Substance that binds to and regulates the activity of chemical receptors
A receptor modulator, or receptor ligand, is a general term for a substance, endogenous or exogenous, that binds to and regulates the activity of chemical receptors. They are ligands that can act on different parts of receptors and regulate activity in a positive, negative, or neutral direction with varying degrees of efficacy. Categories of these modulators include receptor agonists and receptor antagonists, as well as receptor partial agonists, inverse agonists, orthosteric modulators, and allosteric modulators,[1] Examples of receptor modulators in modern medicine include CFTR modulators,[2] selective androgen receptor modulators (SARMs), and muscarinic ACh receptor modulators.
^van Westen GJ, Gaulton A, Overington JP (April 2014). "Chemical, target, and bioactive properties of allosteric modulation". PLOS Computational Biology. 10 (4): e1003559. Bibcode:2014PLSCB..10E3559V. doi:10.1371/journal.pcbi.1003559. PMC 3974644. PMID 24699297.
A receptormodulator, or receptor ligand, is a general term for a substance, endogenous or exogenous, that binds to and regulates the activity of chemical...
Selective androgen receptormodulators (SARMs) are a class of drugs that selectively activate the androgen receptor in specific tissues, promoting muscle...
that an allosteric modulator binds to (i.e., an allosteric site) is not the same one to which an endogenous agonist of the receptor would bind (i.e., an...
A selective progesterone receptormodulator (SPRM) is an agent that acts on the progesterone receptor (PR), the biological target of progestogens like...
estrogen receptors (ERα and ERβ), which are members of the nuclear receptor family of intracellular receptors, and membrane estrogen receptors (mERs) (GPER...
S-22, is a selective androgen receptormodulator (SARM) which is under development for the treatment of androgen receptor-positive breast cancer in women...
pharmacology, GABAA receptor positive allosteric modulators, also known as GABAkines or GABAA receptor potentiators, are positive allosteric modulator (PAM) molecules...
black-market name Testolone or Testalone, is a selective androgen receptormodulator (SARM) which is under development for the treatment of hormone-sensitive...
anabolic effects of S-40503, a novel nonsteroidal selective androgen receptormodulator (SARM), in rat models of osteoporosis". Biol. Pharm. Bull. 26 (11):...
A serotonin modulator and stimulator (SMS), sometimes referred to more simply as a serotonin modulator, is a type of drug with a multimodal action specific...
on the subunit composition of the GABA-A receptor, it can be characterized as a mixed GABA-A receptormodulator. The methaqualone binding site is distinct...
cause or who are pregnant. Clomifene is in the selective estrogen receptormodulator (SERM) family of medication and is a nonsteroidal medication. It works...
array of nuclear and cell surface receptors, and acting as a neurosteroid and modulator of neurotrophic factor receptors. In the United States, DHEA is sold...
VK5211 and by the black-market name Ligandrol, is a selective androgen receptormodulator (SARM) which is under development for the treatment of muscle atrophy...
NMDA receptormodulators (glutamate modulators) are a new form of antipsychotic that are in Phase II FDA studies. The first compound studied was glycine...
anti-convulsant stiripentol acts directly on the GABA(A) receptor as a positive allosteric modulator". Neuropharmacology. 56 (1): 190–197. doi:10.1016/j.neuropharm...
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