A convenient synthesis of the muscarinic cholinergic antagonist (R)-[N-methyl- H]quinuclidinyl benzilate methiodide.

A useful synthesis of (R)-[N-methyl- H]quinuclidinyl benzilate methiodide is described with the product characterized by thin-layer chromatography (TLC), high-performance liquid chromatography (HPLC), tritium nuclear magnetic resonance (NMR), and mass spectrometry (MS). Several methods are provided to purify the radioligand, and its storage and stability are also discussed.

Dopamine: approaches to its side chain labeling with tritium.

Methods are presented to tritiate the side chain of dopamine.

Synthesis of [15, 16- ³H] beta-funaltrexamine.

Beta-funaltrexamine is a unique irreversible antagonist for the mu-opiate receptor and would be useful as a tritiated radioligand. Starting from high specific activity [15, 16-³H] naltrexone, [15, 16-³H] beta-funaltrexamine was synthesized and characterized by means of a two-step reductive amination-acylation process.

Mu opiate active substances trefentanil and naloxonazine: tritiation at high specific activity.

Methods are presented to synthesize and characterize [propyl-(3)H] trefentanil 3 and [propenyl-(3)H] naloxonazine 6.

Tritium labelling of dopaminergic ligands domperidone and (+/-)-7-hydroxy DPAT.

Methods are presented for tritiating the D2 specific dopaminergic antagonist domperidone and D3 specific dopaminergic agonist (+/-)-7-hydroxy DPAT. Techniques to characterize the products of the tritiation are also given.