Analogues of β-LPH61–64 posessing selective agonist activity at μ-opiate receptors
作者： Balraj K. Handa , Anthony C. Lane , John A.H. Lord , Barry A. Morgan , Michael J. Rance
DOI: 10.1016/0014-2999(81)90364-2
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摘要: Abstract Peptides based on the stabilised tetrapeptide HTyr-D-Ala-Gly-MePheOH have been synthesised and shown to substantial opioid activity both in vitro vitro. The selectivity of these compounds for different receptor populations has investigated using isolated tissue assays binding studies. Results suggest that are potent agonists at μ-receptors with little or no affinity δ-receptor population. One compounds, RX783006 (HTyr-D-Ala-Gly-MePhe-NH(CH2)2OH), tritiated high specific radioactivity may prove be a useful probe elucidation function heterogenous opiate
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