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Potassium channel activators blockers

Cromakalim (137) is a potassium channel activator commonly used as an antihypertensive agent (107). The rationale for the design of cromakalim is based on P-blockers such as propranolol (115) and atenolol (123). Conformational restriction of the propanolamine side chain as observed in the cromakalim chroman nucleus provides compounds with desired antihypertensive activity free of the side effects commonly associated with P-blockers. Enantiomerically pure cromakalim is produced by resolution of the diastereomeric (T)-a-meth5lben2ylcarbamate derivatives. X-ray crystallographic analysis of this diastereomer provides the absolute stereochemistry of cromakalim. Biological activity resides primarily in the (—)-(33, 4R)-enantiomer [94535-50-9] (137) (108). In spontaneously hypertensive rats, the (—)-(33, 4R)-enantiomer, at dosages of 0.3 mg/kg, lowers the systoHc pressure 47%, whereas the (+)-(3R,43)-enantiomer only decreases the systoHc pressure by 14% at a dose of 3.0 mg/kg. [Pg.253]

Antihypertensive Agents. Hypertension (high blood pressure) is a significant risk factor for cardiovascular diseases such as angina heart attacks, and strokes. /(-Adrenoceptor (adrenergic nervous system receptors of the /(-type) antagonists (/(-blockers), calcium channel blockers, angiotensinconverting enzyme (ACE) inhibitors, and potassium channel activators... [Pg.1267]

The pharmacological treatment options for ACS include agents that either reduce oxygen demand (beta blockers) or increase oxygen supply (nitrates, potassium channel activators, calcium channel blockers) to the heart and antiplatelet (aspirin, ADP-receptor antagonists, GPIIb/llla receptor blockers) and antithrombin therapy (unfractionated heparin, low molecular weight heparin, direct thrombin inhibitors) (10). [Pg.119]

BETA-BLOCKERS POTASSIUM CHANNEL ACTIVATORS t hypotensive effect Additive effect Monitor BP at least weekly until stable... [Pg.76]

IL-2 BETA-BLOCKERS, CALCIUM CHANNEL BLOCKERS, DIURETICS, NITRATES, POTASSIUM CHANNEL ACTIVATORS t hypotensive effect Additive hypotensive effect may be used therapeutically. Aldesleukin causes 1 vascular resistance and t capillary permeability Monitor BP at least weekly until stable. Warn patients to report symptoms of hypotension (light-headedness, dizziness on standing, etc.)... [Pg.376]

The CALCIUM-CHANNEL BLOCKERS, e.g. diltiazem, nimodipine and verapamil, act to block a subset of voltage-sensitive calcium channels, so reducing Ca -influx into smooth muscle cells. The potassium-channel activators. e.g. cromakalim, diazoxide, minoxidil, nicorandil and pinacidil, are thought to work by opening a subset of K -channels which leads to membrane stabilization. [Pg.288]

These drugs include nitrates, potassium channel activators, P-blockers and calcium channel blockers. [Pg.58]

Ischaemic heart disease can be treated with nitrates, potassium channel activators, P-blockers and calcium channel blockers. All these drugs either improve the blood supply to the myocardium or reduce its metabolic demand for oxygen, or both. Beta blockers are also useful in treating hypertensive patients who do not respond adequately to other antihypertensive drugs, and some types of arrhythmia because they slow the heart rate. [Pg.79]

CALCIUM CHANNEL BLOCKERS 9. DIURETICS 10. NITRATES 11. PERIPHERAL VASODILATORS-moxisylyte (thymoxamine) 12. POTASSIUM CHANNEL ACTIVATORS... [Pg.566]

Peukert S, Brendel J, Pirard B, Briiggemann A, Below P, Kleemann HW, Hem-merle H, Schmidt W. Identification, synthesis, and activity of novel blockers of the voltage-gated potassium channel Kvl.5. J Med Chem 2003 46 486-98. [Pg.422]

The Vaughan-Williams classification of antiarrhythmic drugs has been criticized for a number of reasons. The classification is based on the effects of drugs on normal, rather than diseased, myocardium. In addition, many of the drugs may be placed into more than one class. For example, the class IA drugs prolong repolarization/refractoriness, either via the parent drug8,9 or an active metabolite,10 and therefore also maybe placed in class III. Sotalol is also a 3-blocker, and therefore fits into class II. Amiodarone inhibits sodium and potassium channels, is a non-competitive inhibitor of 3-receptors, and inhibits calcium... [Pg.111]

Crossley R, Opalko A. (1996) The structure-activity relationships of potassium channel Blockers, in JM Evans, et al. (eds). Potassium Channels and their Modulators, Taylor and Francis. [Pg.108]

Ibutilide Potassium channel blocker, may activate inward current IV use for conversion in atrial flutter and fibrillation... [Pg.296]

See other pages where Potassium channel activators blockers is mentioned: [Pg.250]    [Pg.1268]    [Pg.109]    [Pg.135]    [Pg.261]    [Pg.2505]    [Pg.31]    [Pg.208]    [Pg.209]    [Pg.222]    [Pg.348]    [Pg.212]    [Pg.79]    [Pg.220]    [Pg.186]    [Pg.348]    [Pg.878]    [Pg.96]    [Pg.140]    [Pg.298]    [Pg.657]    [Pg.406]    [Pg.408]    [Pg.17]    [Pg.13]    [Pg.77]    [Pg.86]    [Pg.37]    [Pg.329]    [Pg.312]    [Pg.283]    [Pg.67]   
See also in sourсe #XX -- [ Pg.425 ]



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