cj-15-208 and Visceral-Pain

cj-15-208 has been researched along with Visceral-Pain* in 1 studies

Other Studies

1 other study(ies) available for cj-15-208 and Visceral-Pain

Article	Year
Versatile Picklocks To Access All Opioid Receptors: Tuning the Selectivity and Functional Profile of the Cyclotetrapeptide c[Phe-d-Pro-Phe-Trp] (CJ-15,208). Journal of medicinal chemistry, 2016, 10-13, Volume: 59, Issue:19 Recently, the tryptophan-containing noncationizable opioid peptides emerged with atypical structure and unexpected in vivo activity. Herein, we describe analogs of the naturally occurring mixed κ/μ-ligand c[Phe-d-Pro-Phe-Trp] 1 (CJ-15,208). Receptor affinity, selectivity, and agonism/antagonism varied upon enlarging macrocycle size, giving the μ-agonist 9 or the δ-antagonist 10 characterized by low nanomolar affinity. In particular, the μ-agonist c[β-Ala-d-Pro-Phe-Trp] 9 was shown to elicit potent antinociception in a mouse model of visceral pain upon systemic administration. Topics: Analgesics; Animals; HEK293 Cells; Humans; Mice; Models, Molecular; Narcotic Antagonists; Peptides, Cyclic; Receptors, Opioid; Visceral Pain	2016

Article

Year

Versatile Picklocks To Access All Opioid Receptors: Tuning the Selectivity and Functional Profile of the Cyclotetrapeptide c[Phe-d-Pro-Phe-Trp] (CJ-15,208).

Journal of medicinal chemistry, 2016, 10-13, Volume: 59, Issue:19

Recently, the tryptophan-containing noncationizable opioid peptides emerged with atypical structure and unexpected in vivo activity. Herein, we describe analogs of the naturally occurring mixed κ/μ-ligand c[Phe-d-Pro-Phe-Trp] 1 (CJ-15,208). Receptor affinity, selectivity, and agonism/antagonism varied upon enlarging macrocycle size, giving the μ-agonist 9 or the δ-antagonist 10 characterized by low nanomolar affinity. In particular, the μ-agonist c[β-Ala-d-Pro-Phe-Trp] 9 was shown to elicit potent antinociception in a mouse model of visceral pain upon systemic administration.

Topics: Analgesics; Animals; HEK293 Cells; Humans; Mice; Models, Molecular; Narcotic Antagonists; Peptides, Cyclic; Receptors, Opioid; Visceral Pain

2016