<i>N</i>-Methylamide-structured SB366791 derivatives with high TRPV1 antagonistic activity: toward PET radiotracers to visualize TRPV1-Reference-Cited by-同舟云学术

N-Methylamide-structured SB366791 derivatives with high TRPV1 antagonistic activity: toward PET radiotracers to visualize TRPV1

Published:2022 Issue:10 Volume:13 Page:1197-1204
ISSN:2632-8682
Container-title:RSC Medicinal Chemistry
language:en
Short-container-title:RSC Med. Chem.

Author:

Kida Tatsuya¹,Takahashi Nobuaki²,Mori Masayuki X.²,Sun Jiacheng H.²,Oota Hideto²,Nishino Kosuke¹,Okauchi Takashi³,Ochi Yuta³,Kano Daisuke⁴,Tateishi Ukihide⁵,Watanabe Yasuyoshi⁶,Cui Yilong³,Mori Yasuo²,Doi Hisashi¹^ORCID

Affiliation:

1. Laboratory for Labeling Chemistry, RIKEN Center for Biosystems Dynamics Research, 6-7-3 Minatojima-minamimachi, Chuo-ku, Kobe, Hyogo 650-0047, Japan

2. Laboratory of Molecular Biology, Department of Synthetic Chemistry and Biological Chemistry, Graduate School of Engineering, Kyoto University, Nishikyo-ku, Kyoto, 615-8510, Japan

3. Laboratory for Biofunction Dynamics Imaging, RIKEN Center for Biosystems Dynamics Research, 6-7-3 Minatojima-minamimachi, Chuo-ku, Kobe, Hyogo, 650-0047, Japan

4. Pharmaceutical department, National Cancer Center Hospital East, 6-5-1 Kashiwanoha, Kashiwa-shi, Chiba, 277-8577 Japan

5. Department of Diagnostic Radiology and Nuclear Medicine, Tokyo Medical and Dental University Graduate School of Medicine, 1-5-45, Yushima, Bunkyo-ku, Tokyo 113-8519, Japan

6. Laboratory for Pathophysiological and Health Science, RIKEN Center for Biosystems Dynamics Research, 6-7-3 Minatojima-minamimachi, Chuo-ku, Kobe, Hyogo 650-0047, Japan

Abstract

N-Methylamide derivatives of SB366791 show higher antagonistic activity against TRPV1 compared with SB366791. 11C- and 18F-labeled radiotracers of these derivatives were synthesized, and PET imaging studies using rats were performed.

Funder

Japan Agency for Medical Research and Development

Publisher

Royal Society of Chemistry (RSC)

Subject

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

Link

http://pubs.rsc.org/en/content/articlepdf/2022/MD/D2MD00158F

Reference43 articles.

1. The capsaicin receptor: a heat-activated ion channel in the pain pathway

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