An Affinity Label for α2‐Adrenergic Receptors in Rat Brain

• DOI: 10.1111/j.1432-1033.1982.tb06814.x
• Publication Date: 2005-03-03T22:08:07Z
• Authors: Daphne ATLAS; Yael PLOTEK; Ian MISKIN
• Keywords: Alpha-1A adrenergic receptor

Clonidine, a potent and highly selective α 2 ‐adrenergic agonist of the central nervous system, was modified. Insertion strong alkylating isothiocyanate group (NCS) group, at its aromatic residue, makes clonidine potential affinity label receptors. In displacement [ 3 H]clonidine p ‐[ H]aminoclonidine from rat brain membrane preparations, clonidine‐NCS demonstrates high for receptors ( K d = 50 mM). The covalent labelling ‐receptors requires higher concentrations irreversible ligand (1–70 μM), thus indicating possible non‐productive interactions environment receptor site. Only partial protection is observed with reversible ‐agonist. new analog appears to be general might serve as probe these