Abstract:
:1. 125I-Endothelin (ET)-1 binding to the rat anterior pituitary gland was saturable and single, with a Kd of 71 pM and a Bmax of 120 fmol/mg. 2. When 1.0 microM BQ-123 (ETA antagonist) was added to the incubation buffer, the binding parameters were 8.3 pM and 8.0 fmol/mg, whereas 10 nM sarafotoxin S6c (ETB agonist) exerted little change in these binding parameters (Kd, 72 pM; Bmax, 110 fmol/mg). 3. ETB receptor-related compounds such as sarafotoxin S6c, ET-3, IRL1620, and BQ-788 competitively inhibited 125I-ET-1 binding, only when 1.0 microM BQ-123 was present in the incubation buffer. 4. Thus, the ETB receptor is capable of binding ET-1 when the ETA receptor is being occupied by BQ-123. A collaboration mechanism between the ETA and the ETB receptor may function in the recognition of ET-1, a typical "bivalent" ligand.
journal_name
Cell Mol Neurobioljournal_title
Cellular and molecular neurobiologyauthors
Himeno A,Shigematsu K,Taguchi T,Niwa Mdoi
10.1023/a:1022557717481subject
Has Abstractpub_date
1998-08-01 00:00:00pages
447-52issue
4eissn
0272-4340issn
1573-6830journal_volume
18pub_type
杂志文章abstract::Working memory (WM) is a highly heritable cognitive trait that is involved in many higher-level cognitive functions. In the past few years, much evidence has indicated that the reduction of dopamine activity in human brain can impair the WM system of the neuropsychiatric disorders. In this study, we hypothesized that ...
journal_title:Cellular and molecular neurobiology
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journal_title:Cellular and molecular neurobiology
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journal_title:Cellular and molecular neurobiology
pub_type: 杂志文章
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journal_title:Cellular and molecular neurobiology
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journal_title:Cellular and molecular neurobiology
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journal_title:Cellular and molecular neurobiology
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journal_title:Cellular and molecular neurobiology
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journal_title:Cellular and molecular neurobiology
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