brain-imaging

Sodium Glucoheptonate is used as a kit for Tc-99m radiolabeling, as well as for metal cleaning, mercerizing, paint stripping and aluminum etching. Among other things, Tc-99m glucoheptonate is a kidney and brain imaging agent that can be used to detect brain tumors.

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.

[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.

1-1(Z)-Octadecenyl-2-docosahexaenoyl-sn-glycero-3-PE (18:0p/22:6-PE) is a lipid identified in rat brain tissue using mass spectrometry imaging techniques. It exhibits specific structural and distribution properties, allowing the differentiation of isomers of various fatty acid chains through refined methods.

TNIR7-1A is a fused cycloheptatriene-BODIPY derivative that is optimized for near-infrared (NIR) imaging characteristics (Ex/Em = 600/774 nm in PBS) and exhibits high affinity and specificity for neurofibrillary tangles (NFT) in vitro. Additionally, TNIR7-1A can effectively penetrate the blood-brain barrier.

CHL2310 is an inhibitor of CYP46A1 with an IC50 of 0.11 nM and a Kd of 0.37 nM. It is capable of crossing the blood-brain barrier. When labeled with radioactive [18F], CHL2310 can serve as a PET imaging agent.

BF-170 is a selective tau fiber-binding agent with an EC50 of 221 nM. It demonstrates excellent blood-brain barrier penetration, reaching a concentration of 9.1% ID/g in brain tissue 2 minutes after intravenous injection in mice (with a clearance rate of 0.25% ID/g at 30 minutes). BF-170 can serve as a probe for imaging tau protein pathology in Alzheimer's disease (AD). It plays a significant role in early-stage Alzheimer's disease studies and holds promise for imaging research in tau-related neurodegenerative diseases.

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.

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.

P2Y12R ligand-1 (Compound 41) is a high-affinity P2Y12 receptor ligand with a Ki of 17.1 nM. The [18F]-labeled version of P2Y12R ligand-1 is suitable for research involving brain PET imaging.

SK60 is the dimethylated derivative of GSK321, exhibiting high selectivity for IDH1R132H with a potent IC50 of 14.5 nM. It can be utilized as a fluorescent label and tracer for [18F] brain imaging.

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.

Sodium Glucoheptonate Dihydrate is available as a Tc-99m radiolabeling kit. Tc-99m glucoheptonate is a kidney and brain imaging agent for brain tumor detection.

Altanserin is a highly specific 5-HT2A receptor antagonist, frequently used as a radiolabeled ligand for PET imaging to evaluate brain receptor distribution.

CRANAD-28 is a blood-brain barrier (BBB) penetrating two-photon imaging probe capable of visualizing amyloid plaques and labeling plaques and cerebral amyloid angiopathy.

Desmethyl-HD-800 is a PET precursor of preparing radiolabel [11C]HD-800, a high affinity brain penetrant PET tracer for imaging microtubules.

SP203 is a radioligand for brain metabotropic glutamate receptor imaging.

CuATSM is a cell-permeable copper complex and PET tracer for selective hypoxia imaging. It also exhibits neuroprotective potential in ALS and Parkinson's disease by mitigating oxidative damage.

THK-5117 is an arylquinoline derivative with the potential as a PET probe for tau imaging. THK-5117 shows high binding affinity to tau fibrils with a Ki value of 10.5 nM. THK-5117 also shows high binding affinity to tau protein aggregates and tau-rich Alzheimer disease (AD) brain homogenates [1].

THK-5105, an arylquinoline derivative, demonstrates high binding affinity for tau fibrils, protein aggregates, and tau-rich Alzheimer's disease (AD) brain homogenates, indicating its potential as a tau imaging PET (Positron Emission Tomography) probe with the radiolabeled version, 18F-THK-5105 [1].

Astrophloxine is a fluorescent imaging probe that targets antiparallel dimers and can be used to detect aggregated Aβ in brain tissue and cerebrospinal fluid samples from Alzheimer's disease (AD) mice.

TRV-7019 is a butyrylcholinesterase-targeting radioligand capable of penetrating the blood-brain barrier (BBB) for brain imaging. It is utilized for diagnosing conditions such as amyloid diseases, multiple sclerosis, brain tumors, or to assess butyrylcholinesterase activity [1].

PBR28, a TSPO modulator, holds potential for preventative research in Pulmonary Arterial Hypertension (PAH) and is instrumental in brain positron emission tomography (PET) imaging studies through its capacity for radioactive labeling to trace the 18 KDa transporter (TSPO) [1].

AMCPy, a potent electron paramagnetic resonance (EPR) brain imaging agent, boasts excellent lipophilicity, facilitating its penetration through the blood-brain barrier (BBB) [1].