Delta-Selective Glycopeptides Related to Enkephalin Produce Profound Analgesia with Reduced Side Effects in Mice
作者： Robin Polt , Edward J Bilsky , Richard D Egleton , ARIZONA UNIV TUCSON DEPT OF CHEMISTRY
DOI:
关键词:
摘要: Abstract : The use of endogenous neuropeptides such as enkephalins and endorphins drugs has remained an elusive goal since the 1970's. principle reason for this is that peptides generally do not cross blood-brain barrier, are quickly degraded in blood stream prior to delivery opiate receptors brain. Animal research with glycosylated (dynorphins) indicates potent analgesia possible after intravenous or sub-cutaneous injection. Glycopeptides derived from delta-selective opioid agonists have 2-3X potency morphine, lack many side effects associated muagonists morphine. Morphine still used on battlefield combat casualty care, it anticipated further development glycopeptide analgesics will result superior greatly reduced effects. Recent developments area reported.
参考文章(63)
Formulation and delivery of proteins and peptides American Chemical Society. ,(1994) , 10.1021/BK-1994-0567
Protein-lipid interactions : from membrane domains to cellular networks Wiley-VCH Verlag GmbH & Co. KGaA. ,(2006) , 10.1002/3527606769
The delta receptor CRC Press. ,(2003) , 10.1201/9780203025765
Yoshiharu Deguchi, Yusaku Miyakawa, Shinobu Sakurada, Yu Naito, Kazuhiro Morimoto, Sumio Ohtsuki, Ken-ichi Hosoya, Tetsuya Terasaki, Blood-brain barrier transport of a novel μ1-specific opioid peptide, H-Tyr-D-Arg-Phe-β-Ala-OH (TAPA) Journal of Neurochemistry. ,vol. 84, pp. 1154- 1161 ,(2003) , 10.1046/J.1471-4159.2003.01582.X
Lei Jin, Stephen L. Briggs, Srinivasan Chandrasekhar, Nickolay Y. Chirgadze, David K. Clawson, Richard W. Schevitz, David L. Smiley, Armen H. Tashjian, Faming Zhang, Crystal structure of human parathyroid hormone 1-34 at 0.9-A resolution. Journal of Biological Chemistry. ,vol. 275, pp. 27238- 27244 ,(2000) , 10.1016/S0021-9258(19)61502-4
Hiroshi Inooka, Tetsuya Ohtaki, Osamu Kitahara, Takahisa Ikegami, Satoshi Endo, Chieko Kitada, Kazuhiro Ogi, Haruo Onda, Masahiko Fujino, Masahiro Shirakawa, Conformation of a peptide ligand bound to its G-protein coupled receptor. Nature Structural & Molecular Biology. ,vol. 8, pp. 161- 165 ,(2001) , 10.1038/84159
Bryen A. Jordan, Lakshmi A. Devi, G-protein-coupled receptor heterodimerization modulates receptor function Nature. ,vol. 399, pp. 697- 700 ,(1999) , 10.1038/21441
R E Huppler, P E Gilbert, W R Martin, J A Thompson, C G Eades, The effects of morphine- and nalorphine- like drugs in the nondependent and morphine-dependent chronic spinal dog. Journal of Pharmacology and Experimental Therapeutics. ,vol. 197, pp. 517- 532 ,(1976)
R. Polt, M. M. Palian, S. A. Mitchell, R. D. Egleton, T. P. Davis, J. D. Huber, Improved Blood-Brain Barrier Penetration and Enhanced Analgesia of an Opioid Peptide by Glycosylation Journal of Pharmacology and Experimental Therapeutics. ,vol. 299, pp. 967- 972 ,(2001)
Edward J. Bilsky, Robert N. Bernstein, Gavril W. Pasternak, Victor J. Hruby, Dinesh Patel, Frank Porreca, Josephine Lai, Selective inhibition of [D-ALA2, GLU4]deltrophin antinociception by supraspinal, but not spinal, administration of an antisense oligodeoxynucleotide to an opioid delta receptor Life Sciences. ,vol. 55, ,(1994) , 10.1016/0024-3205(94)90110-4