User:Logan753/Inverse agonist
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[edit]Mechanisms of Action
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Like Agonists, inverse agonists have their own unique ways of inducing pharmacological and physiological responses depending on many factors, such as the type of inverse agonist, the type of receptor, mutants of receptors, binding affinities and whether the effects are exerted acutely or chronically based on receptor population density.[1] Because of this, they exhibit a spectrum of activity below the Intrinsic activity level.[1][2] Changes in constitutive activity of receptors affect response levels from ligands like inverse agonists.[3]
To illustrate, mechanistic models have been made for how inverse agonists induce their responses on G protein-coupled receptors (GPCRs). Many types of Inverse agonists for GPCRs have been shown to exhibit the following conventionally accepted mechanism.
Based on the Extended Ternary complex model, the mechanism contends that inverse agonists switch the receptor from an active state to an inactive state by undergoing conformational changes.[4] Under this model, current thinking is that the GPCRs can exist in a continuum of active and inactive states when no ligand is present.[4] Inverse agonists stabilize the inactive states, thereby suppressing agonist-independent activity.[4] However, the implementation of 'constitutively active mutants'[4] of GPCRs change their intrinsic activity.[1][2] Thus, the effect an inverse agonist has an a receptor depends on the the basal activity of the receptor, assuming the inverse agonist has the same binding affinity (as shown in the figure 2.
References
[edit]- ^ a b c Prather, Paul L. (2004-01-05). "Inverse agonists: tools to reveal ligand-specific conformations of G protein-coupled receptors". Science's STKE: signal transduction knowledge environment. 2004 (215): pe1. doi:10.1126/stke.2152004pe1. ISSN 1525-8882. PMID 14722344.
- ^ a b Hirayama, Shigeto; Fujii, Hideaki (2020). "δ Opioid Receptor Inverse Agonists and their In Vivo Pharmacological Effects". Current Topics in Medicinal Chemistry. 20 (31): 2889–2902. doi:10.2174/1568026620666200402115654. ISSN 1873-4294. PMID 32238139.
- ^ Berg, Kelly A.; Clarke, William P. (2018-10-01). "Making Sense of Pharmacology: Inverse Agonism and Functional Selectivity". The International Journal of Neuropsychopharmacology. 21 (10): 962–977. doi:10.1093/ijnp/pyy071. ISSN 1469-5111. PMC 6165953. PMID 30085126.
- ^ a b c d Strange, Philip G. (2002-02). "Mechanisms of inverse agonism at G-protein-coupled receptors". Trends in Pharmacological Sciences. 23 (2): 89–95. doi:10.1016/s0165-6147(02)01993-4. ISSN 0165-6147. PMID 11830266.
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