Journal
CHEMICAL BIOLOGY & DRUG DESIGN
Volume 72, Issue 1, Pages 91-94Publisher
WILEY-BLACKWELL
DOI: 10.1111/j.1747-0285.2008.00678.x
Keywords
binding studies; calcium-based functional assay; enzymatic degradation; unnatural amino acids; mu-receptor agonist
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Novel endomorphin-2 (EM-2) analogs have been synthesized, incorporating unnatural amino acids with six-membered heterocyclic rings, such as piperidine-2-, 3- and 4-carboxylic acids (Pip, Nip and Inp, respectively) instead of Pro in position 2. [(R)-Nip(2)]EM-2 displayed an extremely high affinity for the mu-opioid receptor with IC(50) = 0.04 +/- 0.01 nM in comparison with IC(50) = 0.69 +/- 0.03 nM for EM-2. This analog was also very potent in the aequorin luminescence-based functional calcium assay and showed significantly enhanced stability in rat brain homogenate.
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