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  • 08월 18일 17시 이후 : 초록수정 불가능, 일정확인 및 검색만 가능

제108회 대한화학회 학술발표회, 총회 및 기기전시회 안내 Imaging studies of [76Br]BMK-I-152 as a non-peptide, selective antagonist against corticotropin-releasing hormone type 1 receptor

2011년 8월 1일 17시 21분 46초
Ⅲ-MEDI.P-328 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
금 <발표Ⅲ>
저자 및
이웅섭, 정한샘, 김병문
서울대학교 화학부, Korea

Corticotropin-releasing hormone (CRH) is a neuropeptide, which regulates endocrine and autonomic responses to stress through G-protein coupled receptors, CRHR1 or CRHR2. A radiolabeled ligand which is useful for monitoring changes in vivo in CRF1 receptor occupancy would be of a great help in understanding the course and pathophysiology of stress-related diseases as well as in the clinical development of non-peptide antagonist drug candidates. We have developed a high-affinity CRHR1 antagonist, BMK-I-152 and continued our efforts in developing radioligands based upon BMK-I-152 capable of in vivo PET imaging CRHR1 in the brain. The radiolabelling process of the BMK-I-152 at both the 3 and 4 position with [76Br] were carried out and the PET imaging studies on both compounds have been studied. The result of in vitro autoradiography studies reveals that both 4-[76Br]BMK-152 and 3-[76Br]BMK-152 were found selective for CRF1 receptors, however, only 4-[76Br] isomer displayed subnanomolar affinity binding, and the 4-[76Br] isomer had approximately 70-fold higher affinity than that of the 3-[76Br] isomer. Ex vivo autoradiography studies of rat brain uptakes of 4-[76Br]BMK-152 showed regional localization which is consistent with the known CRF1 receptor distribution and this study confirmed that BMK-I-152 had a potential as an excellent PET ligand for in vivo imaging of CRF1 receptors.