Radioligand

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).

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.

FAUC-365 is a D3 dopamine receptor agonist.

A-317920 is an inverse agonist radioligand.

GSK-215083 is a PET radioligand for the 5-HT6 receptor. GSK 215083 is a quinoline based compounds and acts by antagonising the 5-HT6 receptor. GSK-215083 binds to receptors 5-hydroxytrypamine-6 (5HT6) in the striatum and 5-hydroxytryptamine-2A (5HT2A) in

GSK931145 is a positron emission tomography (PET) radioligand, it is suitable for quantifying glycine transporter (GlyT1) availability in the living brain.

PD 140376 is a highly selective antagonist radioligand for the cholecystokinin(B)-gastrin receptor in guinea pig gastric mucosa & cerebral cortex in the peripheral and central nervous systems.

AH-9700 free base is use for treatment of urge incontinence and pollakiuria.In a radioligand binding study,AH-9700 free base showed high affinities for sigma receptors and it produces a marked inhibitory effect on the micturition reflex (i.e. bladder capacity-increasing effect) in experimental animals with normal bladder functions.

Altanserin can binds to the 5-HT2A receptor. Labeled with the isotope fluorine-18 it is used as a radioligand in positron emission tomography (PET) studies of the brain.

Altanserin tartrate is a compound that binds to the 5-HT2A receptor. Labeled with the isotope fluorine-18 it is used as a radioligand in positron emission tomography (PET) studies of the brain.

AZD-2184 is a radioligand for detecting beta-amyloid deposits.

Flutafuranol, also known as AZD 4694 and NAV4694, is a bio-active chemical. AZD4694 shows high affinity for beta-amyloid fibrils in vitro (K(d) = 2.3 +/- 0.3 nM). The fluorine-18 labeled AZD4694 may have potential for PET-visualization of cerebral beta-am