Radioligand

FAUC-365 is a D3 dopamine receptor agonist.

Sigma-2 Radioligand 2 (compound 4) exhibits low nanomolar affinity for the σ2 receptor (Ki=2.30 nM) and high subtype selectivity (Ki(σ1)/Ki(σ2) > 1500).

CB2 PET Radioligand 1 (compound [18F]9) is a positron emission tomography (PET) radioligand with high affinity for the human cannabinoid receptor 2 (hCB2, Ki=7.7 nM). It is synthesized via Cu-mediated 18F-fluorination and demonstrates significant brain uptake in a mouse model of neuroinflammation [1].

Sigma-2 Radioligand 1 (compound 1) serves as a selective Sigma-2 ligand, demonstrating favorable biodistribution in mice and robust in vivo activity in rats. The [18F] modified version of Sigma-2 Radioligand 1 enhances the visualization of tumors in micro-PET/CT imaging by providing high tumor uptake and an impressive tumor-to-background ratio. Additionally, experiments confirm that this compound binds with high specificity to U87MG glioma xenografts [1].

Lusaperidone (R107474) is a potent α2-adrenergic receptor antagonist, a potential radioligand for the α (2)-adrenergic receptor, with inhibitory effects on α2A and α2C, with Ki values of 0.13 and 0.15 nM, respectively.

MRS 1754 is a selective antagonist radioligand for the A2B adenosine receptor, exhibiting very low affinity for A1 and A3 receptors in both humans and rats.

(S)-Desmethyl-NNC112 ((+)-Desmethyl-NNC112) is a selective PET radioligand that binds to D-dopamine receptors.

Arotinolol hydrochloride(Arotinolol HCl) is a non-selective α/β-adrenergic receptor blocker.Arotinolol hydrochloride inhibits the binding of the radioligand 125I-ICYP to the 5HT1B-hydroxytryptamine receptor. Arotinolol hydrochloride is an antihypertensive and anti-obesity agent that improves aortic stiffness in rats and is used to study obesity-related diseases.

3-aminopropylphosphonic acid (3-APPA) is a phosphonic analog of GABA that acts as a partial agonist of GABAB receptors (IC50 = 1.5 μM in a radioligand binding assay).

The FAP-targeting peptide for FXX489 constitutes the peptide moiety of FXX489, suitable for biochemical assays and drug synthesis studies. FXX489 is a fibroblast activation protein (FAP)-targeting ligand employed in radioligand therapy (RLT) for multiple cancers.

Arotinolol is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker. Arotinolol also shows potency for inhibiting the binding of the radioligand [125I-ICYP] to [5HT1B-serotonergic] receptor sites. It is an antihypertensive agent.

MLi-2 is a structurally novel, highly potent, and selective LRRK2 kinase inhibitor with central nervous system activity. MLi-2 exhibits exceptional potency in a purified LRRK2 kinase assay in vitro (IC50 = 0.76 nM), a cellular assay monitoring dephosphorylation of LRRK2 pSer935 LRRK2 (IC50 = 1.4 nM), and a radioligand competition binding assay (IC50 = 3.4 nM).

PCS1055 dihydrochloride is an effective, selective, and competitive muscarinic M4 receptor antagonist (IC50: 18.1 nM and a Kd: 5.72 nM). PCS1055 dihydrochloride is also a potent AChE inhibitor (IC50 s: 22 nM and 120 nM for electric eel and human AChE, res

PK14105 has been evaluated biologically as a potential radioligand for positron emission tomography (PET) studies targeting peripheral benzodiazepine binding sites (PBBS) receptors. When administered to rats with unilaterally lesioned striata, PK14105 was observed to quickly cross the blood-brain barrier, displaying significant radioactivity retention in the lesioned striatum, in contrast to the unlesioned striatum or cerebellar vermis. Additionally, PK14105 has the capability to inhibit receptor ligands, calcium channel ligands, and co-transporters in all salivary glands.

SB 224289 is a selective antagonist of 5-HT1B receptor with pKi of 8.2. It is a centrally active following oral administration in vivo. SB 224289 displays 60-fold selectivity over 5-HT1D, 5-HT1A, 5-HT1E, 5-HT1F, 5-HT2A and 5-HT2C receptors in radioligand

SDM-8 is a PET radioligand with a high affinity for SV2A, characterized by a Ki of 0.58 nM. This compound is utilized in the research of Alzheimer's disease.

AZ12943203 (Compound 13e) is a PET radioligand targeting GSK-3, with a Kd of 2.94 nM. It demonstrates significant inhibitory potency against GSK-3β (IC50: 4.44 nM) and specifically binds to GSK-3-rich regions in the rodent brain. AZ12943203 is applicable for imaging neurodegenerative diseases, particularly Alzheimer's disease.

OncoACP3 (Compound s43) is a high-affinity radioligand for prostatic acid phosphatase (ACP3). When labeled with lutetium-177, OncoACP3 selectively accumulates in tumors expressing the enzyme in HT1080.hACP3 and PC3.hACP3 xenograft mouse models, demonstrating potent antitumor activity and exceptional tumor-selective payload deposition. OncoACP3 is utilized for prostate cancer research.

RGD-DA6 is an αvβ3-targeting ligand composed of RGDfK (an RGD peptide targeting integrin αvβ3), DOTADG, d-Glu, Lys, AMBA, and IPBA. Through radiolabeling, RGD-DA6 forms an αvβ3-targeted radioligand for high-contrast tumor imaging and improved anticancer efficacy.

BMT-136088 is a radioligand suitable for positron emission tomography (PET) imaging of idiopathic pulmonary fibrosis.

H3R antagonist 6 (Compounds 3) (H3-2406) is a histamine receptor 3 (H3R) antagonist with an IC50 of 5.6 nM. The 18F-labeled version exhibits high radiochemical yield, molar activity, and moderate brain uptake, although it shows off-target binding with the Sigma-1 receptor. It serves as a radioligand for positron emission tomography (PET) imaging in the study of central nervous system (CNS) diseases.

H3R antagonist 7 (compounds 4) is a histamine subtype 3 receptor (H3R) antagonist with a Ki value of 3.15 nM. It can potentially be used as a PET radioligand in the study of central nervous system (CNS) diseases.

OX2-2303 is a potent and selective orexin-2 receptor (OX2R) antagonist with excellent binding affinity to OX2R (Ki= 0.1 nM) and over 890-fold selectivity for OX2R over OX1R. OX2-2303 can serve as a positron emission tomography (PET) radioligand for research related to the central nervous system (CNS).

PSN09 is a high-affinity agonist of PSAM4-GlyR and PSAM4-5-HT3 receptors that can cross the blood-brain barrier. The compound, labeled with 18F, serves as a radioligand for PET imaging in non-human primates.