positron

DOTA-NHS-ester is a linker for affibody molecules with applications in small animal PET, SPECT, and CT. It can be used to label radiotherapeutic agents or imaging probes for tumor detection.

HG-10-102-01 is an inhibitor of leucine-rich repeat kinase 2 (LRRK2, IC50 of 20.3 nM).

Benperidol (Anquil) is a butanone analog with antipsychotic and stabilizing properties, and has been shown to be effective in blocking D2 receptors.Benperidol can be used in positron emission tomography (PET) scanning to measure D(2) dopamine receptor binding in vivo.Benperidol has been shown to be effective in blocking D2 receptors in vivo.Benperidol has been shown to be effective in blocking D2 receptors in vivo.

MK-7337 is a high-affinity α-synuclein PET (positron emission tomography) ligand. Isotope-labeled MK-7337 serves as a PET tracer for imaging neurodegenerative diseases such as Parkinson's disease.

DPA-714 is a high-affinity translocator protein (TSPO) ligand (Ki=7 nM) designed with a fluorine atom, allowing labeling with fluorine-18 for in vivo imaging via positron emission tomography. [18F]DPA-714 successfully enables specific imaging of inflammation in various neuroinflammation models and a brain tumor model.

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.

Verubulin (MPC 6827) is a potent microtubule blocker with cytotoxic and potentially anticancer activity that disrupts newly formed blood vessels in xenografts, and can be used to image microtubules (MTs) using positron emission tomography (PET).

MK-6240 is a tau positron emission tomography (PET) tracer for neurofibrillary tangles (NFTs) that exhibits high specificity and selectivity in binding to NFTs.

T807 (AV-1451) is a novel tracer of tau positron emission tomography (PET).

DOTA-NHS-ester (TFA) serves as a linker for affibody molecules, and it is applicable in small animal imaging techniques such as positron emission tomography (PET), single-photon emission computed tomography (SPECT), and CT scans. It can also be used to label radiopharmaceuticals or imaging probes for tumor detection.

PARP1-IN-29 is an orally active PARP-1 inhibitor with an IC50 of 6.3 nM. When labeled with [18F], PARP1-IN-29 can be utilized for positron emission tomography (PET) imaging, specifically targeting PARP-1 in tumors. This compound is useful in oncology and imaging studies, particularly for detecting PARP-1 activity in cancer.

[11C]MeS-IMPY exhibits a higher binding affinity for β-amyloid plaques extracted from Alzheimer's disease (AD) brains or AD brain homogenates than IMPY, with Ki values of 7.93 nM and 8.95 nM, respectively. [11C]MeS-IMPY is a potential radioactive ligand for positron emission tomography (PET) imaging of β-amyloid plaques.

PXT-012253 is a positron emission tomography (PET) ligand targeting mGluR4, designed to bind to its allosteric sites. This compound is useful for research related to Parkinson's disease and levodopa-induced movement disorders.

N-Methylspiroperidol is a D2 receptor antagonist. This compound can be labeled as [18F]N-Methylspiroperidol, which allows for the investigation of its interaction with 5-HT2C receptors via PET (positron emission tomography), as well as examining the competition and impact of neurotransmitters like dopamine on these receptors.

Tau ligand-1 (Compound 75) is a ligand of aggregated tau protein that can penetrate the blood-brain barrier. In tissues affected by Alzheimer's disease, progressive supranuclear palsy, corticobasal degeneration, and Pick's disease, Tau ligand-1 shows high affinity for aggregated tau protein, with equilibrium dissociation constants (KD) ranging from 1 to 3.8 nM. It holds potential as a positron emission tomography (PET) tracer for imaging studies of tau-related diseases within the central nervous system.

FAP-IN-5 (Compound 4a) is an FAP inhibitor with an IC50 of 1.7 nM. It is applicable in studies involving tumor positron emission tomography (PET) imaging.

KR31173 is an AT1 antagonist with an IC50 of 3.27 nM. When labeled with the 11C isotope, KR31173 can be used as a tracer for positron emission tomography (PET). In mice, KR31173 exhibits favorable biodistribution and pharmacological characteristics. It selectively binds to organs in CD-1 mice known to have a high density of AT1 angiotensin receptors.

Lissamine rhodamine B, a new Radiotracer, is used for Imaging Tumors by Positron Emission Tomography.

PB94 is a selective inhibitor of HDAC11 with an IC50 value of 108 nM. This compound can be radiolabeled as [11C]-PB94 for use in positron emission tomography (PET) to study brain uptake and metabolic characteristics in living animals. Furthermore, PB94 has been shown to alleviate neuropathic pain in mice and is applicable for research into neurological indications.

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

FAP-IN-6 (Compound 21) is a selective FAP inhibitor with an IC50 of 13 pM. It demonstrates high metabolic stability, and its 18F-labeled form serves as a tracer for positron emission tomography (PET). FAP-IN-6 is relevant for studying the cancer microenvironment.

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.

CB2R ligand-1 (Compound L14) is a selective cannabinoid receptor type 2 (CB2R) ligand with a Ki of 0.16 nM, demonstrating higher affinity for CB2R over CB1R. It can serve as a tracer for positron emission tomography (PET) imaging of neurodegenerative diseases, inflammation, and cancer.

3-Deoxy-3-fluoro-D-fructose (Compound 12) is a derivative of 2,5-Anhydro-D-mannitol. It serves as a selective probe for hexose transporter 5 (GLUT5). This compound inhibits the transport of [14C]-labeled D-fructose by GLUT5, with IC50 values of 1.16 µM in EMT-6 cells and 2.37 µM in MCF-7 cells. Additionally, 3-Deoxy-3-fluoro-D-fructose is useful for positron emission tomography (PET) imaging in cancer studies.