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Endomorphin-1 (Tyr-Pro-Trp-Phe-NH 2 ) and endomorphin-2 (Tyr-Pro-Phe-Phe-NH 2 ), peptides recently isolated from bovine and human brain, have high affinity and selectivity for μ opiate receptors. They share sequence similarity with the endogenous opiate-modulating peptide Tyr-W-MIF-1 (Tyr-Pro-Trp-Gly-NH 2 ). The efficacies of these endogenous peptides and of the enkephalin...
The ability of transglutaminase-synthesized 1,3-diaminopropane, spermidine (Spd), spermine (Spm), and monodansylcadaverine γ-(glutamyl 5 )derivatives of substance P (SP) to produce bronchoconstriction was investigated. In urethane-anaesthetized guinea pigs, intravenous injections of SP derivatives contracted differently bronchial smooth muscle and caused hypotension. The most effective bronchoconstrictor...
Pharmacological study of Phe-Met-Leu-Phe-amide (FMRFa) receptors is hindered by the lack of selective ligands. The classification of these selective ligands is further hampered by the limited availability of functional assays. In this study, we evaluated several synthetic FMRFa analogs for agonist and antagonist activity by measuring their abilities to produce [ 35 S]-GTP-γ-S stimulation...
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