1471519-92-2

Upstream product

• 17585-69-2 L-phenylalanine hydrochloride 
• 15761-39-4 1-(tert-butoxycarbonyl)-L-proline 
• 1471519-86-4 N-Boc-(N-Me)Phe-Phe-OMe 
• 37553-65-4 Boc-N-Me-Phe-OH 

Downstream Products

• 1471520-02-1 N-Boc-Tyr-Pro-(N-Me)Phe-Phe-OMe 
• 1471520-12-3 N-Boc-Tyr-Pro-(N-Me)Phe-Phe-NH(CH₂)₂OH 
• 1471520-25-8 C₃₅H₄₃N₅O₆*C₂HF₃O₂ 

Relevant academic research and scientific papers

Hybrid peptides endomophin-2/DAMGO: Design, synthesis and biological evaluation

Endomorphin-2 [Tyr-Pro-Phe-Phe-NH2] and DAMGO [Tyr-D-Ala-Gly-(N-Me)Phe-Gly-ol] are natural (EM2) and synthetic (DAMGO) opioid peptides both selective for μ opioid receptor with high analgesic activity. In this work we report synthesis, in vitro and in vivo biological evaluation of five new hybrid EM2/DAMGO analogues, with the aim to obtain compounds with high affinity at μ-opioid receptor, high activity in animal nociception tests (hot plate and tail flick) and improved enzymatic stability. Double N-methylation on both Phe residues and C-terminal ethanolamide led to analogue 6e, which possesses a good in vitro μ affinity (Kiμ = 34 nM), combined with a remarkable in vivo antinociceptive activity.