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Vasorelaxant potencies and receptor binding affinities of atrial natriuretic hormone (ANH) analogues

Conference · · Fed. Proc., Fed. Am. Soc. Exp. Biol.; (United States)
OSTI ID:5324428
; ; ; ; ; ; ; ;
ANH (1-28) (..cap alpha..-rat ANP) produces hypotensive effects in vivo, presumably via interaction with specific receptors. Vasorelaxant potencies (pD/sub 2/) and intrinsic activities of ANH analogues were measured in histamine constricted rabbit aorta rings. Binding affinities (K/sub I/) of the compounds were studied in rabbit aorta renal cortex and adrenal, using the radio-ligand /sup 125/I-Tyr/sup 28/-ANH (1-28). Significant correlations (r < -.90; p < .01) between the pD/sub 2/s in aorta, and the log D/sub I/s in each of the three tissues were observed for the following cyclic compounds, listed in order of potency: ANH (1-28) greater than or equal to ANH (6-28) greater than or equal to Met/sup 12/-ANH (1-28) (..cap alpha..-human ANP) greater than or equal to cyclohexyl-Ala (Cha)/sup 8/-ANH (5-28) > Lys/sup 11/-ANH (5-28) = ANH (5-28) (atriopeptin III) = ANH (5-27) (atriopeptin II) = Cha/sup 21/-ANH (5-28) greater than or equal to ANH (7-28) > Cha/sup 15/-ANH (5-28) = Pro/sup 10/-ANH (5-28) = ANH (5-25) (atriopeptin I) = Asn/sup 13/-ANH (5-28) = Tyr/sup 9/-ANH (5-28) > des-Gly/sup 9/-ANH (5-28) > ANH (7-23) = Pro/sup 10/-ANH (7-23) greater than or equal to (D)Ala/sup 9/-ANH (7-23) > Pro/sup 9/-ANH (7-13). In summary, the affinities of several ANH analogues for both vascular and nonvascular receptors agree with their vasorelaxant potencies.
Research Organization:
Abbott Labs., Abbott Park, IL
OSTI ID:
5324428
Report Number(s):
CONF-8604222-
Conference Information:
Journal Name: Fed. Proc., Fed. Am. Soc. Exp. Biol.; (United States) Journal Volume: 45:3
Country of Publication:
United States
Language:
English

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550901* -- Pathology-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
ADRENAL GLANDS
AFFINITY
ANIMALS
AORTA
ARTERIES
BETA DECAY RADIOISOTOPES
BIOCHEMICAL REACTION KINETICS
BLOOD VESSELS
BODY
CARDIOVASCULAR AGENTS
CARDIOVASCULAR SYSTEM
DAYS LIVING RADIOISOTOPES
DRUGS
ELECTRON CAPTURE RADIOISOTOPES
ENDOCRINE GLANDS
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HORMONES
HYPOTENSION
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IODINE 125
IODINE ISOTOPES
ISOTOPE APPLICATIONS
ISOTOPES
KIDNEYS
KINETICS
LIGANDS
MAMMALS
MEMBRANE PROTEINS
NUCLEI
ODD-EVEN NUCLEI
ORGANIC COMPOUNDS
ORGANS
PATHOGENESIS
PROTEINS
RABBITS
RADIOISOTOPES
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RECEPTORS
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VASODILATORS
VERTEBRATES