Mason, N. Scott; Hewlett, William A.; Ebert, Michael H.; Schmidt, Dennis E.; de Paulis, Tomas published the artcile< Labeling of (S)-des-4-amino-4-[125I]iodozacopride (DAIZAC), a high-affinity radioligand for the 5-HT-3 receptor>, Recommanded Product: (S)-3-Amino-1-azabicyclo[2.2.2]octane, the main research area is desaminoiodozacoprride iodine 125 preparation serotoninergic receptor.
We have prepared (S)-5-chloro-3-[125I]iodo-2-methoxy-N-(1-azabicyclo[2.2.2]oct-3-yl)-benzamide ([125I]DAIZAC, [125I]-3) as a radioligand for characterization of the 5-HT-3 receptor. Preparation of the 3-tri-n-butylstannyl precursor was accomplished from the corresponding unlabeled DAIZAC by reaction with bis(tributyltin). Treatment of the precursor with 5 mCi of Na125I and chloramine-T in dilute HCl gave 2.58 ± 0.22 mCi (52%) of [125I]DAIZAC with >98% radiochem. purity and 1500 Ci/mmol specific activity. Saturation anal. of the binding of [125I]DAIZAC to rat brain homogenates showed a single binding site with a receptor d. Bmax of 0.66 ± 0.03 pmol/g and a receptor affinity KD of 0.15 ± 0.01 nM. Compared to [125I]iodozacopride, we find the 20-fold higher affinity and easy preparation of [125I]DAIZAC to be advantageous for in vitro identification of brain 5-HT-3 receptors.
Journal of Labelled Compounds & Radiopharmaceuticals published new progress about 5-HT3 receptors Role: ANT (Analyte), BSU (Biological Study, Unclassified), ANST (Analytical Study), BIOL (Biological Study). 120570-05-0 belongs to class quinuclidine, and the molecular formula is C7H14N2, Recommanded Product: (S)-3-Amino-1-azabicyclo[2.2.2]octane.
Referemce:
Quinuclidine – Wikipedia,
Quinuclidine | C7H13N | ChemSpider