Kappa opioid receptor agonists

Details Kappa opioid receptor agonists Kappa opioid receptor agonists

1995-12-05

1998-09-08

McKane, Joseph

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514429, 514646, 514649, 514414, 514415, 514419, 514422, 548469, 548495, 548517, 548566, 548569, 548571, 548577, 548578, 548579, 548506, 548523, 560 39, 560 41, 560 48, 560 51, 562 30, 562 37, 562 44, 562433, 562439, 562440, 562443, 562444, 562455, 564123, 564161, 564182, A61K 31135, A61K 3140, A61K 31405, C07C 69616, C07C23714, C07D20709, C07D20912

Patent

active

058045953

ABSTRACT:
The invention provides certain amino acid conjugates of substituted heterocycloaryl-)ethyl!acetamides useful for selectively agonizing kappa opioid receptors in mammalian tissue.

REFERENCES:
patent: 4806556 (1989-02-01), Portoghese
Chang, A., et al., "k-Opioid Receptor Selective Affinity Labels: Electrophilic Benzeneacetamides as k-selective Opioid Antagonists", Advance ACS Abstracts, vol. 2, No. 22, J. Med. Chem., 79-80, (Nov. 15, 1994).
Barber, A., et al., "Opiod Agonists and Antagonists: An Evaluation of Their Peripheral Actions in Inflammation," Med. Res. Reviews, 12, 525-562 (1992).
Barlow, J. J., et al., "Structure/Activity Studies Related to acetamides: A Novel Series of Potent and Selective .kappa.-Opiod Agonists," J. Med. Chem., 34, 3149-3158 (1991).
Birch, P.J., et al., "Preparation and Evaluation of Some Hydrophilic Phenylacetyl-peperazines as Peripherally Selective .kappa.-Opiod Agonists," Bioorg. Med. Chem. Lett., 2, 1275-1278 (1992).
Brown, D. R., et al., "The Use of Quanternary Narcotic Antagonists in Opiate Research," Neuropharm., 24, 181-191 (1985).
Costello, G.F., et al., !acetamides: The Use of Conformational Analysis in the Development of a Novel Series of Opioid .kappa. Agonists," J. Med. Chem., 34, 181-189 (1991).
Martin, W. R., "Pharmacology of Opioids," Pharmacol. Reviews, 35, 283-232 (1984).
Rogers, H., et al., "GR94839, a .kappa.-Opioid Agonist with Limited Access to the Central Nervous System, has Antinociceptive Activity," Br. J. Pharmacol., 106, 783-789 (1992).
Shaw, J.S., et al., "ICI 204448: A .kappa.-Opioid Agonist with Limited Access to the CNS," Br. J. Pharmacol., 96, 986-992 (1989).
Simon, E.J., et al., "Opioid Receptor Multiplicity: Isolation, Purification, and Chemical Characterization of Binding Sites," In: Opioids I, Herz, A., (ed.), Springer-Verlag, Berlin, pp. 3-26 (1993).
"K Opioid Receptor Selective Affinity Labels: Electrophilic Benzeneacetamides as K-Selective Opioid Antagonists," A. Chang et al., J. Med. Chem.(1994) 37, 4490-4498.

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