What is radioligand binding used for?
Radioligand binding is widely used to characterize receptors and determine their anatomical distribution, particularly the superfamily of seven transmembrane-spanning G protein-coupled receptors for both established transmitters such as endothelin-1 and an increasing number of orphan receptors recently paired with …
What is a radioligand binding assay?
Radioligand binding assays provide sensitive and quantitative information about guanine nucleotide protein G protein-coupled receptor (GPCR) expression and affinity for a wide variety of ligands, making them essential for drug structure-activity studies and basic GPCR research.
What does BMAX mean?
Bmax is the maximum specific binding in the same units as Y. It is the specific binding extrapolated to very high concentrations of radioligand, and so its value is almost always higher than any specific binding measured in your experiment. Kd is the equilibrium dissociation constant, in the same units as X.
What is radioligand therapy?
Radioligand therapy is an innovative approach to treating certain types of cancer. It delivers radiation to specifically targeted cancer cells, with a minimal effect on healthy cells.
How radioligand bindings work?
They are performed by incubating a range of concentrations of the unlabeled test compound with a fixed concentration of radioligand and measuring the IC50 (nM) of the test compound to competitively inhibit binding of the radiolabeled ligand to its receptor.
What is KD in pharmacology?
The equilibrium dissociation constant (Kd) represents the inverse of the affinity of the drug for the receptor and can be defined as; Equilibrium dissociation constant: Kd = K off K on = [ L ] [ R ] [ LR ]
How do you calculate Kd and Bmax?
- = [receptor]× x × This equation is derived as follows: When you substitute [ligand] with x and [re-
- (8) Inserting and rearranging leads to.
- y = =
- y × (Kd + x) = Bmax × x. (12)
- You will get Kd and Bmax as results. Note that, when the concentration of the ligand (the.
- Kd + Kd. 2Kd.
What is BMAX in biology?
Bmax is the total density (concentration) of receptors in a sample of tissue. To refer to the concentration of available (free) receptors, terms Bavail or B’max can be used.
What PSMA 617?
Lu-PSMA-617 is an investigational PSMA-targeted radioligand therapy for metastatic castration-resistant prostate cancer. It is a type of precision cancer treatment combining a targeting compound (ligand) with a therapeutic radioisotope (a radioactive particle)11-13.