PRODUCT LITERATURE

Sartan- AT receptor interactions: evidence for insurmountable antagonism and inverse agonism

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Sartans are non-peptide AT1 receptor antagonists used to treat hypertension and related pathologies. Their effects on the G protein-dependent responses of angiotensin II (Ang II) were the same in vascular tissues and in isolated cell systems. All are competitive but,
when pre-incubated, they act surmountably (only rightward shift of the Ang II concentration-response curve) or insurmountably (also decreasing the maximal response). Insurmountable behaviour reflects the formation of tight sartan-receptor complexes; it is
often partial due to the co-existence of tight and loose complexes. Their ratio positively correlates with the dissociation half-life of the tight complexes and depends on the sartan: i.e. candesartan > olmesartan > telmisartan ≈ EXP3174 > valsartan > irbesartan >>
losartan. When AT1 receptors display sufficient basal activity (in case of receptor overexpression, mutation and, especially, tissue
stretching) sartans may also act as inverse agonists. This rather affects long-term, G protein-independent hypertrophic responses
leading to cardiovascular remodelling.

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Detail Information

Series Title

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Publisher

: .,

Collation

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Language

English

ISBN/ISSN

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Classification

NONE

Content Type

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Media Type

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Carrier Type

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Edition

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Subject(s)

Candesartan
Canderin Duo

Specific Detail Info

Molecular and Cellular Endocrinology, 2009, 302 (2), pp.237

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