allosteric modulator

VU0483605 is an effective and selective positive allosteric modulator of mGluR1 with EC50s of 390 and 356 nM for human and rat, respectively.

GluN2A Allosteric modulator 1 (Compound 11) is an orally bioavailable compound that effectively crosses the blood-brain barrier and functions as a highly selective negative allosteric modulator of GluN2A. It exhibits an IC50 of 0.042 μM for GluN2A and 13 μM for GluN2B. This compound is useful for research in neurological disorders.

CB1R Allosteric Modulator 2 (compound 18) is a potent negative allosteric modulator (NAM) of CB1R receptor activity, as demonstrated in previous studies [1].

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

CB1R Allosteric Modulator 1 (compound 11) is a potent allosteric modulator of CB1Rs, negatively affecting the functional activity of orthosteric ligands [NAM] at CB1Rs.

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

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

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

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

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

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+.

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.

S 18986 is a selective, orally active, brain-penetrant positive allosteric modulator of AMPA-type receptors that enhances cognition in rodents by inducing the release of noradrenaline and acetylcholine in the rat hippocampus, subsequently improving object-recognition memory.

Positive allosteric modulator of GABAA receptors

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.

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

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.

GNE-8324 is a GluN2A selective positive allosteric modulator that selectively enhances NMDAR-mediated synaptic responses in inhibitory, but not excitatory, neurons.GNE-8324 is used in the study of neurological disorders.

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.

DCB (3,3'-dichlorobenzaldazine) is an allosteric ligand for mGluR5 and shows the negative modulatory effect of 3,3′-dimethoxybenzaldazine (DMeOB). DCB blocks the positive allosteric regulation of mGluRs with the help of 3,3′-difluorobenzaldazine (DFB).

Tanshinone IIA sulfonate sodium (Tanshinone IIA sodium sulfonate) is a water-soluble derivative of tanshinone IIA extracted from Savia miltiorrhiza; a potent negative allosteric modulator of the human purinergic receptor P2X7. Tanshinone IIA sulfonate sodium (12.5 μM) inhibits hypoxia-induced PKG and PPAR-γ downregulation in PASMCs and distal pulmonary arteries of rats.

VU0364770 (VU 0364770)(EC50=1.1 μM), a positive allosteric modulator(PAM) of mGlu4, shows insignificant activity at 68 other receptors, including other mGlu subtypes.

6-Methoxyflavanone (6-MeOF) is a positive allosteric modulator of the GABA response in human recombinant GABA A receptors, exhibiting antianxiety and anti-inflammatory properties, and is used to alleviate cisplatin-induced neuropathic pain.