Opioid interaction with K-receptors

Furthermore, the substitution of methyl groups at the T and 6 position of Tyr (Dmt) yielded Dmt-Tic- peptides (3) endowed with dramatically increased 8-affinity, comparable to the 8-affinity observed with deltorphins [59-63]. On the other hand, p-affinity of 3 rose 20-fold relative to 1 and 2, while k-affinity increased over 40-fold in guinea pig brain membranes, 20-fold in rat brain synaptosomes compared to 2 and approximately 40-fold for both membrane preparation relative to 1. Inclusion of the Tyr-D-Ala-Phe message domain (4) essentially eliminated opioid interaction with k-receptors, whereas 8- and p-affinities were only moderately altered in comparison to DYN (1-11) -NH2 (Table... 

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See also in sourсe #XX -- [ , ]

See also in sourсe #XX -- [ ]

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