• 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...
    19 KB (2,273 words) - 12:18, 26 August 2023
  • Thumbnail for Allosteric regulation
    pharmacological selectivity that is unique to allosteric modulators is based on co-operativity. An allosteric modulator may display neutral co-operativity with...
    35 KB (4,264 words) - 00:50, 3 April 2024
  • Allosteric enzymes are enzymes that change their conformational ensemble upon binding of an effector (allosteric modulator) which results in an apparent...
    8 KB (1,027 words) - 11:08, 4 July 2022
  • drugs to treat obesity, and more besides. Channel modulator Enzyme modulator Transporter modulator van Westen GJ, Gaulton A, Overington JP (April 2014)...
    8 KB (982 words) - 17:21, 11 April 2024
  • Thumbnail for GABAA receptor positive allosteric modulator
    receptor positive allosteric modulators, also known as GABAkines or GABAA receptor potentiators, are positive allosteric modulator (PAM) molecules that...
    31 KB (3,523 words) - 16:44, 26 April 2024
  • Thumbnail for NMDA receptor
    Positive allosteric modulators Cerebrosterol – endogenous weak positive allosteric modulator Cholesterol – endogenous weak positive allosteric modulator...
    107 KB (12,051 words) - 23:49, 26 April 2024
  • Thumbnail for Alcohol (drug)
    Alcohol (drug) (category GABAA receptor positive allosteric modulators)
    negative allosteric modulator Nicotinic acetylcholine receptor positive allosteric modulator Opioid receptor endogenous positive allosteric modulator Serotonin...
    209 KB (21,044 words) - 07:40, 10 May 2024
  • Thumbnail for List of neurosteroids
    negative allosteric modulator 3α,5α-Androstanediol (3α-androstanediol): 5α-androstane-3α,17β-diol – GABAA receptor positive allosteric modulator 3α,5β-Androstanediol...
    19 KB (2,007 words) - 23:03, 8 December 2023
  • A GABAA receptor negative allosteric modulator is a negative allosteric modulator (NAM), or inhibitor, of the GABAA receptor, a ligand-gated ion channel...
    10 KB (934 words) - 07:32, 16 September 2023
  • Thumbnail for Dopamine receptor D2
    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...
    34 KB (3,958 words) - 20:55, 28 March 2024
  • Thumbnail for Metabotropic glutamate receptor 5
    (CPPHA) acts through a novel site as a positive allosteric modulator of group 1 metabotropic glutamate receptors". Molecular Pharmacology...
    27 KB (3,218 words) - 03:13, 22 January 2024
  • Thumbnail for Alpha-7 nicotinic receptor
    2007). "Nootropic alpha7 nicotinic receptor allosteric modulator derived from GABAA receptor modulators". Proceedings of the National Academy of Sciences...
    26 KB (2,626 words) - 05:08, 23 August 2023
  • Thumbnail for Allopregnanolone
    Allopregnanolone (category GABAA receptor positive allosteric modulators)
    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...
    50 KB (4,804 words) - 11:18, 26 January 2024
  • Thumbnail for Muscarinic acetylcholine receptor M1
    NCT04051801 for "Multiple Ascending Dose Phase I Study of the M1 Positive Allosteric Modulator VU0467319" at ClinicalTrials.gov Smith DL, Davoren JE, Edgerton JR...
    22 KB (2,214 words) - 12:49, 14 March 2024
  • 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...
    16 KB (1,564 words) - 20:19, 25 March 2024
  • Thumbnail for GABA receptor agonist
    act instead as positive allosteric modulators (PAMs) and while they do bind to the GABA receptors, they bind to an allosteric site on the receptor and...
    8 KB (740 words) - 19:39, 11 March 2024
  • Thumbnail for AMPA receptor positive allosteric modulator
    AMPA receptor positive allosteric modulators are positive allosteric modulators (PAMs) of the AMPA receptor (AMPR), a type of ionotropic glutamate receptor...
    12 KB (1,256 words) - 01:39, 20 November 2023
  • Thumbnail for Opioidergic
    Miyano K, Hirokawa T, Uezono Y (August 2016). "Ignavine: a novel allosteric modulator of the μ opioid receptor". Sci Rep. 6: 31748. Bibcode:2016NatSR....
    4 KB (378 words) - 21:40, 9 March 2024
  • Thumbnail for Metabotropic glutamate receptor 4
    subtype-selective PAM, intrinsic allosteric agonist activity, robust in-vivo activity PHCCC: PAM of mGluR4, negative allosteric modulator of mGluR1, direct agonist...
    15 KB (1,839 words) - 07:49, 23 December 2023
  • Thumbnail for Beta-2 adrenergic receptor
    2019). "Mechanism of β2AR regulation by an intracellular positive allosteric modulator". Science. 364 (6447): 1283–1287. Bibcode:2019Sci...364.1283L. doi:10...
    33 KB (3,372 words) - 23:10, 6 February 2024
  • Thumbnail for Calcium-sensing receptor
    pharmacology for CaSR allosteric modulators. For example, Calhex 231, which shows a positive allosteric activity when bound to the allosteric site in just one...
    34 KB (4,087 words) - 01:24, 21 April 2024
  • ; Powell, A. D.; Barnes, N. M. (2013). "5-Chloroindole: A potent allosteric modulator of the 5-HT3 receptor". British Journal of Pharmacology. 169 (6):...
    22 KB (2,391 words) - 07:50, 12 March 2024
  • Thumbnail for Dextromethorphan/bupropion
    reuptake inhibitor and nicotinic acetylcholine receptor negative allosteric modulator. Bupropion is also a potent inhibitor of CYP2D6, and thereby inhibits...
    21 KB (1,819 words) - 10:13, 31 December 2023
  • Thumbnail for Alprazolam
    Alprazolam (category GABAA receptor positive allosteric modulators)
    benzodiazepines, and method of discontinuation. Alprazolam is a positive allosteric modulator of the gamma-aminobutyric acid (GABA) type A receptor.[unreliable...
    86 KB (8,228 words) - 05:08, 3 May 2024
  • Thumbnail for Pregnenolone
    Pregnenolone (category CB1 receptor negative allosteric modulators)
    against schizophrenia. Pregnenolone is an allosteric endocannabinoid, as it is a negative allosteric modulator of the CB1 receptor. Pregnenolone is involved...
    21 KB (2,059 words) - 19:15, 7 December 2023
  • Thumbnail for Dextromethorphan
    serotonin–norepinephrine reuptake inhibitor) Sigma σ1 receptor agonist Negative allosteric modulator of nicotinic acetylcholine receptors Ligand of the serotonin 5-HT1B/1D...
    51 KB (4,585 words) - 14:47, 7 May 2024
  • Thumbnail for Muscarinic acetylcholine receptor M4
    effects of the selective M4 muscarinic acetylcholine receptor positive allosteric modulator VU0152100". Neuropsychopharmacology. 39 (7): 1578–93. doi:10.1038/npp...
    16 KB (1,853 words) - 03:12, 24 November 2022
  • Thumbnail for AMPA receptor
    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...
    60 KB (7,019 words) - 07:40, 8 May 2024
  • Thumbnail for Saffron
    Glutamate Ibotenic acid Proline Quisqualic acid Willardiine; Positive allosteric modulators: Aniracetam Cyclothiazide CX-516 CX-546 CX-614 Farampator (CX-691...
    70 KB (7,852 words) - 00:48, 3 May 2024
  • AGN-241751) – NMDA receptor positive allosteric modulator TAK-653 (NBI-1065845) – AMPA receptor positive allosteric modulator [5] OPC-64005 – serotonin–norepinephrine–dopamine...
    29 KB (2,454 words) - 14:36, 16 March 2024