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Superagonist information


Efficacy spectrum of receptor ligands.

In the field of pharmacology, 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 thus has an efficacy of more than 100%.[1][2] For example, goserelin is a superagonist of the gonadotropin-releasing hormone receptor.

  1. ^ Carlier PR, Chow ES, Barlow RL, Bloomquist JR (August 2002). "Discovery of non-zwitterionic GABAA receptor full agonists and a superagonist". Bioorg. Med. Chem. Lett. 12 (15): 1985–8. doi:10.1016/S0960-894X(02)00299-8. PMID 12113824.
  2. ^ Tan CM, Wilson MH, MacMillan LB, Kobilka BK, Limbird LE (September 2002). "Heterozygous α2A-adrenergic receptor mice unveil unique therapeutic benefits of partial agonists". Proc. Natl. Acad. Sci. U.S.A. 99 (19): 12471–6. Bibcode:2002PNAS...9912471T. doi:10.1073/pnas.122368499. PMC 129469. PMID 12205290.

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Superagonist

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In the field of pharmacology, a superagonist is a type of agonist that is capable of producing a maximal response greater than the endogenous agonist for...

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Sotio

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America, and Asia. The company has clinical programs which include a superagonist of the immuno-oncology target IL-15, a new generation of potent and stable...

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Agonist

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antagonist. An example is the cannabinoid inverse agonist rimonabant. A superagonist is a term used by some to identify a compound that is capable of producing...

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Deslorelin

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Suprelorin among others, is an injectable gonadotropin releasing hormone superagonist (GnRH agonist) which is used in veterinary medicine for various indications...

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IC50

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Excitatory Agonist Endogenous agonist Irreversible agonist Partial agonist Superagonist Physiological agonist...

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Trophogen

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bovine high affinity glycoprotein hormone and related growth factor superagonist analogs for human infertility and animal superovulation, as well as targeted...

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Nogapendekin alfa inbakicept

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Gonzalgo ML, Agarwal PK, Bassett JC, et al. (January 2023). "IL-15 Superagonist NAI in BCG-Unresponsive Non-Muscle-Invasive Bladder Cancer". NEJM Evidence...

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Ligand binding assay

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Excitatory Agonist Endogenous agonist Irreversible agonist Partial agonist Superagonist Physiological agonist...

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Interleukin 15

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decrease tumor growth mice. Currently there are two varieties of IL-15 superagonist available. One combines IL-15 and IL-15Rα-Fc (R&D Systems) in vitro to...

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Classical pharmacology

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Excitatory Agonist Endogenous agonist Irreversible agonist Partial agonist Superagonist Physiological agonist...

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Volume of distribution

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Excitatory Agonist Endogenous agonist Irreversible agonist Partial agonist Superagonist Physiological agonist...

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Pramipexole

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various sites Site Affinity (Ki, nM) Efficacy (Emax, %) Action D2S 3.3 130 Superagonist D2L 3.9 70 Partial agonist D3 0.5 70 Partial agonist D4 3.9 42 Partial...

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Immune checkpoint

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cells, prompts T cell expansion. CD28 was the target of the TGN1412 'superagonist' which caused severe inflammatory reactions in the first-in-man study...

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Isotonitazene

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Halberstadt A, Stucke A, McCorvy J (July 2023). "Mu-opioid receptor selective superagonists produce prolonged respiratory depression". iScience. 26 (7): 107121...

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CD28

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TeGenero, and unexpectedly caused multiple organ failure in trials, is a superagonist of CD28. Unfortunately, it is often ignored that the same receptors also...

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Feminizing hormone therapy

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goserelin (Zoladex), and buserelin (Suprefact), are GnRH receptor superagonists, and work by producing profound desensitization of the GnRH receptor...

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Intrinsic activity

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Ligand Description % Efficacy (E) Superagonist Efficacy higher than the endogenous agonist E > 100 Full agonist Efficacy equal to the endogenous agonist...

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Pharmacomicrobiomics

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Excitatory Agonist Endogenous agonist Irreversible agonist Partial agonist Superagonist Physiological agonist...

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Theralizumab

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requirements and signaling properties of T cell-activating, anti-CD28 antibody superagonists". The Journal of Experimental Medicine. 197 (8): 955–66. doi:10.1084/jem...

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Buserelin

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Buserelin is a GnRH agonist, or an agonist of the GnRH receptor. It is a superagonist of the GnRH receptor with potency for induction of luteinizing hormone...

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Reverse pharmacology

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Excitatory Agonist Endogenous agonist Irreversible agonist Partial agonist Superagonist Physiological agonist...

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Pharmacoepigenetics

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Excitatory Agonist Endogenous agonist Irreversible agonist Partial agonist Superagonist Physiological agonist...

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Cytokine delivery systems

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Marco, A. (2022). Efficacy of PEGylated ciliary neurotrophic factor superagonist variant in diet-induced obesity mice. PLOS One, 17(3), e0265749. Fernandez-Botran...

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Befiradol

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(October 2010). "Novel pyridylmethylamines as highly selective 5-HT(1A) superagonists". Journal of Medicinal Chemistry. 53 (19): 7167–7179. doi:10.1021/jm100835q...

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