Effects of polar κ receptor agonists designed for the periphery on ATP-induced Ca2+ release from keratinocytes-Reference-Cited by-同舟云学术

Effects of polar κ receptor agonists designed for the periphery on ATP-induced Ca2+ release from keratinocytes

Published:2016 Issue:2 Volume:7 Page:317-326
ISSN:2040-2503
Container-title:MedChemComm
language:en
Short-container-title:Med. Chem. Commun.

Author:

Galla Fabian¹²³⁴,Bourgeois Christian¹²³⁴,Lehmkuhl Kirstin¹²³⁴,Schepmann Dirk¹²³⁴⁵,Soeberdt Michael⁶⁷⁴,Lotts Tobias⁸⁹³⁴,Abels Christoph⁶⁷⁴,Ständer Sonja⁸⁹³⁴,Wünsch Bernhard¹²³⁴⁵

Affiliation:

1. Institut für Pharmazeutische und Medizinische Chemie

2. Westfälische Wilhelms-Universität Münster

3. D-48149 Münster

4. Germany

5. Cells-in-Motion Cluster of Excellence (EXC 1003 – CiM)

6. Dr. August Wolff GmbH & Co. KG Arzneimittel

7. D-33611 Bielefeld

8. Center for Chronic Pruritus and Department of Dermatology

9. University Hospital Münster

Abstract

The very polar pyridylmethyl derivative 5a (log D_7.4 = 1.1) represents a potent and selective full κ-opioid receptor agonist (K_i = 0.13 nM, EC₅₀ = 33 nM), which reduced the release of Ca²⁺-ions into the cytoplasm in human keratinocytes.

Funder

Deutsche Forschungsgemeinschaft

Publisher

Royal Society of Chemistry (RSC)

Subject

Pharmaceutical Science,Biochemistry,Drug Discovery,Molecular Medicine,Pharmacology,Organic Chemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2016/MD/C5MD00414D

Reference37 articles.

1. ETFAD/EADV eczema task force 2009 position paper on diagnosis and treatment of atopic dermatitis

2. Non-Analgesic Effects of Opioids: Peripheral Opioid Receptors as Promising Targets for Future Anti-Pruritic Therapies

3. Possible Roles of Epidermal Opioid Systems in Pruritus of Atopic Dermatitis

4. The Epithelial Cell-Derived Atopic Dermatitis Cytokine TSLP Activates Neurons to Induce Itch

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