisoprolol (Zebeta). These drugs are equally effective as calcium channel blockers and have fewer adverse effects. 7 Glycoprotein Ilb/llla Receptor Antagonists. These compounds are also called blood thinners because they block platelet activity. These drugs are very beneficial for many patients with angina and do not seem to pose an increased risk for stroke, including strokes caused by bleeding.

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