Author Topic: Cocaine receptor binding ligands  (Read 1117 times)

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Cocaine receptor binding ligands
« on: April 22, 2003, 12:07:00 AM »
3-(substituted phenyl)-2-(substituted)-phenyltropane analogs.

Patent US2003023090


The invention relates to novel compounds which show high affinity for cocaine receptors in the brain, particularly dopamine and serotonin transporter sites. The compounds may be used as imaging or pharmaceutical agents, in the diagnosis of drug addiction, depression, anorexia and neurodegenerative diseases.

"The compounds of the present invention may be administered for their activities as a surrogate agonist medicine for cocaine, nicotine, alcohol, amphetamine and other psychostimulant abuse. Because of their favorable binding characteristics to transporters of neurotransmitters, they may be used for inhibiting the uptake of dopamine, norepinephrine, serotonin and other monoamines."

These compounds have an up to 10x longer activity than cocaine in rats.