(±)α-Phenyl-β-(3,4-dimethoxy)- and (±)α-Phenyl-β-(3,4-dihydroxy)phenethylamines: Potential Probes for Nicotinic Acetylcholine Receptor-Ion Channel Molecule from Torpedo Electric Organ

Add time:07/14/2019    Source:sciencedirect.com

The synthesis of some Nmethyl, N-alkyl derivatives of (±)α-phenyl-β-(3,4-dimethoxy)- and (±)α-phenyl-β-(3,4-dihydroxy)-phenethylamines was achieved. These compounds were shown to bear certain structural features of acetylcholine (ACh), as well as phencyclidine (PCP). The latter was reported to act as a specific probe for the nicotinic ACh receptor-ion channel molecule from Torpedo electric organ. Biochemical binding studies revealed that for the nicotinic ACh receptor, the 3,4-dimethoxy derivatives behaved as blockers for the binding interaction of [3H]ACh, whereas the 3,4-dihydroxy analogues stimulated such binding. On the other hand, all of the tested phenethylamines exhibited potent blockade towards [3H]PCP binding interactions. The results indicated that the tested compounds might be applied as potential probes for the ACh receptor-ion channel molecule.

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