Conformationally constrained cyclic enkephalin analogs with delt

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai

Patent

Rate now

  [ 0.00 ] – not rated yet Voters 0   Comments 0

Details

514809, 2601125E, A61K 3700, C07C10352

Patent

active

045187118

ABSTRACT:
Novel compounds which are capable of binding with enhanced specificity to the delta receptor are disclosed. The compounds are a series of cyclic, conformationally constrained analogs of enkephalins which display exceptional delta receptor specificity. The compounds of the present invention are polypeptides of the formula: ##STR1## wherein R.sup.1 and R.sup.2, which may be the same or different, are hydrogen, methyl, or lower alkyl having 1 to 5 carbon atoms;

REFERENCES:
patent: 4148786 (1979-04-01), Sarantakis
H. I. Mosberg & P. W. Schiller, Int. J. Peptide Protein Res., 23, 462-466, (1984).
P. W. Schiller, B. Eggimann, J. DiMaio, C. Lexieux, & T. M.-D. Nguyen, Biochem. Biophys. Res. Commun., 101, 337 (1981).
P. W. Schiller & J. DiMaio, Peptides: Structure and Function, V. J. Hruby & D. H. Rich, eds., Pierce Chemical Co., Rockford, IL, pp. 269-278, (1983).
H. I. Mosberg, R. Hurst, V. J. Hruby, J. J. Galligan, T. F. Burks, K. Gee, & H. I. Yamamura, Biochem. Biophys. Res. Commun., 106, 506, (1982).
ibid., Life Sciences, 32, 2565, (1983).
H. I. Mosberg, R. Hurst, V. J. Hruby, K. Gee, H. I. Yamamura, J. J. Galligan, & T. F. Burks, Proc. Natl. Acad. Sci. USA, 80, 5871 (1983).
H. I. Mosberg, R. Hurst, V. J. Hruby, K. Gee, K. Akiyama, H. I. Yamamura, J. J. Galligan & T. F. Burks, Life Sciences, 33, Suppl. I., 447, (1983).
I. F. James & A. Goldstein, Molec. Pharmacol. 25, 337, (1984).
ibid., 35, 343, (1984).
A. D. Corbett, M. G. C. Gillan, H. W. Kosterlitz, A. T. McKnight & S. J. Paterson, Brit. J. Pharmacol. 86, 669P, (1983).
F. Porreca, H. I. Mosberg, R. Hurst, V. J. Hruby & T. F. Burks, Life Sciences, 33, Suppl. I, 457, (1983).
ibid., J. Pharmacol. Exp. Therap. 230, 341, (1984).
J. J. Galligan, H. I. Mosberg, R. Hurst, V. J. Hruby, & T. F. Burks, J. Pharmacol. Exp. Therap., 229, 641, (1984).
J. Hughes, T. W. Smith, H. W. Kosterlitz, L. A. Fothergill, B. A. Morgan & H. R. Morris "Identification of Two Related Pentapeptides from the Brain with Potent Opiate Agonist Activity", Nature, vol. 258, Dec. 18, 1975.
D. H. Coy & A. J. Kastin, "Structure-CNS Activity Studies with the Enkephalins", Pharmac. Ther., vol. 10: 657-668.
P. E. Gilbert & W. R. Martin, "The Effects of Morphine- and Nalorphine-like Drugs in the Nondependent, Morphine-Dependent and Cyclazocine-Dependent Chronic Spinal Dog", Jour. of Pharm. and Exp. Ther., vol. 198, No. 1: 66-82, 1976.
W. R. Martin, C. G. Eades, J. A. Thompson, R. E. Huppler, & P. E. Gilbert, "The Effects of Morphine- and Nalorphine-like Drugs in the Nondependent and Morphine-Dependent Chronic Spinal Dog", Journ. Pharm. and Exp. Ther., vol. 197, No. 3: 517-531; 1976.
J. A. H. Lord, A. A. Waterfield, J. Hughes & H. W. Kosterlitz, "Endogenous Opioid Peptides: Multiple Agonists and Receptors", Nature, vol. 267: 495-499, Jun. 9, 1977.
R. J. Miller & P. Cuatrecasas, "Enkephalins and Endorphins", Vitamins and Hormones, vol. 36: 297-375, 1978.
A. A. Waterfield, F. M. Leslie, J. A. H. Lord, N. Ling & H. W. Kosterlitz, "Opioid Activities of Fragments of Beta-Endorphin and of its Leucine 65-Analogus Comparison of the Binding Properties of Methionine- and Leucine-Enkephalin", Euro. Jour. Pharm., 58: 11-18, 1978.
K. Chang & P. Cuatrecasas, "Multiple Opiate Receptors: Enkephalins and Morphine Bind to Receptors of Different Specificity", Jour. of Biological Chem., vol. 254, No. 8: 2610-2617, Apr. 25, 1979.
P. W. Schiller, B. Eggimann, J. DiMaio, C. Lemieux & T. M. D. Nguyen, "Cyclic Enkaphalin Analogs Containing a Cystine Bridge", Biochem. and Biophys. Res. Comm., vol. 101, No. 2: 337-343, 1981.
J. S. Morley, "Structure-Activity Relationships of Enkephalin-like Peptides", Ann. Rev. Pharmacol. Toxicol., 20: 81-110, 1980.
H. W. Kosterlitz, J. A. H. Lord, S. J. Paterson & A. A. Waterfield, "Effects of Changes in the Structure of Enkephalins and of Narcotic Analgesic Drugs on Their Interactions with .mu.- and .delta.

LandOfFree

Say what you really think

Search LandOfFree.com for the USA inventors and patents. Rate them and share your experience with other people.

Rating

Conformationally constrained cyclic enkephalin analogs with delt does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Conformationally constrained cyclic enkephalin analogs with delt, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Conformationally constrained cyclic enkephalin analogs with delt will most certainly appreciate the feedback.

Rate now

     

Profile ID: LFUS-PAI-O-1538780

  Search
All data on this website is collected from public sources. Our data reflects the most accurate information available at the time of publication.