A specific template-assembled peptidic agonist for the angiotensin II receptor subtype 2 (AT2) and its effect on inferior olivary neurones.
We synthesized a molecule composed of two angiotensin II 4-8 pentapeptide fragments attached to a carrier molecule (TA), according to the template-assembled synthetic proteins concept. This molecule was investigated for receptor binding on angiotensin type-1 and type-2 receptors (AT1 and AT2) and its biological activity was determined by iontophoretic experiments on neurones of the inferior olive (ION) that express only AT2 receptors. TA binds exclusively to the AT2 receptor and mediates an agonistic angiotensin-II effect on the ION. TA is the first agonist available to study the direct stimulation of AT2 receptors.
Grouzmann
E
E
Division of Hypertension, Centre Hospitalier Universitaire Vaudois, Lausanne, Switzerland.
Felix
D
D
Imboden
H
H
Razaname
A
A
Mutter
M
M
D000595:Amino Acid Sequence; D000803:Angiotensin I / Q000378:metabolism; D000809:Angiotensins / Q000494:pharmacology*; D000818:Animals; D002118:Calcium / Q000378:metabolism; D007478:Iontophoresis; D008969:Molecular Sequence Data; D009847:Olivary Nucleus / Q000187:drug effects*; D010446:Peptide Fragments / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D011945:Receptors, Angiotensin / Q000819:agonists* / Q000378:metabolism; D013698:Templates, Genetic
D000809:Angiotensins; D010446:Peptide Fragments; D011945:Receptors, Angiotensin; C022782:angiotensin pentapeptide; D000803:Angiotensin I; D002118:Calcium