CB1R Allosteric modulator 4 is an effective and positive modulator of cannabinoid type-1 (CB1R), exhibiting significant biological activity. This compound inhibits the production of cAMP and demonstrates strong β-arrestin-2 recruitment [1].

CB1R Allosteric modulator 1 (compound 11) is a potent allosteric modulator of CB1R. CB1R Allosteric modulator 1 negatively affects the functional activity of orthosteric ligands (NAM) at CB1Rs.

CB1R Allosteric modulator 3 is a potent CB1R modulator.CB1R Allosteric modulator 3 inhibits cAMP and β-Arrestin, and can be used for the study of obesity and nicotine addiction.

CB1R Allosteric modulator 2 (compound 18) is a potent allosteric modulator of the CB1R receptor. It exhibits negative modulation of the functional activity of orthosteric ligands (NAM) at CB1Rs, as demonstrated in previous studies [1].

6-Methoxyflavanone (6-MeOF) is A positive allosteric modulator of the GABA response of human recombinant GABA A receptor, with antianxiety and anti-inflammatory activity, and can be used to reduce cisplatin induced neuropathic pain.

VU 0285683 is a specific negative allosteric modulator of mGluR5 with a high affinity for the MPEP binding site. VU 0285683 shows anxiolytic-like activity.

2'MeO6MF is a brain-penetrant positive allosteric modulator at α2β1γ2L and all α1-containing GABAA receptors.It offers neuroprotection and improved functional recovery and dampens the stroke-induced inflammatory response. 2'MeO6MF has anxiolytic and sedative effects.

(Rac)-VU 6008667 is a selective negative allosteric modulator of muscarinic acetylcholine receptor subtype 5 (M5 NAM) with IC50 of 1.8 μM and pIC50 of 5.75, has high CNS penetration.

JNJ-39393406 is an α7 nicotinic acetylcholine receptor positive allosteric modulator for the study of tobacco dependence and Alzheimer's disease.

(S, R)-LSN 3318839 is an allosteric modulator of the glucagon-like peptide-3318839 receptor (GLP-1R) that has demonstrated powerful hypoglycemic effects in animal models alone or in combination with sitagliptin.

Positive allosteric modulator of GABAA receptors

LY2033298, a positive allosteric modulator of muscarine M4 receptor, enhances the inhibitory effect of oximoline on light-induced phase shift in circadian activity in hamsters and can be used in neurosystem-related diseases.

RVD-Hpα acetate is the N-terminally extended form of human hemopressin that acts as a selective CB1 receptor agonist. Increases intracellular Ca2+ levels in cells expressing CB1 receptors in vitro. Also high affinity CB2 positive allosteric modulator (Ki

E1R is a positive sigma-1 receptor (Sig1R PAM) allosteric modulator. It has a cognition-enhancing activity.

Tecalcet Hydrochloride (R-568 hydrochloride) is an allosteric and positive modulator of the calcium-sensing receptor(CaSR). Tecalcet Hydrochloride increases the sensitivity to the activation of extracellular Ca2+.

VU6012962 is an orally bioavailable negative allosteric modulator of CNS-penetrant metabotropic glutamate receptor 7(mGlu7; IC50: 347 nM).

FzM1, a negative allosteric modulator (NAM) of the Frizzled receptor FZD4, diminishes WNT5A-dependent WNT responsive element (WRE) activity (log EC50inh=−6.2) by binding to an allosteric site on intracellular loop 3 (ICL3) of FZD4. This interaction changes the receptor's conformation and inhibits the WNT/β-catenin signaling pathway.

BA-53038B is an HBV core protein allosteric modulator (CpAM), binding to the HAP pocket and modulating HBV capsid assembly in a distinct manner (EC50: 3.32 μM).

Dopamine D2 Receptor Antagonist-1 functions as a negative allosteric modulator (NAM) of the dopamine D2 receptor (D2R), demonstrating sub-millimolar affinity.

AZ10606120 dihydrochloride is a selectable, potent, high-affinity receptor antagonist with K D values of 1.4 and 19 nM at human and rat P2X 7 receptors, respectively. AZ10606120 dihydrochloride inhibits tumor growth and has anti-angiogenic activity. AZ 10606120 acts as a negative allosteric modulator when bound to a site coupled to the ATP binding site.

(2R,3S)-E1R (Compound 2c) is an enantiomer of E1R. (2R,3R)-E1R is a sigma-1 receptor positive allosteric modulator for the treatment of cognition/memory disorders.

(2S,3S)-E1R (Compound 2d) is an enantiomer of E1R. (2R,3R)-E1R is a sigma-1 receptor positive allosteric modulator for the treatment of cognition/memory disorders.

PSNCBAM-1 (PSNCBAM 1) is a CB1 receptor negative allosteric modulator (EC50 = 0.1 μM) with hypophagic effects in vivo. PSNCBAM-1 can be used for obesity studies.

S 18986 is a selective, orally active, brain penetrant positive allosteric modulator of AMPA-type receptors, showcasing cognitive-enhancing properties in rodents. It induces the release of noradrenaline and acetylcholine in the rat hippocampus, leading to enhanced object-recognition memory.

CPPHA, a positive allosteric modulator of glutamate receptors mGluR5 and mGluR1, is commonly used in development for central nervous system diseases.

ML353 (VU0478006) is a selective activator of TREK-1 and TREK-2 and a selective ligand (Ki =18.2 nM) for the mGlu5 Silencing Allosteric Modulator (SAM). ML353 has potential as a solution to the intrinsic activity or pharmacological blockade of SAM in vivo.

(E)-GABAB receptor antagonist 1 is a trans-GABAB receptor antagonist 1. (E)-GABAB receptor antagonist 1 decreases GABA-induced IP3 (inositol trisphosphate) production with IC50 of 37.9 μM. GABAB receptor antagonist 1 is a selective and negative allosteric modulator of GABAB (γ-Aminobutyric acid) receptors.

BMT-145027 is a positive allosteric modulator of mGluR5 without inherent agonist activity (EC50 = 47 nM).

N-terminally extended form of human hemopressin that acts as a selective CB1 receptor agonist. Increases intracellular Ca2+ levels in cells expressing CB1 receptors in vitro. Also high affinity CB2 positive allosteric modulator (Ki = 50 nM).

PF-06372222 is a small-molecule negative allosteric modulator of the glucagon receptor (GCGR). PF-06372222 is also an antagonist for glucagon-like peptide-1 receptor GLP-1R, which inhibits glucagon secretion and glucose-dependent insulin secretion.

A-867744 is an effective and selective type II positive allosteric modulator of the α7 nAChR (EC50: 1.0 μM).

JAMI1001A is a positive allosteric modulator of the AMPA receptor, effectively modulating the deactivation and desensitization of both flip and flop receptor isoforms.

Loreclezole is a selective GABAA receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit-containing receptors.

VU-1545 is mGlu5 positive allosteric modulator.

BPAM344 is a potent positive allosteric modulator (PAM) of the KAR subunits GluK1b, GluK2a, and GluK3a.

TAK-615 is commonly used to study pulmonary fibrosis and is a negative allosteric modulator of LPA1 receptors.

Basmisanil (RG1662) is a negative allosteric modulator/inverse agonist of GABAAα5 receptors.Formulations containing basmisanil are in clinical trials for the treatment of cognitive impairments associated with Down syndrome.

TQS (4-Naphthalen-1-yl-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-8-sulfonamide) is a positive allosteric modulator of α7 nACh receptors.

SGE516 is a neuroactive steroid and a positive allosteric modulator of both gamma- and delta-containing GABAA receptors. SGE516 reduces neuronal firing rates and epileptiform activity in vitro. SGE-516 protects against acute seizures and reduces neuronal

Br-PBTC is a highly potent, 2/4 subtype-selective positive allosteric modulator of nicotinic acetylcholine receptors (nAChRs). It specifically targets α2β2, α2β4, α4β2, α4β4, (α4β2)2α4, and (α4β2)2β2 subtypes of nAChRs, with EC50 values ranging from 0.1 to 0.6 μM. Br-PBTC exerts its activity by binding to the c-tail region of an α subunit.

ONO-8590580 (CS-2894) is a negative allosteric modulator of GABAA α5.

BMS986188 is a novel Potent and Selective Positive Allosteric Modulator of the delta-Opioid Receptor.

VU0453379 is a highly selective and central nervous system penetrant positive allosteric modulator of glucagon-like peptide-1R (EC50: 1.3 μM).

VPC171 is a novel adenosine A1 receptor positive allosteric modulator (PAM).

LSN3160440 is an allosteric modulator of GLP-1R, functioning as a protein-protein interaction (PPI) stabilizer or molecular glue. It aids in the binding of inactive GLP-1 (9-36) NH2 to GLP-1R, enhancing receptor activation and potential therapeutic effects [1] [2].

Pregnanolone is a cell membrane modulator potentially for the treatment of pain. Pregnanolone is an endogenous neurosteroid that is biosynthesized from progesterone. It is a positive allosteric modulator of the GABAA receptor, as well as a negative allost

LY404187 is a positive allosteric modulator of AMPA receptors

VU0477886 is a potent mGlu4 positive allosteric modulator (PAM) with robust efficacy in a standard preclinical Parkinson's disease model, haloperidol-induced catalepsy (HIC).

CX516 (Ampalex), an ampakine and nootropic, acts as an AMPA receptor positive allosteric modulator as a therapy for Alzheimer's disease, schizophrenia and mild cognitive impairment (MCI).

BNC210 (IW-2143) is a α7 nAChR negative allosteric modulator. BNC210 has potent activity in animal models of anxiety and depression.

L838417 is a modulator of the GABAA receptor.