ar a 2

AR-A 2 is a selective 5-HT1B receptor antagonist with high affinity to guinea pig cortex 5-HT1B/1D and recombinant guinea pig 5-HT1B receptors (Ki: 0.24 and 0.47 nM), exhibiting a 10-fold lower affinity to guinea pig 5-HT1D receptor (Ki: 5 nM).

A2AR/A2BR antagonist 1 (compound 7ai) acts as a dual antagonist to A2AR and A2BR with IC50 values of 11.2 nM and 6.4 nM, respectively. Additionally, A2AR/A2BR antagonist 1 enhances T cell-mediated cancer cell death.

A2AR-agonist-1 (N-(2-(1H-Indol-3-yl)ethyl)adenosine) is a potent A2AR and ENT1 agonist (Ki: 4.39 and 3.47 for A2AR and ENT1. It targets the Adenosine A2A Receptor and Adenosine Transporter for Neuroprotection.

1H-Pyrrolo[2,1-c][1,2,4]benzothiadiazine, 2,3,3a,4-tetrahydro-, 5,5-dioxide, (3aR)- is a low activity isomer of S 18986. S 18986 is a AMPA receptor positive modulator with EC2 (Concentration that doubles the intensity of the AMPA-induced current) of 35 μM.

β2AR/M-receptor agonist-2 is a dual-function compound acting as a muscarinic antagonist and β2 adrenoceptor agonist (MABA). It demonstrates significant activity towards the β2 adrenoceptor with an EC50 of 3.7 nM and exhibits affinity for the human cloned M3 receptor with a Ki of 0.73 nM. This potent bronchodilator holds potential for research in chronic obstructive pulmonary disease (COPD) treatment.

Cyclopenta[c][1]benzopyran-8-ol, 1,2,3,3a,4,9b-hexahydro-4-(4-hydroxyphenyl)-, (3aR,4S,9bS)-rel- is an estrogen receptor beta (ERβ) agonist.

β3-AR agonist 2 is a potent and selective agonist of β3-adrenergic receptor (β3-AR with an EC50 of 8 nM).

A1AR antagonist 2 (compound 18h) is a potent antagonist of the A1 adenosine receptor (AR) with Ki values of 1.49, 10.2, and 50.1 nM for hA1, hA2A, and hA2B, respectively [1].

AR antagonist 2 (compound 58) is a potent inhibitor of the androgen receptor (AR) with an IC50 of 0.95 μM.

AR Degrader-2 (Compound 2) is a degrader of the androgen receptor (AR), exhibiting a DC50 range of 0.3-0.5 μM in VCaP cells.

5-HT1AR Agonist 2 (Compound 4f) is a potent agonist of the 5-HT1A receptor with a Ki value of 10.0 nM. It also binds to SERT, D2, and 5-HT6 receptors with Ki values of 2.8 nM, 23 nM, and 192 nM, respectively. Furthermore, this compound demonstrates stability in microsomes and induces hypothermia in mice.

hA3AR agonist 2 is a potent activator of A3AR, with a Ki value of 3.5 nM.

β2AR agonist 2 (compound 8a) is an agonist of the β2-adrenergic receptor (β2AR). It is a saturated azacyclic compound featuring a 4- to 7-membered heterocycle. The compound has a chiral structure in the -R form by incorporating a carbon with a requisite hydroxyl group, which significantly stimulates glucose uptake in skeletal muscle cells, thereby enhancing cellular glucose uptake (GU). β2AR agonist 2 is applicable in the study of type 2 diabetes (T2D).

β2AR agonist 4 (compound A19) is an effective selective agonist for the β2-adrenoceptor (β2-Adrenoceptor), exhibiting an EC50 of 3.7 pM. In a rat model with COPD, β2AR agonist 4 reduces the elevation of inflammatory factors and leukocytes, thereby improving lung function.

Compound 4, known as β2AR ligand 1, serves as a bivalent ligand for the β2-adrenergic receptor (β2AR) at both the orthosteric binding site (OBS) and the metastable binding site (MBS).

α2AR agonist 1 (compound S6a) is a morpholinopyrimidinone that serves as an agonist for the α2-adrenergic receptor (α2AR). This compound elicits a concentration-dependent relaxation in precontracted aortic rings induced by phenylephrine (pEC50=6.81). Additionally, α2AR agonist 1 elevates levels of NOx and NO in HUVEC.

A2AR modulator-1 (Compound 45) is a selective negative allosteric modulator of the adenosine A2a receptor (A2aR), with an IC50 value of 9 nM. It reduces the affinity of endogenous adenosine for the receptor and inhibits the activation of the cAMP signaling pathway. A2AR modulator-1 effectively restores pCREB phosphorylation in CD4+ T cells, reverses immunosuppression in the tumor microenvironment, and shows potential in inhibiting tumor growth and metastasis in a triple-negative breast cancer model.

5-HT2AR ligand 1 (Compound 2 cis) is a ligand for the 5-HT2AR with nanomolar affinity (Ki: 32 nM). It can induce the recruitment of β-arrestin2 and is applicable for research in neurological disorders.

((2S,7aR)-2-Fluorotetrahydro-1H-pyrrolizin-7a(5H)-yl)methanol-d2, also known as ((2S,7aR)-2-Fluorotetrahydro-1H-pyrrolizine-7a(5H)-methanol-d2), is the deuterium-labeled form of ((2S,7aR)-2-Fluorotetrahydro-1H-pyrrolizin-7a(5H)-yl)methanol.

5-HT2AR-IN-1 (Compound Ie) is an orally active inhibitor of the serotonin 2A receptor (5-HT2AR) with antidepressant effects. It reduces the expression of 5-HT2AR and levels of SERT protein. This compound holds potential for research in central nervous system (CNS) conditions, including depression and addiction-related disorders.

A2A/A1 AR antagonist-1 (compound 1a) is a potent dual antagonist with Ki values of 5.58 nM and 24.2 nM for A2A and A1 AR, respectively, demonstrating potential for ischemic stroke research [1].

The compound is an A1/A3 adenosine receptor antagonist that aids in the treatment of (neurological) inflammatory diseases.

5-HT6/5-HT2AR antagonist-1 is a potent dual antagonist for the 5-HT6 and 5-HT2A receptors, demonstrating high efficacy with K_i values of 11 nM and 39 nM, respectively [1].

C5aR-IN-2 is a potent inhibitor of C5aR, offering potential for studying inflammatory diseases.