Hewlett, William A.; De Paulis, Tomas; Mason, N. Scott; Schmidt, Dennis E.; Trivedi, Bakula L.; Zhang, Zhang-Jin; Ebert, Michael H. published the artcile< Synthesis and radiolabeling of (S)-4-amino-5-iodo-2-methoxy-N-(1-azabicyclo[2.2.2]oct-3-yl)benzamide, the active enantiomer of [125I]iodozacopride, and re-evaluation of its 5-HT3 receptor affinity>, Name: (S)-3-Amino-1-azabicyclo[2.2.2]octane, the main research area is iodozacopride radiolabeled preparation receptor affinity; HT3 receptor affinity radiolabeled iodozacopride.
Unlabeled (S)-iodozacopride was prepared in seven steps from 4-aminosalicylic acid via alk. hydrolysis of its 4-acetamide derivative Catalytic hydrogenation of (S)-iodozacopride gave dechloro-(S)-zacopride, identical to that obtained from (S)-3-aminoquinuclidine and 4-amino-2-methoxybenzoic acid via its corresponding 1-imidazole derivative Radioiodination to produce (S)-[125]iodozacopride was accomplished by treatment of dechloro-(S)-zacopride with 5 mCi sodium 125iodide and chloramine-T in hydrochloric acid. Purification of the reaction products using an HPLC system capable of detecting chlorinated side-products revealed a mixture of 2.1 mCi (1.3 nmol) (S)-[125I]iodozacopride and (S)-zacopride (1.5 nmol). Saturation anal. of the binding of the purified (S)-[125I]iodozacopride to whole rat brain homogenates gave an estimated KD of 1.10±0.07 nM. As anticipated, this is approx. half the KD reported for binding of racemic [125I]iodozacopride, and differs from the previously reported value by an order of magnitude. Anal. of the apparent binding affinity of a 1:1 mixture of (S)-[125I]iodozacopride and (S)-zacopride suggests that the previous result may have been confounded by contamination of the product with unlabeled (S)-zacopride. Competition anal. of the displacement of (S)-[125I]iodozacopride binding by unlabeled (S)-iodozacopride and (S)-zacopride gave Ki values of 0.95 and 0.21 nM, resp.
Chemical & Pharmaceutical Bulletin published new progress about 5-HT3 receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 120570-05-0 belongs to class quinuclidine, and the molecular formula is C7H14N2, Name: (S)-3-Amino-1-azabicyclo[2.2.2]octane.
Referemce:
Quinuclidine – Wikipedia,
Quinuclidine | C7H13N | ChemSpider