Vasoactive intestinal peptide (VIP) is a neuropeptide having a wide range of effects on a large number of tissues. To gain insight into the role VIP plays in retinal function, VIP receptors in bovine retinal membranes were analyzed in competition binding assays and by affinity labeling studies and compared to VIP receptors in rat liver membranes. In both membrane preparations, high affinity VIP binding sites (KD approximately 1 nM) were detected. Secretin and glucagon, each having close structural homology to VIP, were found to have negligible effects on [125I]VIP binding in retina. In contrast, secretin (KD = 70 nM) was modestly effective in inhibiting [125I]VIP binding to rat liver membranes. Affinity labeling analysis revealed a VIP binding site of 59 kDa in both bovine retinal and rat liver membranes. Digestion of affinity-labeled receptor proteins with endoglycosidase F generated final cleavage products of approx. 45 kDa for both receptors. These results indicate that the retina expresses a high affinity, highly selective VIP receptor thereby supporting a specific function for VIP in this tissue.
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http://dx.doi.org/10.1016/0014-4835(90)90028-s | DOI Listing |
Pharmaceutics
December 2024
Center of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, Nanjing 210009, China.
SPT-07A, a D-borneol, is currently being developed in China for the treatment of ischemic stroke. We aimed to create a whole-body physiologically-based pharmacokinetic (PBPK) model to predict the pharmacokinetics of SPT-07A in rats, dogs, and humans. The in vitro metabolism of SPT-07A was studied using hepatic, renal, and intestinal microsomes.
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December 2024
Department of Medical Zoology, School of Medicine, Kyung Hee University, Seoul 02447, Republic of Korea.
: Clonorchiasis is a foodborne parasitic disease that can lead to severe biliary fibrosis and cholangiocarcinoma. While praziquantel (PZQ) is available for clonorchiasis treatment, it cannot revert the histopathological damage incurred through parasite-induced fibrosis. Curcumin (CUR) is an emerging experimental drug possessing anti-inflammatory and fibrosis-alleviating effects, thus signifying its potential as an anthelmintic drug.
View Article and Find Full Text PDFPharmaceutics
November 2024
Chengdu Origen Biotechnology Co., Ltd., Chengdu 610036, China.
Interleukin-1 (IL-1) is a pivotal mediator in the pathological progression of osteoarthritis (OA), playing a central role in disease progression. However, the rapid clearance of IL-1 receptor antagonist (IL-1Ra) from the joints may hinder the efficacy of intra-articular IL-1Ra injections in reducing OA-associated pain or cartilage degradation. Sustaining sufficient levels of IL-1Ra within the joints via adeno-associated virus (AAV)-mediated gene therapy presents a promising therapeutic strategy for OA.
View Article and Find Full Text PDFToxics
November 2024
College of Animal Science and Technology, Nanjing Agricultural University, Nanjing 210095, China.
Bisphenol A (BPA), extensively utilized in the manufacture of epoxy resins and polycarbonate plastics, is prevalent in the environment. Its exposure has been associated with an increased risk of hepatic lesions; however, the underlying mechanisms and the spectrum of its effects remain poorly understood. This study investigates the role of the Keap1-Nrf2 signaling pathway in regulating BPA-induced hepatotoxicity in vivo using a rat model.
View Article and Find Full Text PDFNutrients
December 2024
Department of Nutrition and Food Hygiene, School of Public Health, Qingdao University, 308 Ningxia Road, Qingdao 266071, China.
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