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Access of peripherally administered DuP 753 to rat brain angiotensin II receptors
Author(s) -
Song Keifu,
Zhuo Jialong,
Mendelsohn Frederick A.O.
Publication year - 1991
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1991.tb12503.x
Subject(s) - circumventricular organs , receptor , endocrinology , medicine , angiotensin ii , solitary tract , nucleus , dup , hypothalamus , blood–brain barrier , chemistry , angiotensin receptor , subfornical organ , in vivo , solitary nucleus , biology , central nervous system , microbiology and biotechnology , biochemistry , gene duplication , gene
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 [ 125 I]‐[Sar 1 , Ile 8 ] Ang II as a ligand. DuP 753 markedly inhibited the binding to sites which contain exclusively AT 1 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 AT 2 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 AT 1 receptors in specific brain nuclei.