Access of peripherally administered DuP 753 to rat brain angiotensin II receptors

The in vivo access of the nonpeptide angiotensin II (Ang II) antagonist, DuP 753 (10 mg kg−1, i.v.), to Ang II receptors of rat brain was investigated by in vitro autoradiography with [125I]‐[Sar1, Ile8] Ang II as a ligand. DuP 753 markedly inhibited the binding to sites which contain exclusively AT...

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Bibliographic Details
Published in:British journal of pharmacology 1991-12, Vol.104 (4), p.771-772
Main Authors: Song, Keifu, Zhuo, Jialong, Mendelsohn, Frederick A.O.
Format: Article
Language:English
Subjects:
1-Sarcosine-8-Isoleucine Angiotensin II - pharmacology
angiotensin II
Angiotensin II - antagonists & inhibitors
Angiotensin Receptor Antagonists
Animals
antagonist
Autoradiography
Biological and medical sciences
Biphenyl Compounds - administration & dosage
Biphenyl Compounds - pharmacology
Brain Chemistry - drug effects
Imidazoles - administration & dosage
Imidazoles - pharmacology
Iodine Radioisotopes
Losartan
Male
Medical sciences
Medulla Oblongata - drug effects
Medulla Oblongata - physiology
Miscellaneous
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Pharmacology. Drug treatments
Rat brain
Rats
Rats, Inbred Strains
receptor subtypes
Tetrazoles - administration & dosage
Tetrazoles - pharmacology
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Summary:The in vivo access of the nonpeptide angiotensin II (Ang II) antagonist, DuP 753 (10 mg kg−1, i.v.), to Ang II receptors of rat brain was investigated by in vitro autoradiography with [125I]‐[Sar1, Ile8] Ang II as a ligand. DuP 753 markedly inhibited the binding to sites which contain exclusively AT1 receptors both outside and within the blood brain barrier, such as the circumventricular organs, paraventricular hypothalamic nucleus, median preoptic nucleus and nucleus of the solitary tract. However, binding to other nuclei containing AT2 receptors was not significantly inhibited. These results demonstrate that DuP 753 and/or its active metabolite readily cross the blood brain barrier in vivo and selectively inhibit binding to AT1 receptors in specific brain nuclei.
ISSN:0007-1188
1476-5381
DOI:10.1111/j.1476-5381.1991.tb12503.x