Sigma brain receptor ligands and their use

Details Sigma brain receptor ligands and their use Sigma brain receptor ligands and their use

1986-07-10

1987-11-24

Killos, Paul J.

Organic compounds -- part of the class 532-570 series

Organic compounds

Amino nitrogen containing

514634, C07C12912

Patent

active

047090944

ABSTRACT:
1,3-Disubstituted-guanidines, e.g., of the formula ##STR1## wherein R and R' are hydrocarbon groups which preferably are the same, e.g., 1,3-dibutyl-guanidine, 1,3-diphenyl-guanidine and 1,3-di-o-tolyl-guanidine, are highly selective ligands for sigma brain receptors and are useful in the diagnosis and treatment of hallucination associated psychotic mental illness and chronic mental depression. Tritium labeled 1,3-di-(o-tolyl)-guanidine is useful as a screening tool for compounds having selective sigma receptor binding activity, as it is displaced from isolated mammalian brain membrane to which it is bound portionately to the activity of such a compound.

REFERENCES:
patent: 1642180 (1927-09-01), Scott
patent: 1672431 (1928-06-01), Schotte
patent: 1915922 (1931-06-01), Christmann
patent: 2633474 (1953-03-01), Beaver

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