Abstract
The transient receptor potential vanilloid 1 (TRPV1) is a member of nonselective cation channels and has been implicated in the progression of neurogenic inflammation and nociception. Through the synthesis of over 2,000 new compounds, a novel non-vanilloid TRPV1 antagonist PAC-14028 was discovered. As well as ideal physicochemical and pharmacokinetic properties, PAC-14028 showed meaningful efficacies against diverse disease models that include visceral pain, inflammatory bowel disease, and inflammatory pain. Of note, PAC-14028 effectively attenuates atopic dermatitis and pruritus without significant adverse effects, which is a substantial benefit over conventional pharmacotherapy. This report introduces the potential of a novel TRPV1 antagonist PAC-14028 as a new drug for atopic dermatitis and pruritus.
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Edited by Mi-Kyoung Kwak, College of Pharmacy (Rm 408), The Catholic University of Korea, Bucheon 420-743, Korea Tel: 82-2-2164-6532 E-mail: mkwak@catholic.ac.kr
Young-Ho Park Medical Beauty Research Institute, Amorepacific Corporation R&D Center Main Research Area Biochemistry: TRPV1, PAR-2 Pharmacology: Pain, Inflammation Development of Dermatological Drug, Quasi-Drug and Functional Cosmetic Ingredients
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Lim, KM., Park, YH. Development of PAC-14028, a novel transient receptor potential vanilloid type 1 (TRPV1) channel antagonist as a new drug for refractory skin diseases. Arch. Pharm. Res. 35, 393–396 (2012). https://doi.org/10.1007/s12272-012-0321-6
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DOI: https://doi.org/10.1007/s12272-012-0321-6