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Endogenous agonist information


In pharmacology, an endogenous agonist for a particular receptor is a compound naturally produced by the body which binds to and activates that receptor. For example, the primary endogenous agonist for serotonin receptors is serotonin, and the primary endogenous agonist for dopamine receptors is dopamine.[1]

In general, receptors for small molecule neurotransmitters such as serotonin will have only one endogenous agonist, but often have many different receptor subtypes (e.g. 13 different receptors for serotonin). On the other hand, neuropeptide receptors tend to have fewer subtypes, but may have several different endogenous agonists. This allows for a high degree of complexity in the body's signalling system, with different tissues often showing quite distinct responses to a particular ligand. Some endogenous antagonists and inverse agonists are also known (e.g., kynurenic acid at the NMDA receptor), but these are much less common.

  1. ^ Goodman and Gilman's Manual of Pharmacology and Therapeutics. (11th edition, 2008). p14. ISBN 0-07-144343-6

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Endogenous agonist

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In pharmacology, an endogenous agonist for a particular receptor is a compound naturally produced by the body which binds to and activates that receptor...

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Agonist

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example, the endogenous agonist for serotonin receptors is serotonin, and the endogenous agonist for dopamine receptors is dopamine. Full agonists bind to...

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Partial agonist

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Clinically, partial agonists can be used to activate receptors to give a desired submaximal response when inadequate amounts of the endogenous ligand are present...

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Allosteric modulator

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the same one to which an endogenous agonist of the receptor would bind (i.e., an orthosteric site). Modulators and agonists can both be called receptor...

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Opioid

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Dezocine—agonist/antagonist Pentazocine—agonist/antagonist Phenazocine Buprenorphine—partial agonist Dihydroetorphine Etorphine Butorphanol—agonist/antagonist...

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Cannabinoid

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Shalev DE, et al. (March 2001). "2-arachidonyl glyceryl ether, an endogenous agonist of the cannabinoid CB1 receptor". Proceedings of the National Academy...

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Opioid peptide

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the highest potency endogenous ligand ... Morphine occurs endogenously (Poeaknapo et. al. 2004) ... Principal endogenous agonists (Human) [are] β-endorphin...

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Cannabinoid receptor 1

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by the phytocannabinoid tetrahydrocannabivarin (THCV). The primary endogenous agonist of the human CB1 receptor is anandamide. The CB1 receptor shares the...

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Inverse agonist

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which inverse agonists have been identified include the GABAA, melanocortin, mu opioid, histamine and beta adrenergic receptors. Both endogenous and exogenous...

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Nicotinic agonist

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nicotine. Examples include nicotine (by definition), acetylcholine (the endogenous agonist of nAChRs), choline, epibatidine, lobeline, varenicline and cytisine...

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Serotonin receptor agonist

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A serotonin receptor agonist is an agonist of one or more serotonin receptors. They activate serotonin receptors in a manner similar to that of serotonin...

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Sympathomimetic drug

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adrenergic amines) are stimulant compounds which mimic the effects of endogenous agonists of the sympathetic nervous system. Examples of sympathomimetic effects...

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NMDA receptor

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(quinolinate) – endogenous glutamate site agonist Glycine – endogenous glycine site agonist Alanine (D-alanine, L-alanine) – endogenous glycine site agonist Milacemide...

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Adrenergic agonist

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adrenergic agonism. Epinephrine and norepinephrine are endogenous and broad-spectrum. More selective agonists are more useful in pharmacology. An adrenergic agent...

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Superagonist

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a superagonist is a type of agonist that is capable of producing a maximal response greater than the endogenous agonist for the target receptor, and...

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Intrinsic activity

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the way in which agonists vary in the response they produce, even when they occupy the same number of receptors. High efficacy agonists can produce the...

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Melanocortin receptor

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by endogenous inverse agonists agouti signalling peptide and agouti-related peptide, and activated by synthetic (i.e. afamelanotide) and endogenous agonist...

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Lactic acid

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addition to other biological roles, L-lactic acid is the primary endogenous agonist of hydroxycarboxylic acid receptor 1 (HCA1), which is a Gi/o-coupled...

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Ibutamoren

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non-peptide agonist of the ghrelin receptor and a growth hormone secretagogue, mimicking the growth hormone (GH)-stimulating action of the endogenous hormone...

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Sigma receptor

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neurosteroid steroid hormone DHEA is an agonist at sigma receptors and along with pregnenolone could be endogenous agonist ligands; opposed by sigma antagonistic...

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Dopamine receptor D3

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dopamine agonist) Bromocriptine (non-selective dopamine agonist) Captodiame CJ-1639 compound R,R-16: 250x binding selectivity over D2 Dopamine (endogenous agonist)...

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Nociceptin receptor

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Unlike MOP agonists such as codeine and morphine, NOP agonists do not have reinforcing effects. Nociceptin is thought to be an endogenous antagonist of...

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IC50

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higher concentration of inhibitor leads to lowered agonist activity. IC50 value increases as agonist concentration increases. Furthermore, depending on...

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Indirect agonist

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agonist or indirect-acting agonist is a substance that enhances the release or action of an endogenous neurotransmitter but has no specific agonist activity...

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Dynorphin A

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"Cryo-EM structure of human κ-opioid receptor-Gi complex bound to an endogenous agonist dynorphin A". Protein & Cell. 14 (6): 464–468. doi:10.1093/procel/pwac033...

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PPAR agonist

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targets of a number of marketed drugs. The main classes of PPAR agonists are: An endogenous compound, 7(S)-Hydroxydocosahexaenoic Acid (7(S)-HDHA), which...

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Vascular smooth muscle

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are: alpha-1, alpha-2 and beta-2 adrenergic receptors|. The main endogenous agonist of these cell receptors is norepinephrine (NE). The adrenergic receptors...

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