Characterization of binding kinetics of [3H]Tyr-D-Arg2-Phe-Sar4 at opioid receptors

European Journal of Pharmacology

Volumn 473, Issue 2-3, 2003, Pages 127-134

  Vonhof, Stefan ^a   Feuerstein, Giora ^b   Sirén, Anna Leena ^c,d  

^a UNIVERSITY OF GÖTTINGEN   (Germany)

^b BRISTOL MYERS SQUIBB   (United States)

^c MAX PLANCK INSTITUTE OF EXPERIMENTAL MEDICINE   (Germany)

^d UNIFORMED SERVICES UNIVERSITY OF THE HEALTH SCIENCES   (United States)

Author keywords

Brain; Dermorphin; Kinetic; Receptor binding; TAPS; Tetrapeptide

Indexed keywords

DERMORPHIN DERIVATIVE; DIVALENT CATION; EDETIC ACID; GUANYLYLIMIDODIPHOSPHATE; LIGAND; MAGNESIUM SULFATE; MU OPIATE RECEPTOR; OPIATE RECEPTOR; SODIUM ION; TETRAPEPTIDE; TYROSYL DEXTRO ARGINYL 2 PHENYLALANYLSARCOSINE 4 H 3; UNCLASSIFIED DRUG;

ANIMAL TISSUE; ANTINOCICEPTION; ARTICLE; BINDING KINETICS; BREATHING; CATTLE; CONTROLLED STUDY; DISSOCIATION; DRUG BINDING SITE; DRUG POTENCY; DRUG RECEPTOR BINDING; MEMBRANE; NONHUMAN; PRIORITY JOURNAL; RECEPTOR AFFINITY; STIMULATION; THALAMUS;

EID: 0042206725     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0014-2999(03)01999-X     Document Type: Article

References (32)

1. Abbadie C., Pan Y., Drake C.T., Pasternak G.W. Comparative immunohistochemical distributions of carboxy terminus epitopes from the mu-opioid receptor splice variants MOR-1D, MOR-1 and MOR-1C in the mouse and rat CNS. Neuroscience. 100:2000;141-153.
2. Abbadie C., Pan Y.X., Pasternak G.W. Differential distribution in rat brain of mu opioid receptor carboxy terminal splice variants MOR-1C-like and MOR-1-like immunoreactivity: evidence for region-specific processing. J. Comp. Neurol. 419:2000;244-256.
3. Broccardo M., Erspamer V., Falconieri Erspamer G., Improta G., Linari G., Melchiorri P., Montecucchi P.C. Pharmacological data on dermorphins, a new class of potent opioid peptides from amphibian skin. Br. J. Pharmacol. 73:1981;625-631.
4. Bylund D.B., Yamamura H. Methods for receptor binding. Yamamura H., Enna S.J., Kuhar M.J. Methods in Neurotransmitter Receptor Analysis. 1990;1-36 Raven Press, New York, NY.
5. Chen Y., Mestek A., Liu J., Hurley J.A., Yu L. Molecular cloning and functional expression of a mu-opioid receptor from rat brain. Mol. Pharmacol. 44:1993;8-12.
6. Clark J.A., Itzhak Y., Hruby V.J., Yamamura H.I., Pasternak G.W. [D-Pen2, D-Pen5]enkephalin (DPDPE): a delta-selective enkephalin with low affinity for mu 1 opiate binding sites. Eur. J. Pharmacol. 128:1986;303-304.
7. Clark J.A., Houghten R., Pasternak G.W. Opiate binding in calf thalamic membranes: a selective mu 1 binding assay. Mol. Pharmacol. 34:1988;308-317.
8. Giagnoni G., Mennuni L., Pecora N., Basilico L., Parolaro D., Gori E. Binding studies of dermorphin and its L-form on rat brain opioid receptors. Pharmacol. Res. Commun. 19:1987;173-181.
9. Goodman R.R., Pasternak G.W. Visualization of mu1 opiate receptors in rat brain by using a computerized autoradiographic subtraction technique. Proc. Natl. Acad. Sci. U. S. A. 82:1985;6667-6671.
10. Guglietta A., Irons B.J., Lazarus L.H., Melchiorri P. Structure-activity relationship of dermorphin on gastric secretion. Endocrinology. 120:1987;2137-2143.
11. Kinouchi K., Standifer K.M., Pasternak G.W. Modulation of mu 1, mu 2, and delta opioid binding by divalent cations. Biochem. Pharmacol. 40:1990;382-384.
12. Ling G.S., Pasternak G.W. Morphine catalepsy in the rat: involvement of mu 1 (high affinity) opioid binding sites. Neurosci. Lett. 32:1982;193-196.
13. Ling G.S., Spiegel K., Lockhart S.H., Pasternak G.W. Separation of opioid analgesia from respiratory depression: evidence for different receptor mechanisms. J. Pharmacol. Exp. Ther. 232:1985;149-155.
14. Montecucchi P.C., de Castiglione R., Piani S., Gozzini L., Erspamer V. Amino acid composition and sequence of dermorphin, a novel opiate-like peptide from the skin of Phyllomedusa sauvagei. Int. J. Pept. Protein Res. 17:1981;275-283.
15. Munson P.J., Rodbard D. Ligand: a versatile computerized approach for characterization of ligand-binding systems. Anal. Biochem. 107:1980;220-239.
16. Paakkari P., Paakkari I., Siren A.L., Feuerstein G. Respiratory and locomotor stimulation by low doses of dermorphin, a mu1 receptor-mediated effect. J. Pharmacol. Exp. Ther. 252:1990;235-240.
17. 2-Phe-sarcosine-induced opioid analgesia and respiratory stimulation: the role of mu 1-receptors? J. Pharmacol. Exp. Ther. 266:1993;544-550.
18. Pan Y.X., Xu J., Bolan E., Abbadie C., Chang A., Zuckerman A., Rossi G., Pasternak G.W. Identification and characterization of three new alternatively spliced mu-opioid receptor isoforms. Mol. Pharmacol. 56:1999;396-403.
19. Pan Y.X., Xu J., Bolan E., Chang A., Mahurter L., Rossi G., Pasternak G.W. Isolation and expression of a novel alternatively spliced mu opioid receptor isoform, MOR-1F. FEBS Lett. 466:2000;337-340.
20. Rossi G.C., Pan Y.X., Brown G.P., Pasternak G.W. Antisense mapping the MOR-1 opioid receptor: evidence for alternative splicing and a novel morphine-6 beta-glucuronide receptor. FEBS Lett. 369:1995;192-196.
21. 2-substituted tetrapeptides. J. Pharmacol. Exp. Ther. 242:1987;654-659.
22. Schuller A.G., King M.A., Zhang J., Bolan E., Pan Y.X., Morgan D.J., Chang A., Czick M.E., Unterwald E.M., Pasternak G.W., Pintar J.E. Retention of heroin and morphine-6 beta-glucuronide analgesia in a new line of mice lacking exon 1 of MOR-1. Nat. Neurosci. 2:1999;151-156.
23. 4 activates phospholipase C-coupled mu2-opioid receptors in SH-SY5Y cells. Eur. J. Pharmacol. 305:1996;235-238.
24. Standifer K.M., Clark J.A., Pasternak G.W. Modulation of Mu1 opioid binding by magnesium: evidence for multiple receptor conformations. J. Pharmacol. Exp. Ther. 266:1993;106-113.
25. Stevens C.W., Yaksh T.L. Spinal action of dermorphin, an extremely potent opioid peptide from frog skin. Brain Res. 385:1986;300-304.
26. Vonhof S., Barone F.C., Price W.J., Paakkari P., Millison J.H., Feuerstein G.Z., Siren A.K. Receptor binding and biological activity of the dermorphin analog Tyr-D-Arg(2)-Phe-Sar (TAPS). Eur. J. Pharmacol. 416:2001;83-93.
27. Wang J.B., Imai Y., Eppler C.M., Gregor P., Spivak C.E., Uhl G.R. mu Opiate receptor: cDNA cloning and expression. Proc. Natl. Acad. Sci. U. S. A. 90:1993;10230-10234.
28. Weiland G.A., Molinoff P.B. Quantitative analysis of drug-receptor interactions: I. Determination of kinetic and equilibrium properties. Life Sci. 29:1981;313-330.
29. Werling L.L., Brown S., Cox B.M. The sensitivity of opioid receptor types to regulation by sodium and GTP. Neuropeptides. 5:1984;137-140.
30. Werling L.L., Brown S.R., Puttfarcken P., Cox B.M. Sodium regulation of agonist binding at opioid receptors: II. Effects of sodium replacement on opioid binding in guinea pig cortical membranes. Mol. Pharmacol. 30:1986;90-95.
31. Werling L.L., Puttfarcken P.S., Cox B.M. Multiple agonist-affinity states of opioid receptors: regulation of binding by guanyl nucleotides in guinea pig cortical, NG108-15, and 7315c cell membranes. Mol. Pharmacol. 33:1988;423-431.
32. Zukin R.S., Eghbali M., Olive D., Unterwald E.M., Tempel A. Characterization and visualization of rat and guinea pig brain kappa opioid receptors: evidence for kappa 1 and kappa 2 opioid receptors. Proc. Natl. Acad. Sci. U. S. A. 85:1988;4061-4065.