Related Products of 83435-58-9. The protonation of heteroatoms in aromatic heterocycles can be divided into two categories: lone pairs of electrons are in the aromatic ring conjugated system; and lone pairs of electrons do not participate. Compound: Boc-D-Prolinol, is researched, Molecular C10H19NO3, CAS is 83435-58-9, about Endomorphin-1 Analogues Containing β-Proline Are μ-Opioid Receptor Agonists and Display Enhanced Enzymatic Hydrolysis Resistance. Author is Cardillo, Giuliana; Gentilucci, Luca; Qasem, Ahmed R.; Sgarzi, Fabio; Spampinato, Santi.
This paper describes the synthesis and affinity toward the μ-opioid receptor of tetrapeptides obtained from endomorphin-1, H-Tyr-Pro-Trp-Phe-NH2 (1), by substituting each amino acid in turn with its β-homolog. For example, peptides H-Tyr-Pro-Trp-βPhe-NH2 (2), H-Tyr-Pro-βTrp-Phe-NH2 (3), H-Tyr-βPro-Trp-Phe-NH2 (4), H-Tyr-D-βPro-Trp-Phe-NH2 (5) and H-βTyr-Pro-Trp-Phe-NH2 (6), where β indicates a β-amino acid homolog, were prepared The ability to bind μ-opioid receptors depends on the β-amino acid, and in particular, 4 (containing β-L-Pro) has a KI in the nanomolar range. Peptides 4 and 5 are significantly more resistant to enzymic hydrolysis than 1. These peptides, including 1, produced a concentration-dependent inhibition of forskolin-stimulated cAMP formation, thus behaving as μ-opioid agonists. These features suggest that this novel class of endomorphin-1 analogs may represent suitable candidates for the in vivo investigation as potential μ-opioid receptor agonists.
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Reference:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica