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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).
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.
An adrenergic agonist is a drug that stimulates a response from the adrenergic receptors. The five main categories of adrenergic receptors are: α 1, α 2, β 1, β 2, and β 3, although there are more subtypes, and agonists vary in specificity between these receptors, and may be classified respectively. However, there are also other mechanisms ...
Diproqualone has sedative, anxiolytic, antihistamine, and analgesic properties, resulting from its agonist activity at the β subtype of the GABA a receptor, antagonist activity at all histamine receptors, inhibition of the cyclooxygenase-1 enzyme, and possibly its agonist activity at both the Sigma-1 receptor and Sigma-2 receptor.
Orthosteric agonist (A) binds to orthosteric site (B) of a receptor (E). Allosteric modulator (C) binds to allosteric site (D). Modulator increases/lowers the affinity (1) and/or efficacy (2) of an agonist. Modulator may also act as an agonist and yield an agonistic effect (3). Modulated orthosteric agonist affects the receptor (4).
Since ergot-dopamine agonist have antihypertensive qualities it is wise to monitor blood pressure when using dopamine agonists with antihypertensive drugs to ensure that the patient does not get hypotension. That includes the drug sildenafil which is commonly used to treat erectile dysfunction but also used for pulmonary hypertension. [21]
In an essay for 'Women's Health,' Dr. Nora Volkow discusses the future of semaglutide weight-loss meds, and their potential to treat substance use disorder.
Beta 2-adrenergic agonists, also known as adrenergic β 2 receptor agonists, are a class of drugs that act on the β 2 adrenergic receptor. Like other β adrenergic agonists , they cause smooth muscle relaxation. β 2 adrenergic agonists' effects on smooth muscle cause dilation of bronchial passages , vasodilation in muscle and liver ...