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Drug-Target Interaction

Drug

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PubChem ID:11151
Structure:
Synonyms:
3-(Aminooxymethyl)-6-bromphenol
5-((Aminooxy)methyl)-2-bromophenol
5-(aminooxymethyl)-2-bromophenol
555-65-7
AC1L1WQ1
alpha-(Aminooxy)-6-bromo-m-cresol
BRN 1945736
Brocresin
Brocresina
Brocresina [INN-Spanish]
Brocresine
Brocresine (USAN/INN)
Brocresine [USAN:BAN:INN]
Brocresine [USAN:INN:BAN]
Brocresinum
Brocresinum [INN-Latin]
C7H8BrNO2
CL 54998
D03158
LS-55318
m-Cresol, .alpha.-(aminooxy)-6-bromo-
m-CRESOL, alpha-(AMINOOXY)-6-BROMO-
NSD 1055
NSD-1055
O-)4-Brom-3-hydroxybenzyl)hydroxylamin
Phenol, 5-((aminooxy)methyl)-2-bromo-
UNII-11F6O06WN0

Target

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Uniprot ID:DCHS_RAT
Synonyms:
HDC
Histidine decarboxylase
EC-Numbers:4.1.1.22
Organism:Rat
Rattus norvegicus
PDB IDs:-

Binding Affinities:

Ki: Kd:Ic 50:Ec50/Ic50:
----

References:

37141
Electron microscopic radioautographic identification of the ECL cell as the histamine-synthesizing endocrine cell in the rat stomach.. W Rubin; B Schwartz (1979) Gastroenterology display abstract
Rat gastric oxyntic glands contain argyrophil "enterochromaffin-like" endocrine cells that synthesize and store histamine and also have APUD ability--they can take up exogenous L-5-hydroxytryptophan (5-HTP), can decarboxylate it to 5-hydroxytryptamine (5-HT, serotonin) by the enzyme DOPA-decarboxylase, and can store the amine. Previous cytochemical studies suggested that these cells correspond to both the ECL and A-like cells, the two predominant endocrine cells identified by electron microscopy (EM) in rat oxyntic glands. In a recent study, however, we demonstrated that the ECL but not the A-like cell exhibited APUD ability when rat gastric mucosa was incubated with H3-5-HTP and studied by EM radioautography. The purpose of the present study was to identify by EM radioautography the histamine-synthesizing endocrine cells in the rat stomach. Pieces of rat (male Sprague-Dawley) gastric mucosa were incubated in organ culture with L-H3-histidine (50 muCi, 1.8 x 10(-5) M) with and without inhibitors and were processed for LM and EM radioautography. H3-histidine labeled the ECL cells heavily but the A-like and other endocrine cells only lightly. The labeling of ECL cells was only modestly reduced by cycloheximide, an inhibitor of protein synthesis, whereas the labeling of A-like and other endocrine cells was almost abolished. In contrast, the labeling of ECL cells was markedly reduced by 4-bromo-3-hydroxybenzyloxyamine (NSD-1055), an inhibitor of histidine decarboxylase and DOPA decarboxylase, but was not appreciably affected by carbidopa, an inhibitor of only the DOPA decarboxylase. Incubations with H3-histamine (50 muCi, 0.9 x 10(-5) M) failed to label endocrine cells. Thus, this study demonstrates that the ECL but not the A-like cell is the histamine-synthesizing endocrine cell of the rat stomach.