In Vitro Assessment of the Metabolic Stability of Two Novel Endomorphin-2 Analogs, CYX-5 and CYX-6, in Rat Liver Microsomes-Reference-Cited by-同舟云学术

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In Vitro Assessment of the Metabolic Stability of Two Novel Endomorphin-2 Analogs, CYX-5 and CYX-6, in Rat Liver Microsomes

Published:2023-05-12 Issue:4 Volume:48 Page:463-466
ISSN:0378-7966
Container-title:European Journal of Drug Metabolism and Pharmacokinetics
language:en
Short-container-title:Eur J Drug Metab Pharmacokinet

Author:

Imam Mohammad Zafar^ORCID,Ghassabian Sussan^ORCID,Kuo Andy^ORCID,Cai Yunxin^ORCID,Qin Yajuan^ORCID,Li Tingyou^ORCID,Smith Maree T.^ORCID

Funder

Research Training Program (RTP) Scholarship

UQ Graduate School Scholarship

Australian Research Council Large Linkage grant in collaboration with Boehringer Ingelheim Pharma GmbH & Co. KG

Therapeutic Innovation Australia

National Natural Science Foundation of China

Publisher

Springer Science and Business Media LLC

Subject

Pharmacology (medical),Pharmacology

Link

https://link.springer.com/content/pdf/10.1007/s13318-023-00828-6.pdf

Reference14 articles.

1. Siramshetty VB, Shah P, Kerns E, Nguyen K, Yu KR, Kabir M, et al. Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models. Sci Rep. 2020;10:20713.

2. Ackley DC, Rockich KT, Baker TR. Metabolic stability assessed by liver microsomes and hepatocytes. In: Yan Z, Caldwell GW, editors. Optimization in drug discovery: in vitro methods. Totowa: Humana Press; 2004. p. 151–62.

3. Imam MZ, Kuo A, Ghassabian S, Cai Y, Qin Y, Li T, et al. Intracerebroventricular administration of CYX-6, a potent μ-opioid receptor agonist, a δ- and κ-opioid receptor antagonist and a biased ligand at μ, δ & κ-opioid receptors, evokes antinociception with minimal constipation and respiratory depression in rats in contrast to morphine. Eur J Pharmacol. 2020;871:172918.

4. Imam MZ, Kuo A, Ghassabian S, Cai Y, Qin Y, Li T, et al. CYX-5, a G-protein biassed MOP receptor agonist, DOP receptor antagonist and KOP receptor agonist, evokes constipation but not respiratory depression relative to morphine in rats. Pharmacol Rep. 2023. https://doi.org/10.1007/s43440-023-00446-8.

5. Staniszewska R, Fichna J, Gach K, Toth G, Poels J, Vanden Broeck J, et al. Synthesis and biological activity of endomorphin-2 analogs incorporating piperidine-2-, 3- or 4-carboxylic acids instead of proline in position 2. Chem Biol Drug Des. 2008;72:91–4.

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