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The beta-1 receptor is a G-protein-coupled receptor with the Gs alpha subunit as its main signaling protein. [4] The subunit dissociates from the receptor when activated, subsequently activating adenylyl cyclase to convert adenosine triphosphate (ATP) to cAMP, which is a secondary messenger mediating the pharmacological effects. [4]
Diltiazem, sold under the brand name Cardizem among others, is a nondihydropyridine calcium channel blocker medication used to treat high blood pressure, angina, and certain heart arrhythmias. [9] It may also be used in hyperthyroidism if beta blockers cannot be used. [ 9 ]
Reverse use dependence is relevant for potassium channel blockers used as class III antiarrhythmics. Reverse use dependent drugs that slow heart rate (such as quinidine) can be less effective at high heart rates. [11] The refractoriness of the ventricular myocyte increases at lower heart rates.
Adenosine A 2A receptor antagonists, including the non-selective antagonists like caffeine, show pro-motivational effects in animals, whereas selective adenosine A 1 receptor antagonists, like DPCPX and CPX, do not. [13] [89] Adenosine A 2A receptor antagonists appear to exert their pro-motivational effects in the nucleus accumbens core and can ...
Also known as P2Y12 receptor antagonists, they work by reversibly interacting with the P2Y12 receptor to inhibit the adenosine diphosphate (ADP) receptors on platelets, thus preventing the linkage of platelets by fibrinogen. [34] [35] ADP-induced platelet aggregation and activation are hence hindered.
Caffeine keeps you awake by blocking adenosine receptors. Each type of adenosine receptor has different functions, although with some overlap. [3] For instance, both A 1 receptors and A 2A play roles in the heart, regulating myocardial oxygen consumption and coronary blood flow, while the A 2A receptor also has broader anti-inflammatory effects throughout the body. [4]
ATP can be metabolised in cardiovascular tissues to pro-aggregatory ADP, AMP or adenosine. Replacement of anhydride oxygen between phosphorus β (Pβ) and phosphorus γ (Pγ) with di-Chloro or di-Fluoro-methylene leads to a compound that is equipotent to ATP and have a similar pKa. Because of this replacement the metabolism of ATP to pro ...
Via indirect action, it leads to an increase in acetylcholine production, stimulating M2 receptors on AV node leading to an overall decrease in speed of conduction. Magnesium sulfate is an antiarrhythmic drug, but only used against very specific arrhythmias [ 14 ] such as torsades de pointes .