Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1986-01-31
1988-08-09
Hollrah, Glennon H.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
558 17, 546229, 514514, C07D21128, A61K 3126, A61K 31445
Patent
active
047628464
ABSTRACT:
A derivative of phencyclidine (1) bearing an isothiocyanate moiety on the meta position of the aromatic ring (3; Metaphit as methanesulfonate and HCl salt) has been synthesized and identified as a rapid and specific site-directed acylating agent of the [.sup.3 H]-phencyclidine binding site in rat brain homogenates. Additional related compounds to Metaphit are Thiophit (oxalate salt), Ethylphit (HCl salt), and Isopropylphit (HCl salt).
REFERENCES:
patent: 3097136 (1963-06-01), Godefroi et al.
patent: 4196185 (1980-04-01), Focella et al.
Quirion et al, Evidence for an Endogenous Peptide Ligand for PCP Recepter, Peptides vol. 5, pp. 967-973 (1984).
Itzhak et al, (I), New Analgesic Drugs Derived from PCP J. Med. Chem 24, pp. 496-499 (1981).
Itzhak et al, II, Receptor Binding and Antinociceptive Prop. of PCP Opiate-Like Derivatives, European J. Pharmacology, 72, pp. 305-311, (1981).
CA 95:24749p, Johnson et al, Synthesis of Amine Derivatives of PCP (1981).
Contreras Patricia
Jacobson Arthur E.
Lessor Ralph A.
Mattson Mariena V.
O'Donohue Thomas L.
Dinner D. L.
Hollrah Glennon H.
Roberts, Jr. John S.
The United States of America as represented by the Department of
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