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Intrinsic activity information


Efficacy spectrum of receptor ligands.

Intrinsic activity (IA) and efficacy refer to the relative ability of a drug-receptor complex to produce a maximum functional response. This must be distinguished from the affinity, which is a measure of the ability of the drug to bind to its molecular target, and the EC50, which is a measure of the potency of the drug and which is proportional to both efficacy and affinity. This use of the word "efficacy" was introduced by Stephenson (1956)[1] to describe 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 maximal response of the receptor system while occupying a relatively low proportion of the receptors in that system. There is a distinction between efficacy and intrinsic activity.[clarification needed]

  1. ^ Stephenson RP (December 1956). "A modification of receptor theory". British Journal of Pharmacology and Chemotherapy. 11 (4): 379–393. doi:10.1111/j.1476-5381.1956.tb00006.x. PMC 1510558. PMID 13383117.

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Intrinsic activity

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Intrinsic activity (IA) and efficacy refer to the relative ability of a drug-receptor complex to produce a maximum functional response. This must be distinguished...

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Inverse agonist

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constitutive (also known as intrinsic or basal) level of activity in the absence of any ligand. An agonist increases the activity of a receptor above its...

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Aripiprazole

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partial agonist (with an intrinsic activity of ~25%) as being similar to a full agonist but at a reduced level of activity presents a misleading oversimplification...

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Agonist

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response curve Excitatory postsynaptic potential Functional selectivity Intrinsic activity Inverse agonist Mixed agonist/antagonist Receptor antagonist Receptor...

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IC50

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effect of different concentrations of antagonist on reversing agonist activity. IC50 values can be calculated for a given antagonist by determining the...

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Brexpiprazole

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where aripiprazole has an intrinsic activity or agonist effect at the D2 receptor of 60%+, brexpiprazole has an intrinsic activity at the same receptor of...

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Drug action

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a response are: Intrinsic Activity which defines: Agonists as having Intrinsic Activity = 1 Antagonists as having Intrinsic Activity = 0 and, Partial...

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Cefditoren

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for cephalosporin resistance when mutated. Cefditoren pivoxil high intrinsic activity against Streptococcus pneumoniae, including penicillin-resistant strains...

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Motivation

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between intrinsic and extrinsic motivation as a spectrum rather than a clear dichotomy. This is linked to the idea that the more autonomous an activity is...

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Volume of distribution

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Metrics Efficacy Intrinsic activity Potency (EC50, IC50, ED50, LD50, TD50) Therapeutic index Affinity...

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Myometrium

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rhythmic oscillations, which have been termed slow waves, and reflect intrinsic activity of slow wave potentials. These slow waves are caused by changes in...

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Receptor antagonist

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Silent antagonists are competitive receptor antagonists that have zero intrinsic activity for activating a receptor. They are true antagonists, so to speak...

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Dystonia

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dystonias. The Na+ -K+ pump has been shown to control and set the intrinsic activity mode of cerebellar Purkinje neurons. This suggests that the pump might...

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Efficacy

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from an applied or dosed agent, for instance, a small molecule drug. Intrinsic activity is a relative term for a drug's efficacy relative to a drug with the...

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Intrinsic safety

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Intrinsic safety (IS) is a protection technique for safe operation of electrical equipment in hazardous areas by limiting the energy, electrical and thermal...

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Dopamine receptor D1

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receptors versus the D2-like family. Some of the benzazepines have high intrinsic activity whereas others do not. In 2015 the first positive allosteric modulator...

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Pharmacodynamics

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capacity of an agonist (in some receptor models it is termed intrinsic efficacy or intrinsic activity) and of the signal amplification capacity of the corresponding...

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Uterine contraction

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rhythmic oscillations, which have been termed slow waves, and reflect intrinsic activity of slow wave potentials. These slow waves are caused by changes in...

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Neural oscillation

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alpha activity. Neural oscillations in humans were observed by researchers as early as 1924 (by Hans Berger). More than 50 years later, intrinsic oscillatory...

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Beta blocker

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α1-blocking activity) Nadolol Oxprenolol (has intrinsic sympathomimetic activity) Penbutolol (has intrinsic sympathomimetic activity) Pindolol (has intrinsic sympathomimetic...

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Desmethylclozapine

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atypical antipsychotic drug clozapine. Unlike clozapine, it possesses intrinsic activity at the D2/D3 receptors, and acts as a weak partial agonist at these...

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Diprenorphine

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agonism of the KOR, where it appears to possess significantly greater intrinsic activity relative to the MOR, diprenorphine can produce sedation as well as...

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Emax

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Kowloonbay International Trade & Exhibition Centre Maximal efficacy, or intrinsic activity IPS E.max, a type of lithium disilicate glass-ceramic used in dental...

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