allosteric agonist

LUF6096 (CF-602) is a potent allosteric enhancer of the adenosine A3 receptor, exhibiting the capability to enhance agonist binding allosterically while demonstrating low orthosteric affinity across adenosine receptors. It displays protective effects in myocardial ischemia reperfusion injury.

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

Cinacalcet (AMG 073) is an orally active, allosteric Ca receptor (CaR) agonist used in the treatment of cardiovascular disease.

4-CMTB is a selective agonist of FFA2 and GPR43.It also is a positive allosteric modulator (pEC50=6.38).

VU0155041 is an effective and positive allosteric modulator allosteric agonist at mGlu4 receptors (EC50: 798 693 nM, at human rat).

ATI-2341 acetate is an effective allosteric agonist of CXCR4, it activates Gα1 instead of Gα13. ATI-2341 acetate activates inhibitory heterotrimeric G protein (GI) to promote the inhibition of cAMP production and induce calcium mobilization.

VU0119498 is a M1 muscarinic receptor agonist (EC50 = 3.1 μM) and pan mAChR M3, M5 positive allosteric modulator (PAM),and is a neuroprotective agent.

GPR40 FFAR1 modulator 1 is a Gq-coupled free fatty acid receptor 1 (GPR40 FFAR1) agonist and allosteric modulator.

ADH-503 (GB1275) is an orally available, allosteric CD11b small molecule agonist that can lead to repolarization of tumor-associated macrophages, reduction in the number of tumor-infiltrating immunosuppressive myeloid cells, and enhancement of dendritic cell responses.

L-838417 D9 (C-21191) is a novel deuterated subtype-selective GABAA positive allosteric modulator, acting as a partial agonist at α2, α3 and α5 subtypes[1].

4BP-TQS is an allosteric agonist of α7 nAChRs.

ATI-2341 is an effective functionally selective allosteric agonist for the c-x-c chemokine receptor type 4 (CXCR4), which ACTS as a biased ligand in favor of G G G G G 1 activation instead of G G G G G 13.ATI-2341 activates the inhibitory heterotrimer G p

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).

GAT229 is a positive allosteric modulator of cannabinoid receptor 1 (CB1) and the S-(-) enantiomer of the CB1 modulator GAT211. It does not activate the receptor on its own but enhances the binding and activity of CB agonists. GAT229 (1 μM) enhances the binding of the CB1 full agonist CP 55,940 to CHO cells expressing human recombinant CB1 (hCB1), as well as the activity of 2-arachidonoyl glycerol , arachidonoyl ethanolamide , and CP 55,940 in arrestin2 recruitment assays and increases ERK1/2 and PLCβ3 phosphorylation in HEK293 cells expressing hCB1. GAT229 (1 μM) enhances depolarization-induced suppression of excitation but does not inhibit excitatory postsynaptic currents (EPSCs) in murine autaptic hippocampal neurons. GAT229 (0.2%, topical) reduces intraocular pressure by 5.8 and 7.7 mm Hg after 6 and 12 hours, respectively, in a transgenic mouse model of ocular hypertension using nose, ear, eye mutation (nee) mice.

MRS8247 is a positive allosteric modulator (PAM) of the A3 adenosine receptor (A3AR), which also slows the dissociation rate of the agonist.

DFPQ is a powerful and selective β-arrestin-biased negative allosteric modulator(NAM) targeting the β2-adrenergic receptor. It specifically inhibits the interaction of β-arrestin with β2AR without altering β-agonist-induced cAMP production. Additionally, DFPQ reduces functional desensitization of the β2AR in airway smooth muscle, enhancing β-agonists' capacity to maintain bronchorelaxation and curbing cell migration during prolonged β-agonist treatment.

CVN636, a potent and selective allosteric agonist for the mGluR7 receptor, exhibits oral activity and CNS permeability [1], with an EC50 of 7 nM for human mGluR7.

AP5 sodium is a selective, potent, orally active GPR40 receptor agonist that exhibits positive allosteric modulation of endogenous ligands (AgoPAM). sodium exhibits potential for the study of type II diabetes.

GAT100 is a potent and covalent negative allosteric modulator (NAM). GAT-100 behaved as a robust positive allosteric modulator of binding of orthosteric agonist CP55,940. This novel covalent probe can serve as a useful tool for characterizing CB1R allosteric ligand-binding motifs.

mGlu4 receptor agonist 1 (compound 62) is a potent positive allosteric modulator of mGlu4 receptors, with an EC50 of 308 nM, and exhibits significant anxiolytic and antipsychotic properties [1].

Fenobam shows inverse agonist activity which blocks the mGlu5 receptor basal activity(IC50: 84 nM). Fenobam has anxiolytic activity. Fenobam is a selective and non-competitive mGluR5 antagonist acting at an allosteric modulatory site (Kd values are 54 and 31 nM for rat and human recombinant mGlu5 receptors, respectively).

24(S)-hydroxy Cholesterol (24S-OHC) is the terminal product of the cholesterol elimination pathway in neural tissues. It is an LXR agonist and a selective positive allosteric modulator of NMDARs. It can serve as a biomarker for NPD, induce cognitive decline in mice, and is useful for studying neurological diseases.

Smoothened (SMO) is a GPCR-like receptor which, with Patched, mediates hedgehog signaling to regulate gene expression through the Gli transcription factors. 20(S)-hydroxy Cholesterol (20(S)-OHC) is an oxysterol which binds SMO and activates hedgehog signaling (EC50 = 3 μM), and this activation is selective for the nat-20(S)-OHC enantiomer. Nat-20(S)-OHC synergizes with the SMO agonist SAG, suggesting an allosteric effect. Nat-20(S)-yne is a form of nat-20(S)-OHC with a terminal alkyne group, which can be used in linking reactions known as click chemistry. Click chemistry involves highly dependable and specific azide-alkyne bioconjugation reactions and can be used to capture or immobilize bioactive molecules. Thus, nat-20(S)-yne has been conjugated with magnetic beads to demonstrate that nat-20(S)-OHC directly binds SMO.

VU0424465 is a mGlu5-selective allosteric agonist.