Analogues of β-LPH61–64 posessing selective agonist activity at μ-opiate receptors
BK Handa, AC Lane, JAH Lord, BA Morgan… - European journal of …, 1981 - Elsevier
BK Handa, AC Lane, JAH Lord, BA Morgan, MJ Rance, CFC Smith
European journal of pharmacology, 1981•ElsevierPeptides based on the stabilised tetrapeptide HTyr-D-Ala-Gly-MePheOH have been
synthesised and shown to have substantial opioid activity both in vitro and in vitro. The
selectivity of these compounds for different receptor populations has been investigated
using both isolated tissue assays and binding studies. Results suggest that the compounds
are potent agonists at μ-receptors with little or no affinity for the δ-receptor population. One of
the compounds, RX783006 (HTyr-D-Ala-Gly-MePhe-NH (CH 2) 2 OH), has been tritiated to …
synthesised and shown to have substantial opioid activity both in vitro and in vitro. The
selectivity of these compounds for different receptor populations has been investigated
using both isolated tissue assays and binding studies. Results suggest that the compounds
are potent agonists at μ-receptors with little or no affinity for the δ-receptor population. One of
the compounds, RX783006 (HTyr-D-Ala-Gly-MePhe-NH (CH 2) 2 OH), has been tritiated to …
Abstract
Peptides based on the stabilised tetrapeptide HTyr-D-Ala-Gly-MePheOH have been synthesised and shown to have substantial opioid activity both in vitro and in vitro. The selectivity of these compounds for different receptor populations has been investigated using both isolated tissue assays and binding studies. Results suggest that the compounds are potent agonists at μ-receptors with little or no affinity for the δ-receptor population. One of the compounds, RX783006 (HTyr-D-Ala-Gly-MePhe-NH(CH2)2OH), has been tritiated to high specific radioactivity and may prove to be a useful probe in the elucidation of the function of the heterogenous opiate receptor population.
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