Not to be confused with Antagonist or Protagonist.
Dose response curves of a full agonist, partial agonist, neutral antagonist, and inverse agonist
In pharmacology, an inverse agonist is a drug that binds to the same receptor as an agonist but induces a pharmacological response opposite to that of the agonist.
A neutral antagonist has no activity in the absence of an agonist or inverse agonist but can block the activity of either;[1] they are in fact sometimes called blockers (examples include alpha blockers, beta blockers, and calcium channel blockers). Inverse agonists have opposite actions to those of agonists but the effects of both of these can be blocked by antagonists.[2]
A prerequisite for an inverse agonist response is that the receptor must have a constitutive (also known as intrinsic or basal) level of activity in the absence of any ligand.[3] An agonist increases the activity of a receptor above its basal level, whereas an inverse agonist decreases the activity below the basal level.
The efficacy of a full agonist is by definition 100%, a neutral antagonist has 0% efficacy, and an inverse agonist has < 0% (i.e., negative) efficacy.
^Kenakin T (April 2004). "Principles: receptor theory in pharmacology". Trends in Pharmacological Sciences. 25 (4): 186–92. doi:10.1016/j.tips.2004.02.012. PMID 15063082.
^Nutt D, Stahl S, Blier P, Drago F, Zohar J, Wilson S (January 2017). "Inverse agonists - What do they mean for psychiatry?". European Neuropsychopharmacology. 27 (1): 87–90. doi:10.1016/j.euroneuro.2016.11.013. hdl:10044/1/43624. PMID 27955830. S2CID 25113284.
^Berg, Kelly A; Clarke, William P (2018-08-06). "Making Sense of Pharmacology: Inverse Agonism and Functional Selectivity". International Journal of Neuropsychopharmacology. 21 (10): 962–977. doi:10.1093/ijnp/pyy071. ISSN 1461-1457. PMC 6165953. PMID 30085126.
an inverseagonist is a drug that binds to the same receptor as an agonist but induces a pharmacological response opposite to that of the agonist. A neutral...
antagonist blocks the action of the agonist, while an inverseagonist causes an action opposite to that of the agonist. From the Greek αγωνιστής (agōnistēs)...
binding will disrupt the interaction and inhibit the function of an agonist or inverseagonist at receptors. Antagonists mediate their effects by binding to...
antagonist or an inverseagonist at histamine receptors. Only a few currently marketed H1-antihistamines are known to function as inverseagonists. Histamine...
modulators are categorized in the Agonist, Partial Agonist, Selective Tissue Modulators, Antagonist, and InverseAgonist categories in terms of the effect...
histaminergic neurons by an inverseagonist of the histamine H3 receptor, which enhances histamine release in hypothalamus. An inverseagonist of the histamine H3...
prevents their activation by endocannabinoids. They include antagonists, inverseagonists, and antibodies of CBRs. The discovery of the endocannabinoid system...
Olanzapine, an atypical antipsychotic Buspirone, an anxiolytic FAUC F41: inverseagonist, subtype selectivity of more than 3 orders of magnitude over D2 and...
opioid receptors because their activation is not reversed by the opioid inverse-agonist naloxone, they do not exhibit high-affinity binding for classical opioids...
administration of receptor agonists may result in receptor internalization and/or a reduction in receptor protein signaling. The inverseagonist MK-9470 makes it...
modulating CB2 receptor activity by either selective CB2 receptor agonists or inverseagonists/antagonists depending on the disease and its progression holds...
A GABA receptor agonist is a drug that is an agonist for one or more of the GABA receptors, producing typically sedative effects, and may also cause other...
antagonist. It is approved as a generic medication. Pimavanserin acts as an inverseagonist and antagonist at serotonin 5-HT2A receptors with high binding affinity...
sympathomimetic activity of beta blockers Inverseagonist Mixed agonist/antagonist Calvey N, Williams N (2009). "Partial agonists". Principles and Practice of Pharmacology...
Desloratadine (trade names Clarinex and Aerius) is a tricyclic H1 inverseagonist that is used to treat allergies. It is an active metabolite of loratadine...
barbiturates. On the other hand, Naloxone has no partial agonist effects, and is in fact a partial inverseagonist at μ-opioid receptors, and so is the preferred...
nuclear receptors are known as inverseagonists. A number of drugs that work through nuclear receptors display an agonist response in some tissues and an...
are in fact partial agonists or inverseagonists, but with very low efficacy (less than 10%). Compounds considered partial agonists tend to have efficacy...
Global Information