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孤啡肽、内吗啡肽-1和-2与无脊椎动物免疫和神经系统的μ3阿片受体无相互作用（英文）

Acta Pharmacologica Sinica 2000年第6期21卷 38-42页

作者： christos m rialas,benjamin weeks,patrick cadet,yannick goumon,george b stefano Neuroscience Research Institute State University of New York at Old Westbury Old Westbury NY 11568-0210 USA biology Department Adelphi University Garden City New York 11530 USA Neuroscience Research Institute State University of New York at Old Westbury Old Westbury NY 11568-0210 USA Neuroscience Research Institute State University of New York at Old Westbury Old Westbury NY 11568-0210 USA biology Department Adelphi University Garden City New York 11530 USA Neuroscience Research Institute NY 11568-0210 USA

AIm: To determine if endomorphin-1,-2 and nociceptin (orphanin FQ) bind to the μ3 opiate receptor subtype or release nitric oxide as μ3 selective ligands do. mETHODS: These opioid peptides were examined for their ability to displace [3H]dihydromorphine (DHm) binding from the invertebrate (immunocytes and pedal ganglia)μ3 opiate receptor in membrane homogenates. The ligands were also tested for their ability to release nitric oxide from the same intact tissues utilizing an amperometric probe that measures nitric oxide in real-time. RESULTS: Endomorphin-1,-2 and nociceptin do not displace [3H]DHm binding from immunocyte or pedal ganglia membrane homogenates nor do they release nitric oxide from these tissues. CONCLUSION: Since these newly discovered opioid peptides do not interact with the μ3 opiate receptor subtype, endogenous morphine' s significance is enhanced because it appears to be the only naturally occurring opiate ligand for the receptor. Furthermore, since this study involves invertebrate t

关键词：阿片样肽类吗啡一氧化氮贻贝免疫细胞 mu阿片受体

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直接评估吗啡刺激糖尿病人隐静脉内皮一氧化氮释放减少

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Acta Pharmacologica Sinica 2002年第2期23卷 5-10页

作者： Thomas V bILHNGER, James A VOSSWINKEL, patrick cadet, christos m rialas, Harold I mAGAZINE, george b stefano(Division of Cardiothoracic Surgery, Department of Surgery, University Hospital and medical Center, HSC, T19-080, Stony brook, New York 11794-8191 Neuroscience Research Institute, State University of New York College at Old Westbury, Old Westbury, New York , USA) Division of Cardiothoracic Surgery Department of SurgeryUniversity Hospital and Medical CenterHSC T19-080Stony Brook 澳大利亚 11794-8191 Neuroscience Research Institute State University of New York College at Old WestburyOld Westbury 美国 New York

to directly measure in real time basal and stimulated levels of NO released from human saphenous vein endothelium and to quantify the expression of the μopiate receptor, which has been linked with NO release. mETHODS: Saphenous vein segments from patients with type 2 diabetes ( n = 12) and patients without diabetes (n =8) were obtained. The release of NO was measured directly from the endothelium using a NO-specific amperometric probe. NΩ-nitro-L-arginine methyl ester (L-NAmE, 0.1 mmol/L), a NO synthase (NOS) inhibitor, or morphine (1 μmol/L), a stimulant, was administered and the measurements were repeated. Values were reported relative to the mean initial measurement of NO release from diabetic endothelium, which was defined as the relative zero level of NO release. A RT-PCR was then performed on the endothelium to measureμ opiate receptor expression. RESULTS: Diabetic patients (n = 12) showed a relative and significantly diminished basal level of released NO, (0.049± 0.012) nmol/L, compared with

关键词：一氧化氮糖尿病心肌血管重建术阿片受体隐静脉

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