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- W1970783565 abstract "Abstract Intracellular cyclic AMP levels were determined for dimeric and monomeric enkephalins interacting with PGE 1 -stimulated NG108-15 cells. The dimeric pentapeptide enkephalin (DPE 2 ), [D-Ala 2 , Leu 5 -NH-CH 2 ] 2 , displaying very high affinity (K = 4.2 ± 0.3 nM −1 ) for the δ-opiate receptor, inhibited cyclic AMP production by 70%. Its IC 50 -value was between 0.1 and 0.2 nM, similar to that of the potent δ-agonist [D-Ala 2 , D-Leu 5 ] enkephalin (DADLE) with K = 1.0 ± 0.1 nM −1 . [D-Ala 2 , Leu 5 ] enkephalin amide (DALEA), which is the monomer of DPE 2 , showed an IC 50 = 4 nM. The dimeric tetrapeptide enkephalin (DTE 12 ), [D-Ala 2 , des-Leu 5 -NH-(CH 2 ) 6 ] 2 and its monomer [D-Ala 2 , desLeu 5 ] enkephalin amide (DAPEA) showed IC 50 = 2 and 20 nM, respectively. These results indicate that the DPE 2 and DTE 12 enkephalin dimers are potent δ-agonists." @default.
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- W1970783565 date "1983-01-01" @default.
- W1970783565 modified "2023-09-23" @default.
- W1970783565 title "Enkephalin dimers: Regulation of cyclic AMP levels in NG108-15 cells" @default.
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- W1970783565 doi "https://doi.org/10.1016/0024-3205(83)90145-5" @default.
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