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An adenosine reuptake inhibitor (AdoRI) is a type of drug which acts as a reuptake inhibitor for the purine nucleoside and neurotransmitter adenosine by blocking the action of one or more of the equilibrative nucleoside transporters (ENTs).
Caffeine's stimulatory effects are credited primarily (although not entirely) to its capacity to block adenosine receptors, thereby reducing the inhibitory tonus of adenosine in the CNS. This reduction in adenosine activity leads to increased activity of the neurotransmitters dopamine and glutamate . [ 35 ]
Based on the knowledge of thienopyridine's chemistry a significant number of derivatives of thienopyridines were synthesized. The derivatives were tested in-vivo and ex-vivo in mice and rats but the results of the tests didn't demonstrate any anti-inflammatory or analgesic effects at all but instead they displayed unexpected antiplatelet and ...
It also causes a negative dromotropic effect through the inhibition of AV-nodal conduction. [20] From the 1980s onwards, these effects of adenosine have been used in the treatment of patients with supraventricular tachycardia. [21] The regulation of vascular tone in the endothelium of blood vessels is mediated by purinergic signalling.
Adenosinergic means "working on adenosine". An adenosinergic agent (or drug) is a chemical which functions to directly modulate the adenosine system in the body or brain. Examples include adenosine receptor agonists, adenosine receptor antagonists (such as caffeine), and adenosine reuptake inhibitors.
Adenosine is a neuromodulator that is responsible for motor function, mood, memory, and learning. Its main purpose is the coordination of responses to different neurotransmitters. [5] Adenosine plays many important roles in biological systems, for example in the central nervous-, cardiovascular-, hepatic-, renal- and respiratory system.
Abundant extracellular adenosine can then bind to the A2A receptor resulting in a G s-protein coupled response, resulting in the accumulation of intracellular cAMP, which functions primarily through protein kinase A to upregulate inhibitory cytokines such as transforming growth factor-beta (TGF-β) and inhibitory receptors (i.e., PD-1). [56]
An adenosine receptor antagonist is a drug which acts as an antagonist of one or more of the adenosine receptors. [1] The best known are xanthines and their derivatives (natural: caffeine, [2] theophylline, [3] and theobromine; and synthetic: PSB-1901 [4]), but there are also non-xanthine representatives (e.g. ISAM-140, [5] ISAM-R316, [6] etrumadenant, [7] and AZD-4635 [8])