function as psychoactive drugs. The site that an allosteric modulator binds to (i.e., an allosteric site) is not the same one to which an endogenous agonist...

In the fields of biochemistry and pharmacology an allosteric regulator (or allosteric modulator) is a substance that binds to a site on an enzyme or receptor...

receptor positive allosteric modulators, also known as GABAkines or GABAA receptor potentiators, are positive allosteric modulator (PAM) molecules that...

Positive allosteric modulators Cerebrosterol – endogenous weak positive allosteric modulator Cholesterol – endogenous weak positive allosteric modulator...

Marampon F, Maggio R, Scarselli M (June 2017). "The First Negative Allosteric Modulator for Dopamine D2 and D3 Receptors, SB269652 May Lead to a New Generation...

"Neuropeptide oxytocin enhances μ opioid receptor signaling as a positive allosteric modulator". J Pharmacol Sci. 137 (1): 67–75. doi:10.1016/j.jphs.2018.04.002...

Clark PJ, Paparoidamis N, et al. (2019). "Identification of a Novel Allosteric Modulator of the Human Dopamine Transporter". ACS Chem Neurosci. 10 (8): 3718–3730...

positive allosteric modulator NLX-101 (F-15599) – serotonin 5-HT1A receptor full agonist PSIL-001 (DMT analogue) – serotonin 5-HT1 receptor modulator (non-hallucinogenic)...

2007). "Nootropic alpha7 nicotinic receptor allosteric modulator derived from GABAA receptor modulators". Proceedings of the National Academy of Sciences...

negative allosteric modulator 3α,5α-Androstanediol (3α-androstanediol): 5α-androstane-3α,17β-diol – GABAA receptor positive allosteric modulator 3α,5β-Androstanediol...

A GABAA receptor negative allosteric modulator is a negative allosteric modulator (NAM), or inhibitor, of the GABAA receptor, a ligand-gated ion channel...

Allosteric enzymes are enzymes that change their conformational ensemble upon binding of an effector (allosteric modulator) which results in an apparent...

AMPA receptor positive allosteric modulators are positive allosteric modulators (PAMs) of the AMPA receptor (AMPR), a type of ionotropic glutamate receptor...

with the SBP is a requirement for allosteric pharmacology. The compound SB269652 is a negative allosteric modulator of the D2R. It was observed that D2R...

(CPPHA) acts through a novel site as a positive allosteric modulator of group 1 metabotropic glutamate receptors". Molecular Pharmacology...

anti-addictive efficacy. BMS-986187 – also a δ-opioid receptor (DOR) positive allosteric modulator KOR agonists have been investigated for their therapeutic potential...

drugs to treat obesity, and more besides. Channel modulator Enzyme modulator Transporter modulator van Westen GJ, Gaulton A, Overington JP (April 2014)...

PMID 11641424. Adams CL, Lawrence AJ (2007). "CGP7930: a positive allosteric modulator of the GABAB receptor". CNS Drug Reviews. 13 (3): 308–16. doi:10...

Miyano K, Hirokawa T, Uezono Y (August 2016). "Ignavine: a novel allosteric modulator of the μ opioid receptor". Sci Rep. 6: 31748. Bibcode:2016NatSR....

composition of the AMPAR is also important for the way this receptor is modulated. If an AMPAR lacks GluA2 subunits, then it is susceptible to being blocked...

a norepinephrine–dopamine reuptake inhibitor (NDRI) and negative allosteric modulator of several nicotinic acetylcholine receptors. Bupropion does not...

receptors and neurotransmitter transporters. Methaqualone is a positive allosteric modulator at many subtypes of GABA-A receptor, similar to classical benzodiazepines...

loss of consciousness. It is a neurosteroid and acts as a positive allosteric modulator of the GABAA receptor, the major biological target of the inhibitory...

reuptake inhibitor and nicotinic acetylcholine receptor negative allosteric modulator. Bupropion is also a potent inhibitor of CYP2D6, and thereby inhibits...

NCT04051801 for "Multiple Ascending Dose Phase I Study of the M1 Positive Allosteric Modulator VU0467319" at ClinicalTrials.gov Smith DL, Davoren JE, Edgerton JR...

receptors, including acting as a positive allosteric modulator of the NMDA receptor, as a negative allosteric modulator of the GABAA receptor, and as an agonist...

oxytocin receptor agonism, oxytocin has been found to act as a positive allosteric modulator (PAM) of the μ- and κ-opioid receptors and this may be involved in...

subtype-selective PAM, intrinsic allosteric agonist activity, robust in-vivo activity PHCCC: PAM of mGluR4, negative allosteric modulator of mGluR1, direct agonist...

effects of the selective M4 muscarinic acetylcholine receptor positive allosteric modulator VU0152100". Neuropsychopharmacology. 39 (7): 1578–93. doi:10.1038/npp...

sigma σ1 receptor agonist, nicotinic acetylcholine receptor negative allosteric modulator, dopaminergic agent, and weak NMDA receptor antagonist, among other...