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Design, synthesis, ...
Design, synthesis, and biological evaluation of the first selective nonpeptide AT2 receptor agonist
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- Wan, Y. (author)
- Uppsala universitet,Institutionen för läkemedelskemi,OrgFarmKemi
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- Wallinder, Charlotta (author)
- Uppsala universitet,Institutionen för läkemedelskemi,OrgFarmKemi
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Plouffe, B. (author)
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Beaudry, H. (author)
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- Mahalingam, A. K. (author)
- Uppsala universitet,Institutionen för läkemedelskemi,OrgFarmKemi
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Wu, X. (author)
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- Johansson, Berndt, 1969 (author)
- Gothenburg University,Göteborgs universitet,Institutionen för de kirurgiska disciplinerna, Avdelningen för gastroforskning,Institute of Surgical Sciences, Department of Gastro Research
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- Holm, Mathias, 1969 (author)
- Gothenburg University,Göteborgs universitet,Institutionen för de kirurgiska disciplinerna, Avdelningen för gastroforskning,Institute of Surgical Sciences, Department of Gastro Research
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- Botoros, M. (author)
- Uppsala universitet,Institutionen för farmaceutisk biovetenskap
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Karlen, A. (author)
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- Pettersson, Anders, 1959 (author)
- Gothenburg University,Göteborgs universitet,Institutionen för de kirurgiska disciplinerna, Avdelningen för gastroforskning,Institute of Surgical Sciences, Department of Gastro Research
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- Nyberg, F. (author)
- Uppsala universitet,Institutionen för farmaceutisk biovetenskap
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- Fändriks, Lars, 1956 (author)
- Uppsala universitet,Gothenburg University,Göteborgs universitet,Institutionen för de kirurgiska disciplinerna, Avdelningen för gastroforskning,Institute of Surgical Sciences, Department of Gastro Research,Institutionen för läkemedelskemi,OrgFarmKemi
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Gallo-Payet, N. (author)
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- Hallberg, A. (author)
- Uppsala universitet,Institutionen för läkemedelskemi,OrgFarmKemi
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- Alterman, M. (author)
- Uppsala universitet,Institutionen för läkemedelskemi,OrgFarmKemi
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(creator_code:org_t)
- 2004-10-15
- 2004
- English.
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In: J Med Chem. - : American Chemical Society (ACS). - 0022-2623 .- 1520-4804. ; 47:24, s. 5995-6008
- Related links:
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https://gup.ub.gu.se...
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https://doi.org/10.1...
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Abstract
Subject headings
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- The first druglike selective angiotensin II AT(2) receptor agonist (21) with a K(i) value of 0.4 nM for the AT(2) receptor and a K(i) > 10 microM for the AT(1) receptor is reported. Compound 21, with a bioavailability of 20-30% after oral administration and a half-life estimated to 4 h in rat, induces outgrowth of neurite cells, stimulates p42/p44(mapk), enhances in vivo duodenal alkaline secretion in Sprague-Dawley rats, and lowers the mean arterial blood pressure in anesthetized, spontaneously hypertensive rats. Thus, the peptidomimetic 21 exerts a similar biological response as the endogenous peptide angiotensin II after selective activation of the AT(2) receptor. Compound 21, derived from the prototype nonselective AT(1)/AT(2) receptor agonist L-162,313 will serve as a valuable research tool, enabling studies of the function of the AT(2) receptor in more detail.
Subject headings
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Farmaceutiska vetenskaper (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Pharmaceutical Sciences (hsv//eng)
Keyword
- Adminstration
- Oral
- Animals
- Antihypertensive Agents/chemical synthesis/chemistry/pharmacology
- Bicarbonates/metabolism
- Biological Availability
- Cell Line
- Drug Design
- Enzyme Activation
- Female
- Half-Life
- Intestinal Mucosa/metabolism
- Liver/metabolism
- Male
- Mitogen-Activated Protein Kinases/metabolism
- Molecular Mimicry
- Neurites/drug effects/physiology
- Peptides/chemistry
- Radioligand Assay
- Rats
- Rarts
- Inbred SHR
- Rats
- Sprague-Dawley
- Receptor
- Angiotensin
- Type 2/*antagonists/metabolism
- Sulfonamides/*chemical synthesis/chemistry/pharmacology
- Swine
- Thiophenes/*chemical synthesis/chemistry/pharmacology
- Uterus/metabolism
- Administration; Oral
Publication and Content Type
- ref (subject category)
- art (subject category)
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J Med Chem
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- By the author/editor
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Wan, Y.
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Wallinder, Charl ...
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Plouffe, B.
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Beaudry, H.
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Mahalingam, A. K ...
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Wu, X.
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Johansson, Bernd ...
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Holm, Mathias, 1 ...
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Botoros, M.
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Karlen, A.
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Pettersson, Ande ...
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Nyberg, F.
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Fändriks, Lars, ...
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Gallo-Payet, N.
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Hallberg, A.
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Alterman, M.
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- About the subject
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- MEDICAL AND HEALTH SCIENCES
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MEDICAL AND HEAL ...
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and Basic Medicine
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and Pharmaceutical S ...
- Articles in the publication
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J Med Chem
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Journal of Medic ...
- By the university
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University of Gothenburg
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Uppsala University