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Development of selective non-peptide angiotensin II type 2 receptor agonsists
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- Alterman, Mathias (author)
- Uppsala universitet,Institutionen för läkemedelskemi
- (creator_code:org_t)
- 2009-10-30
- 2010
- English.
- In: jraas. Journal of the renin-angiotensin-aldosterone system. - : Hindawi Limited. - 1470-3203 .- 1752-8976. ; 11:1, s. 57-66
- Journal article (peer-reviewed)
Abstract
Subject headings
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- 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
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Farmaceutiska vetenskaper (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Pharmaceutical Sciences (hsv//eng)
Keyword
- angiotensin
- AT(2) receptor
- AT(2) receptor agonist
- drug development
- medical chemistry
- PHARMACY
- FARMACI
Publication and Content Type
- ref (subject category)
- art (subject category)
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