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Substance that binds to a receptor to change its response to stimuli
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
Allosteric_modulator
Regulation of enzyme activity
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
Allosteric_regulation
Class of neurotransmitter modulators
receptor positive allosteric modulators, also known as GABAkines or GABAA receptor potentiators, are positive allosteric modulator (PAM) molecules that
GABAA receptor positive allosteric modulator
GABAA_receptor_positive_allosteric_modulator
Investigational insomnia drugs
GABAA receptor positive allosteric modulator), and zolpidem (nonbenzodiazepine/Z-drug and GABAA receptor positive allosteric modulator) Zuranolone (BIIB-125;
List of investigational insomnia drugs
List_of_investigational_insomnia_drugs
Investigational anxiety disorder drugs
receptor positive allosteric modulator and neurosteroid (brexanolone prodrug) [4] Cannabidiol (CBD; Arvisol) – cannabinoid receptor modulator and other actions
List of investigational anxiety disorder drugs
List_of_investigational_anxiety_disorder_drugs
Class of drug
Istradefylline Paraxanthine Others GABAA receptor antagonists and negative allosteric modulators (e.g., clarithromycin, flumazenil, pentylenetetrazol (pentetrazol))
Dopamine_reuptake_inhibitor
Investigational generalized anxiety disorder drugs
allosteric modulator and nonbenzodiazepine/pyrazolopyrimidine [31] Pagoclone (IP-456; Panex; RP-62955) – GABAA receptor positive allosteric modulator
List of investigational generalized anxiety disorder drugs
List_of_investigational_generalized_anxiety_disorder_drugs
Class of drugs
AMPA receptor positive allosteric modulators are positive allosteric modulators (PAMs) of the AMPA receptor (AMPR), a type of ionotropic glutamate receptor
AMPA receptor positive allosteric modulator
AMPA_receptor_positive_allosteric_modulator
TrkA and TrkB positive modulator
is a tropomyosin receptor kinase TrkA, TrkB, and TrkC positive allosteric modulator which is under development for the treatment of Alzheimer's disease
ACD856
Investigational substance-related disorder drugs
alcoholism Zolpidem (ALM-006; ALM006) – GABAA receptor positive allosteric modulator/nonbenzodiazepine – substance-related disorders Metyrapone/oxazepam
List of investigational substance-related disorder drugs
List_of_investigational_substance-related_disorder_drugs
Drug class
A GABAA receptor negative allosteric modulator is a negative allosteric modulator (NAM), or inhibitor, of the GABAA receptor, a ligand-gated ion channel
GABAA receptor negative allosteric modulator
GABAA_receptor_negative_allosteric_modulator
Category of drug
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
GABA_receptor_agonist
Class of opioid receptors found in humans
"Neuropeptide oxytocin enhances μ opioid receptor signaling as a positive allosteric modulator". Journal of Pharmacological Sciences. 137 (1): 67–75. doi:10.1016/j
Mu-opioid_receptor
negative allosteric modulator 3α,5α-Androstanediol (3α-androstanediol): 5α-androstane-3α,17β-diol – GABAA receptor positive allosteric modulator 3α,5β-Androstanediol
List_of_neurosteroids
List of pharmaceutical drugs under clinical development for treatment of depression
receptor negative allosteric modulator ONO-1110 – endocannabinoid synthesis regulator and indirect cannabinoid receptor modulator [1] [2] [3] Opakalim
List of investigational antidepressants
List_of_investigational_antidepressants
Type of cell receptor found in humans
2007). "Nootropic alpha7 nicotinic receptor allosteric modulator derived from GABAA receptor modulators". Proceedings of the National Academy of Sciences
Alpha-7_nicotinic_receptor
Glutamate receptor and ion channel protein found in nerve cells
Positive allosteric modulators Cerebrosterol – endogenous weak positive allosteric modulator Cholesterol – endogenous weak positive allosteric modulator
NMDA_receptor
Substance related to dopamine functions
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
Dopaminergic
Atypical opioid drug
receptor. In addition, the drug appears to also act as a MOR positive allosteric modulator, with this possibly being its primary action. Unlike conventional
SR-17018
Experimental antidepressant
(Millennium Pharmaceuticals, Inc.). Osavampator is a selective positive allosteric modulator (PAM) of the AMPA receptor. Osavampator and other AMPA PAMs potentiate
Osavampator
Investigational antipsychotics
receptor positive allosteric modulator – schizophrenia [157] Davunetide intranasal (AL-108; NAP; NAPVSIPQ) – microtubule modulator – schizophrenia [158]
List of investigational antipsychotics
List_of_investigational_antipsychotics
Enzymes that change shape and activity
Allosteric enzymes are enzymes that change their conformational ensemble upon binding of an effector (allosteric modulator) which results in an apparent
Allosteric_enzyme
Subtype of serotonin receptor
serotonin 5-HT2A receptor positive allosteric modulator. A dual serotonin 5-HT2C and 5-HT2A receptor positive allosteric modulator is the oleamide analogue JPC0323
5-HT2A_receptor
Mammalian protein found in humans
(CPPHA) acts through a novel site as a positive allosteric modulator of group 1 metabotropic glutamate receptors". Molecular Pharmacology
Metabotropic glutamate receptor 5
Metabotropic_glutamate_receptor_5
Pharmaceutical compound
RAP-219, formerly known as JNJ-64300912, is an AMPA receptor negative allosteric modulator which is under development for the treatment of partial epilepsies
RAP-219
Investigational cognition and memory disorder drugs
receptor positive allosteric modulator [18] JN-0413 – synthetic α-klotho protein [19] TET-104 – AAV-based gene therapy modulating E2F4 [20] Amdiglurax
List of investigational cognition and memory disorder drugs
List_of_investigational_cognition_and_memory_disorder_drugs
Chemical compound
VU-0152099 is a positive allosteric modulator of the M4 receptor used in scientific research. VU-0152099 is a positive allosteric modulator acting at M4 receptors
VU-0152099
Obsolete sedative–hypnotic drug
sleep. It binds to GABAA receptors, where it functions as a positive allosteric modulator at many receptor subtypes, enhancing the inhibitory effects of the
Methaqualone
Ionotropic serotonin receptor
; Powell, A. D.; Barnes, N. M. (2013). "5-Chloroindole: A potent allosteric modulator of the 5-HT3 receptor". British Journal of Pharmacology. 169 (6):
5-HT3_receptor
Pharmaceutical compound
LTI-291) is a β-glucocerebrosidase (GCase) activator or positive allosteric modulator which is under development for the treatment of Parkinson's disease
Pariceract
Chemical compound
IDRA-21 is a positive allosteric modulator of the AMPA receptor and a benzothiadiazine derivative. It is a chiral molecule, with (+)-IDRA-21 being the
IDRA-21
Transmembrane protein family
Albert Y.; Huganir, Richard L.; Twomey, Edward C. (November 2024). "Allosteric competition and inhibition in AMPA receptors". Nature Structural & Molecular
AMPA_receptor
Sustained Efficacy of Onfasprodil (MIJ821), a Novel NR2B Negative Allosteric Modulator, in Patients With Treatment-Resistant Depression: A Phase 2, Randomized
NMDA_receptor_modulator
Investigational Parkinson's disease drugs
agonist [32] Glovadalen (UCB-0022) – dopamine D1 receptor positive allosteric modulator [33] GRF-6021 (AKST-6021) – plasma protein fraction and neurogenesis
List of investigational Parkinson's disease drugs
List_of_investigational_Parkinson's_disease_drugs
Drug whose use induces sleep
allopregnanolone that likewise acts as a GABAA receptor positive allosteric modulator but is orally active. It is under development for the treatment of
Hypnotic
Ionotropic receptor and ligand-gated ion channel
(RO-7308480) (selective γ1 positive allosteric modulator; classical benzodiazepines are selective γ2 positive allosteric modulators) α5IA (selective inverse agonist
GABAA_receptor
Protein-coding gene in the species Homo sapiens, named for ketazocine
GPR139 receptor. In addition, oxytocin was found to be a positive allosteric modulator of KOR, and a variety of natural alkaloids, terpenoids, and synthetic
Κ-opioid_receptor
G-protein coupled receptor
Retrieved 2009-04-12. Adams CL, Lawrence AJ (2007). "CGP7930: a positive allosteric modulator of the GABAB receptor". CNS Drug Reviews. 13 (3): 308–16. doi:10
GABAB_receptor
Pharmaceutical compound
GT-02287 is a β-glucocerebrosidase (GCase) activator, positive allosteric modulator, and/or chaperone which is under development for the treatment of Parkinson's
GT-02287
Investigational antimigraine drugs
Sepranolone (isoallopregnanolone; UC-1010) – GABAA receptor negative allosteric modulator and neurosteroid – menstrual migraine [25] TRV-250 – δ-opioid receptor
List of investigational headache and migraine drugs
List_of_investigational_headache_and_migraine_drugs
Chaperone protein
Svalbe B, Domracheva I, Vilskersts R, et al. (2015). "Novel positive allosteric modulators of sigma-1 receptor". SpringerPlus. 4 (Suppl 1): 51. doi:10
Sigma-1_receptor
Drug that blocks hallucinogen effects
psychedelic experiences. Alcohol, which is also a GABAA receptor positive allosteric modulator with similar effects, has been used for such purposes as well. Besides
Trip_killer
nicotinic acetylcholine receptor negative allosteric modulator Cannabidiol (CBD) – cannabinoid receptor modulator and other actions, found in cannabis Gabapentinoids
List of investigational social anxiety disorder drugs
List_of_investigational_social_anxiety_disorder_drugs
Chemical compound
BMS‐986122 is a selective positive allosteric modulator (PAM) of the μ-opioid receptor (MOR). MOR PAMs like BMS-986122 could be useful as novel analgesics
BMS‐986122
name Quaalude). They are known to act as GABAA receptor positive allosteric modulators to produce their effects. Methaqualone itself was invented in the
List of methaqualone analogues
List_of_methaqualone_analogues
Substance that binds to and regulates the activity of chemical receptors
Channel modulator Transporter modulator van Westen GJ, Gaulton A, Overington JP (April 2014). "Chemical, target, and bioactive properties of allosteric modulation"
Receptor_modulator
Pharmaceutical compound
an NR2B (GluN2B; GRIN2B) subunit-selective NMDA receptor negative allosteric modulator which is under development for the treatment of neurodevelopmental
Radiprodil
Investigational tinnitus drugs
(allopregnanolone; SAGE-547; SGE-102; Zulresso) – GABAA receptor positive allosteric modulator and neurosteroid [1] Ebselen (DR-3305; ebselene; ebseleno; ebselenum;
List of investigational tinnitus drugs
List_of_investigational_tinnitus_drugs
Classification of chemicals that directly modulate opioid neuropeptide systems
Miyano K, Hirokawa T, Uezono Y (August 2016). "Ignavine: a novel allosteric modulator of the μ opioid receptor". Sci Rep. 6 31748. Bibcode:2016NatSR..
Opioidergic
Pharmaceutical compound
receptor positive allosteric modulator. 5-HT2C receptor § Positive allosteric modulators 5-HT2A receptor § Positive allosteric modulators AB0124 and CTW0404
JPC0323
Mammalian protein found in humans
subtype-selective PAM, intrinsic allosteric agonist activity, robust in-vivo activity VU0364770 PHCCC: PAM of mGluR4, negative allosteric modulator of mGluR1, direct
Metabotropic glutamate receptor 4
Metabotropic_glutamate_receptor_4
Serotonin receptor protein distributed in the cerebrum and raphe nucleus
of a Minor Cannabinoid: Cannabicyclol (CBL) Is a Potent Positive Allosteric Modulator of Serotonin 5-HT1A Receptor". J Nat Prod. 88 (1): 58–66. Bibcode:2025JNAtP
5-HT1A_receptor
Chemical compound
Darigabat acts as a GABAA receptor positive allosteric modulator It is specifically a positive allosteric modulator that selectively targets α2, α3, and α5
Darigabat
Mammalian protein found in Homo sapiens
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
Dopamine_transporter
Chemical agents that inhibit Cholinesterase
Partial agonist Antagonist Inverse agonist Positive allosteric modulator (PAM) Negative allosteric modulator (NAM) ♦ Transporter [Reuptake vs Efflux]: Enhancer
Cholinesterase_inhibitor
Hypnotic medication
enhancing the natural effect of GABA receptors by acting as a positive allosteric modulator on GABA-A expressing neurons. Common side effects include headache
Eszopiclone
Combination medication
reuptake inhibitor and nicotinic acetylcholine receptor negative allosteric modulator. Bupropion is also a potent inhibitor of CYP2D6, and thereby inhibits
Dextromethorphan/bupropion
Pharmaceutical compound
experimental drug which acts as a selective antagonist (or perhaps negative allosteric modulator) at the free fatty acid receptor GPR84. It has antiinflammatory and
GLPG1205
Pharmaceutical compound
ASP-8062, or ASP8062, is a GABAB receptor positive allosteric modulator which is under development for the treatment of alcoholism. It was also under development
ASP-8062
muscaria) Indirect GABAA receptor agonists: GABAA receptor positive allosteric modulators (nonbenzodiazepines/Z-drugs) (e.g., eszopiclone, zaleplon, zolpidem
List_of_hallucinogens
Cough suppressant and dissociative drug
serotonin–norepinephrine reuptake inhibitor) Sigma σ1 receptor agonist Negative allosteric modulator of nicotinic acetylcholine receptors Ligand of the serotonin 5-HT1B/1D
Dextromethorphan
Chemical compound; modulator of the cannabinoid CB1 receptor
GAT100 is a negative allosteric modulator of the cannabinoid CB1 receptor. Org 27569 PSNCBAM-1 ZCZ-011 Kulkarni PM, Kulkarni AR, Korde A, Tichkule RB,
GAT100
Pharmaceutical compound
CTW0404 is an experimental drug which is described as a positive allosteric modulator of the 5-HT2A receptor, with neutral or negative modulation of the
CTW0404
Medication used to treat dyskinesia
sigma σ1 receptor agonist, nicotinic acetylcholine receptor negative allosteric modulator, dopaminergic agent, and weak NMDA receptor antagonist, among other
Amantadine
Chemical compound
without acting as a sedative or stimulant. Piracetam is a positive allosteric modulator of the AMPA receptor, although this action is very weak and its clinical
Piracetam
Pharmaceutical compound
INDV-1000 is a GABAB receptor positive allosteric modulator (PAM) which is under development for the treatment of substance-related disorders. Its route
INDV-1000
Chemical compound
NSC 87503) is an indole alkaloid mood enhancer. It is a positive allosteric modulator of the serotonin 5-HT3 receptor. "5-Hydroxyindole 97 1953-54-4".
5-Hydroxyindole
Chemical compound
does not functionally act at human nAChRs α4β2 or α7 as a positive allosteric modulator. Galantamine also works as a weak competitive and reversible cholinesterase
Galantamine
Protein and coding gene in humans
lisuride (nanomolar range) have all been reported to act as positive allosteric modulators of TrkB. However, subsequent studies with LSD and psilocin failed
Tropomyosin_receptor_kinase_B
Class of drugs
Methylphenylpiracetam, a derivative of phenylpiracetam, is a positive allosteric modulator of the sigma σ1 receptor. It is currently the only racetam known
Racetam
Sleep medication
or Z-drug, which acts as a sedative and hypnotic as a positive allosteric modulator at the GABAA receptor. It is an imidazopyridine and increases GABA
Zolpidem
Brexanolone (allopregnanolone; Zulresso) – GABAA receptor positive allosteric modulator – approved for postpartum depression Dextromethorphan/bupropion (Auvelity)
List_of_antidepressants
Chemical compound
drug used in scientific research that acts as a selective positive allosteric modulator for the metabotropic glutamate receptor group II subtype mGluR2.
LY-487,379
Psychoactive drug, often called ecstasy
likely that TAARs contribute to the actions of specific stimulants to modulate dopaminergic, serotonergic, and glutamate signaling,90 and drugs acting
MDMA
Class of antidepressant medication
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
Serotonin modulator and stimulator
Serotonin_modulator_and_stimulator
Genetic disorder caused by a mutation of chromosome 15
α5 receptor. Alogabat is a small molecule that acts as a positive allosteric modulator (PAMs) of the receptor. It does not involve replacing or activating
Angelman_syndrome
Endogenous inhibitory neurosteroid
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
Allopregnanolone
Chemical compound
those with Parkinson's disease. It acts as a selective positive allosteric modulator (PAM) of the dopamine D1 receptor. The drug is orally active and
Mevidalen
Psychedelic drug
agonism. LSD has also been reported to act as a highly potent positive allosteric modulator of the tropomyosin receptor kinase B (TrkB), one of the receptors
LSD
Antibiotic medication
antibiotic activity, clarithromycin has been found to act as a negative allosteric modulator of the GABAA receptor. In relation to this action, it may have
Clarithromycin
Pharmaceutical compound
drug from the piperidine family, which acts as a selective positive allosteric modulator of the 5-HT2C receptor, with higher potency than older drugs such
CTW0415
Chemical compound
is taken by mouth. The drug acts as a highly selective negative allosteric modulator (NAM) of the α7-nicotinic acetylcholine receptor (α7-nAChR). It produces
Soclenicant
Mammalian protein found in Homo sapiens
Ulotaront Urapidil VML-670 (CEB-1555) Xaliproden Yohimbine Positive allosteric modulators: Cannabicyclol (CBL) Oleamide Antagonists: Atypical antipsychotics
5-HT1B_receptor
Muscle relaxant medication
cyclobenzaprine as a muscle relaxant is unknown. However, it may work through modulating the serotonergic and noradrenergic systems. The antihistamine activity
Cyclobenzaprine
Serotonin receptor protein distributed mainly in the choroid plexus
Rodríguez R, Codesido E, Cruces J, et al. (December 2017). "A Positive Allosteric Modulator of the Serotonin 5-HT2C Receptor for Obesity". Journal of Medicinal
5-HT2C_receptor
Pharmaceutical compound
drug from the indole family, which is acts as a selective positive allosteric modulator of the 5-HT2C receptor. It has anorectic effects in animal studies
VA012
Parasympathetic nervous system inhibitors
Partial agonist Antagonist Inverse agonist Positive allosteric modulator (PAM) Negative allosteric modulator (NAM) ♦ Transporter [Reuptake vs Efflux]: Enhancer
Anticholinergic
Possible drug for treating drug dependence
SBP 9330 is an investigational small-molecule drug and a positive allosteric modulator (PAM) of the metabotropic glutamate receptor 2 (mGluR2), being developed
SBP-9330
Investigational other psychiatric disorder drugs
[32] DT-201 (DT201) – α5 subunit-containing GABAA receptor negative allosteric modulator – psychiatric disorders [33] KAR-501 (KAR501) – undefined mechanism
List of investigational other psychiatric disorder drugs
List_of_investigational_other_psychiatric_disorder_drugs
Medication of the barbiturate type
for barbiturate poisoning is available. Phenobarbital acts as an allosteric modulator which extends the amount of time the chloride ion channel is open
Phenobarbital
Pharmaceutical compound
ASP-4345, or ASP4345, is a dopamine D1 receptor positive allosteric modulator which is or was under development for the treatment of schizophrenia. It
ASP-4345
Main receptor for most antipsychotic drugs
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
Dopamine_receptor_D2
Mammalian protein found in humans
pharmacology for CaSR allosteric modulators. For example, Calhex 231, which shows a positive allosteric activity when bound to the allosteric site in just one
Calcium-sensing_receptor
Class of depressant drugs derived from barbituric acid
depression caused by the barbiturates) Barbiturates act as positive allosteric modulators and, at higher doses, as agonists of GABAA receptors. GABA is the
Barbiturate
Class of CNS depressant drugs
Unlike other positive allosteric modulators that increase ligand binding, benzodiazepine binding acts as a positive allosteric modulator by increasing the
Benzodiazepine
Class of anesthetics
to glycine sites; noncompetitive antagonists inhibit binding to NMDARs allosteric sites; and uncompetitive antagonists block binding to a site within the
NMDA_receptor_antagonist
Pharmaceutical compound
BI-1569912 is a selective negative allosteric modulator of NR2B-containing NMDA receptors. It is being developed by Boehringer Ingelheim to treat major
BI-1569912
Small neuroactive peptide
undisclosed. However, it has been described as acting as a positive allosteric modulator of the AMPA receptor and has been found to increase brain-derived
Cyclic_glycine-proline
Pharmaceutical compound
also known as BAER-101 or as AZD-7325, is a GABAA receptor positive allosteric modulator and nonbenzodiazepine which is under development for the treatment
AXS-17
Type of pharmaceutical drug
A reuptake modulator, or transporter modulator, is a type of drug which modulates the reuptake of one or more neurotransmitters via their respective neurotransmitter
Reuptake_modulator
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