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[21] [22] Perforation of the phagosome membrane mediated by ESX1 secretion system allows extracellular mycobacterial DNA to access host cytosolic DNA sensors, thus inducing the production of type I interferon in macrophages. High type I interferon signature leads to the M. tuberculosis pathogenesis and prolonged infection. [22]
A co-agonist works with other co-agonists to produce the desired effect together. NMDA receptor activation requires the binding of both glutamate, glycine and D-serine co-agonists. Calcium can also act as a co-agonist at the IP3 receptor. A selective agonist is selective for a specific type of receptor. E.g.
PIEZO1 functions as a non-selective cation channel capable of conducting both monovalent and divalent cations, including Na+, K+, and Ca2+. The mechanosensitivity of PIEZO1 is a defining characteristic. It can be directly activated by membrane tension, with the peripheral blade and beam structures likely acting as mechanotransduction modules.
The name "NMDA receptor" is derived from the ligand N-methyl-D-aspartate (NMDA), which acts as a selective agonist at these receptors. When the NMDA receptor is activated by the binding of two co-agonists, the cation channel opens, allowing Na + and Ca 2+ to flow into the cell, in turn raising the cell's electric potential. Thus, the NMDA ...
Partial agonists do not activate receptors with maximal efficacy, even with maximal binding, causing partial responses compared to those of full agonists (efficacy between 0 and 100%). Antagonists bind to receptors but do not activate them. This results in a receptor blockade, inhibiting the binding of agonists and inverse agonists.
Measuring changes in threshold can indicate changes in membrane potential, axonal properties, and/or the integrity of the myelin sheath. Threshold tracking allows for the strength of a test stimulus to be adjusted by a computer in order to activate a defined fraction of the maximal nerve or muscle potential.
In the example shown to the right, two different ligands bind to the same receptor binding site. Only one of the agonists shown can maximally stimulate the receptor and, thus, can be defined as a full agonist. An agonist that can only partially activate the physiological response is called a partial agonist.
Agonist vs. antagonist. In pharmacology the term agonist-antagonist or mixed agonist/antagonist is used to refer to a drug which under some conditions behaves as an agonist (a substance that fully activates the receptor that it binds to) while under other conditions, behaves as an antagonist (a substance that binds to a receptor but does not activate and can block the activity of other agonists).