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- Alterman, MathiasUppsala universitet,Institutionen för läkemedelskemi (author)
Development of selective non-peptide angiotensin II type 2 receptor agonsists
- Article/chapterEnglish2010
Publisher, publication year, extent ...
- 2009-10-30
- Hindawi Limited,2010
- printrdacarrier
Numbers
- LIBRIS-ID:oai:DiVA.org:uu-135602
- https://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-135602URI
- https://doi.org/10.1177/1470320309347790DOI
Supplementary language notes
- Language:English
- Summary in:English
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- SwePubSwePub
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Notes
- The development of the first drug-like selective angiotensin II type 2 (AT(2)) receptor agonist (22) derived from the non-selective angiotensin II type 1 (AT(1)) receptor/AT(2) receptor agonist L-162,313 is presented. Compound 22 with a K-i value of 0.4 nM for the AT(2) receptor and a K-i > 10 mu M for the AT(1) receptor induces outgrowth of neurite cells, stimulates p42/p44(mapk), enhancesin vivo duodenal alkaline secretion in Sprague-Dawley rats and lowers the mean arterial blood pressure in anaesthetised spontaneously hypertensive rats. Thus, the peptidomimetic 22 exerts a similar biological response as the endogenous peptide angiotensin II after selective activation of the AT(2) receptor. In addition, Compound 22 has a bioavailability of 20-30% after oral administration and a half-life estimated to four hours in the rat. Compound 22 will therefore serve as a valuable research tool enabling studies of the function of the AT(2) receptor in more detail.
Subject headings and genre
- MEDICIN OCH HÄLSOVETENSKAP Medicinska och farmaceutiska grundvetenskaper Farmaceutiska vetenskaper hsv//swe
- MEDICAL AND HEALTH SCIENCES Basic Medicine Pharmaceutical Sciences hsv//eng
- angiotensin
- AT(2) receptor
- AT(2) receptor agonist
- drug development
- medical chemistry
- PHARMACY
- FARMACI
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- Uppsala universitetInstitutionen för läkemedelskemi (creator_code:org_t)
Related titles
- In:jraas. Journal of the renin-angiotensin-aldosterone system: Hindawi Limited11:1, s. 57-661470-32031752-8976
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