Pharmaceutica acta Helvetiae最新文献

{"title":"Excitatory amino acid receptors","authors":"G Gaviraghi","doi":"10.1016/S0031-6865(99)00052-7","DOIUrl":"10.1016/S0031-6865(99)00052-7","url":null,"abstract":"","PeriodicalId":19830,"journal":{"name":"Pharmaceutica acta Helvetiae","volume":"74 2","pages":"Pages 219-220"},"PeriodicalIF":0.0,"publicationDate":"2000-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/S0031-6865(99)00052-7","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"21659337","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Selection, design and evaluation of new radioligands for PET studies of cardiac adrenoceptors","authors":"V.W Pike ,&nbsp;M.P Law ,&nbsp;S Osman ,&nbsp;R.J Davenport ,&nbsp;O Rimoldi ,&nbsp;D Giardinà ,&nbsp;P.G Camici","doi":"10.1016/S0031-6865(99)00032-1","DOIUrl":"10.1016/S0031-6865(99)00032-1","url":null,"abstract":"<div><p><span>Changes in the numbers of human cardiac adrenoceptors<span><span> (ARs) are associated with various diseases, such as myocardial ischemia, </span>congestive heart failure<span>, cardiomyopathy<span> and hypertension. There is a clear need for capability to assess human cardiac ARs directly in vivo. Positron emission tomography (PET) is an imaging technique that provides this possibility, if effective radioligands can be developed for the targeted ARs. Here, the status of myocardial AR radioligand development for PET is described. Currently, there exist effective radioligands for imaging β-ARs in human myocardium. One of these, [</span></span></span></span><span><math><msup><mi></mi><mn>11</mn></msup><mtext>C</mtext></math></span>](<em>S</em><span>)-CGP 12177, is applied extensively to clinical research with PET, sometimes with other tracers of other aspects of the noradrenalin system. Alternative radioligands are in development for β-ARs, including β</span>₁-selective radioligands. A promising radioligand for imaging myocardial α₁-ARs, [<span><math><msup><mi></mi><mn>11</mn></msup><mtext>C</mtext></math></span>]GB67, is now being evaluated in human PET experiments.</p></div>","PeriodicalId":19830,"journal":{"name":"Pharmaceutica acta Helvetiae","volume":"74 2","pages":"Pages 191-200"},"PeriodicalIF":0.0,"publicationDate":"2000-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/S0031-6865(99)00032-1","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"21659333","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Cholinergic receptors and neurodegenerative diseases","authors":"Fulvio Gualtieri","doi":"10.1016/S0031-6865(99)00021-7","DOIUrl":"10.1016/S0031-6865(99)00021-7","url":null,"abstract":"","PeriodicalId":19830,"journal":{"name":"Pharmaceutica acta Helvetiae","volume":"74 2","pages":"Pages 85-89"},"PeriodicalIF":0.0,"publicationDate":"2000-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/S0031-6865(99)00021-7","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"21660174","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Pharmacological evidence of muscarinic receptor heterodimerization","authors":"S Chiacchio,&nbsp;M Scarselli,&nbsp;M Armogida,&nbsp;R Maggio","doi":"10.1016/S0031-6865(99)00041-2","DOIUrl":"10.1016/S0031-6865(99)00041-2","url":null,"abstract":"","PeriodicalId":19830,"journal":{"name":"Pharmaceutica acta Helvetiae","volume":"74 2","pages":"Pages 315-326"},"PeriodicalIF":0.0,"publicationDate":"2000-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/S0031-6865(99)00041-2","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"21660308","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Constitutive activity of G protein coupled receptors and drug action","authors":"Rob Leurs,&nbsp;Maria Sol Rodriguez Pena,&nbsp;Remko A Bakker,&nbsp;Astrid E Alewijnse,&nbsp;Henk Timmerman","doi":"10.1016/S0031-6865(99)00042-4","DOIUrl":"10.1016/S0031-6865(99)00042-4","url":null,"abstract":"","PeriodicalId":19830,"journal":{"name":"Pharmaceutica acta Helvetiae","volume":"74 2","pages":"Pages 327-331"},"PeriodicalIF":0.0,"publicationDate":"2000-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/S0031-6865(99)00042-4","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"21660309","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"New dimensions in G protein signalling: Gβ5 and the RGS proteins","authors":"William F Simonds,&nbsp;Jian-Hua Zhang","doi":"10.1016/S0031-6865(99)00043-6","DOIUrl":"10.1016/S0031-6865(99)00043-6","url":null,"abstract":"<div><p><span>The βγ complex of G-proteins regulates effectors independently of the Gα subunits, such that upon activation G proteins give may signal downstream along one or both pathways. The Gβ</span>₅ isoform exhibits much less homology with other Gβ isoforms (∼50%) and is preferentially expressed in brain. The Gβ₅<span> isoform exhibits novel properties in its activation of effector pathways such as MAPK, phospholipase C-β, and adenylyl cyclase type II when compared to Gβ</span>₁. Recently specific native complexes between Gβ5 and the regulator of G protein signaling (RGS) protein-7 (RGS7) and between Gβ₅<span>L (a splice variant with a 42 amino acid N-terminal extension) and RGS9 have been isolated from different retinal fractions. Such findings are not accounted for by current models as only the Gα subunits and not Gβ had been previously implicated in RGS protein function. These recent novel observations further reinforce the view of Gβ</span>₅ as a unique and highly specialized G protein subunit.</p></div>","PeriodicalId":19830,"journal":{"name":"Pharmaceutica acta Helvetiae","volume":"74 2","pages":"Pages 333-336"},"PeriodicalIF":0.0,"publicationDate":"2000-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/S0031-6865(99)00043-6","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"21660310","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Hijacked receptors","authors":"David J Triggle","doi":"10.1016/S0031-6865(99)00054-0","DOIUrl":"10.1016/S0031-6865(99)00054-0","url":null,"abstract":"<div><p>Pharmacological receptors are typically defined by their selectivity of ligand recognition, including where appropriate stereoselectivity of interaction. It is increasingly clear that receptors may, in fact, be promiscuous species. This promiscuity arises at several levels of organization: two appear to be of particular importance. A given ligand–receptor complex may couple with different effectors and may generate quite different physiological responses: this is particularly common, although not uniquely so, for G protein-coupled receptors. Or a single receptor may recognize fundamentally different ligands often of significantly different characteristics: a number of viruses gain entry to cells through their interaction at receptors for neurotransmitters, peptides or hormones.</p></div>","PeriodicalId":19830,"journal":{"name":"Pharmaceutica acta Helvetiae","volume":"74 2","pages":"Pages 287-290"},"PeriodicalIF":0.0,"publicationDate":"2000-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/S0031-6865(99)00054-0","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"21659960","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Metabotropic glutamate receptors: a structural view point","authors":"Roberto Pellicciari,&nbsp;Gabriele Costantino,&nbsp;Antonio Macchiarulo","doi":"10.1016/S0031-6865(99)00055-2","DOIUrl":"10.1016/S0031-6865(99)00055-2","url":null,"abstract":"","PeriodicalId":19830,"journal":{"name":"Pharmaceutica acta Helvetiae","volume":"74 2","pages":"Pages 231-237"},"PeriodicalIF":0.0,"publicationDate":"2000-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/S0031-6865(99)00055-2","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"21659339","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Rediscovering good old friend IGF-I in the new millenium: possible usefulness in Alzheimer's disease and stroke","authors":"Sylvain Doré,&nbsp;Satyabrata Kar,&nbsp;When-Hua Zheng,&nbsp;Rémi Quirion","doi":"10.1016/S0031-6865(99)00037-0","DOIUrl":"10.1016/S0031-6865(99)00037-0","url":null,"abstract":"<div><p><span>Much research has been done over the past two decades on the role of insulin-like growth factors I and II (IGF) in the maintenance of normal body homeostasis, especially in regard to various endocrine functions, growth and aging. For example, IGF-I is a well established promoter of tissue growth and has been used in the clinics for the treatment of growth related disorders, even being abused by athletes to enhance performance in competitions. In contrast, comparatively limited attention has been given to the potential significance of the IGFs in the central nervous system. Over the past few years, we have studied the trophic as well as neuromodulatory roles of the IGFs in the brain. IGF-I and IGF-II are potent modulators of acetylcholine<span> release; IGF-I inhibiting release while IGF-II is a potent stimulant. Moreover, only the internalization of the IGF-I receptor complex was blocked by an inhibitor of phosphotyrosylation. This is in accordance with the differential nature of the IGF-I and IGF-II receptors, the former being a tyrosine kinase receptor while the later is a single transmembrane domain protein bearing binding sites for 6-mannose phosphate containing residues. The activation of IGF-I receptors protected neurons against cell death induced by amyloidogenic derivatives likely by an intracellular mechanism distinct from those involved in the regulation of acetylcholine release and neuronal growth. The stimulation of IGF-I receptors can activate intracellular pathways implicating a PI3/Akt kinase and CREB phosphorylation or modulate the production of free radicals. The effects, particularly those of IGF-I on key markers of the Alzheimer's (AD) brains namely </span></span>cholinergic<span> dysfunction, neuronal amyloid toxicity, tau phosphorylation and glucose metabolism suggest the potential usefulness of this growth factor in the treatment of neurodegenerative diseases<span>. However, the poor bioavailability, enzymatic stability and brain penetration of IGF-I hamper progress in this regard. The recent development of a small, non-peptidyl mimetic of insulin able to directly activate the insulin receptor [Zhang, B., Salituro, G., Szalkowski, D., Li, Z., Zhang, Y., Royo, I., Vilella, D., Diez, M.T., Pelaez, F., Ruby, C., Kendall, R.L., Mao, X., Griffin, P., Calaycay, J., Zierath, J.R., Heck, J. V., Smith, R.G., Moller, D.E., 1999. Science, 284, 974–977] suggests that a similar strategy could be used for IGF-I and the IGF-I receptor leading to the characterization of IGF-I mimics of potential clinical usefulness.</span></span></p></div>","PeriodicalId":19830,"journal":{"name":"Pharmaceutica acta Helvetiae","volume":"74 2","pages":"Pages 273-280"},"PeriodicalIF":0.0,"publicationDate":"2000-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/S0031-6865(99)00037-0","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"21659958","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Neurotrophin receptor structure and interactions","authors":"Hiroko Yano,&nbsp;Moses V Chao","doi":"10.1016/S0031-6865(99)00036-9","DOIUrl":"10.1016/S0031-6865(99)00036-9","url":null,"abstract":"","PeriodicalId":19830,"journal":{"name":"Pharmaceutica acta Helvetiae","volume":"74 2","pages":"Pages 253-260"},"PeriodicalIF":0.0,"publicationDate":"2000-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/S0031-6865(99)00036-9","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"21659955","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}