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Drug-Target Interaction

Drug

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PubChem ID:2214
Structure:
Synonyms:
1-(4-hydroxy-3-methoxyphenyl)-ethanone
1-(4-hydroxy-3-methoxyphenyl)ethan-1-one
1-(4-Hydroxy-3-methoxyphenyl)ethanone
3-Methoxy-4-hydroxyacetophenone
3-Metoksy-4-hydroksyacetofenon
3-Metoksy-4-hydroksyacetofenon [Polish]
4'-Hydroxy-3'-methoxyacetophenone
4-08-00-01814 (Beilstein Handbook Reference)
4-Acetyl-2-methoxyphenol
4-Hydroxy-3-methoxyacetophenone
4-Hydroxy-3-methoxyphenyl methyl ketone
498-02-2
A10809_ALDRICH
AA-504/20839006
AB1003774
AC-11656
AC1L1D6F
AC1Q46A5
AC1Q7AD6
Acetoguaiacon
Acetoguaiacone
Acetophenone, 4'-hydroxy-3'-methoxy-
ACETOPHENONE,4-HYDROXY,3-METHOXY ACETOVANILLON
ACETOPHENONE,4-HYDROXY,3-METHOXY ACETOVANILLON
Acetovanillon
Acetovanillone
Acetovanilone
Acetovanyllon
AI3-15892
AKOS000120562
Apocynin
Apocynine
AR-1H7512
BB_NC-2250
bmse000584
bmse010031
BRN 0637373
C056165
C11380
C9H10O3
CCRIS 7285
CHEBI:2781
CHEMBL346919
EINECS 207-854-5
Ethanone, 1-(4-hydroxy-3-methoxyphenyl)-
H0261
I01-7005
LS-13569
MLS001304972
MolPort-000-000-274
NCGC00247065-01
nchembio.83-comp20
NSC 209524
NSC209524
NSC2146
SBB008060
SMR000752909
W508454_ALDRICH
WLN: 1VR DQ CO1
ZINC00162515

Target

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Uniprot ID:EDNRB_RAT
Synonyms:
Endothelin B receptor
Endothelin receptor non-selective type
ET-B
EC-Numbers:-
Organism:Rat
Rattus norvegicus
PDB IDs:-

Binding Affinities:

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

16788136
Endothelin-A and -B receptors, superoxide, and Ca2+ signaling in afferent arterioles.. Susan K Fellner; William Arendshorst (2007) American journal of physiology. Renal physiology display abstract
It is unknown if endothelin-A and -B receptors (ET(A)R and ET(B)R) activate the production of superoxide via NAD(P)H oxidase and subsequently stimulate the formation of cyclic adenine diphosphate ribose (cADPR) in afferent arterioles. Vessels were isolated from rat kidney and loaded with fura 2. Endothelin-1 (ET-1) rapidly increased cytosolic Ca(2+) concentration ([Ca(2+)](i)) by 303 nM. The superoxide dismutase mimetic tempol, the NAD(P)H oxidase inhibitor apocynin, and nicotinamide, an inhibitor of ADPR cyclase, diminished the response by approximately 60%. The ET(B)R agonist sarafotoxin 6c (S6c) increased peak [Ca(2+)](i) by 117 nM. Subsequent addition of ET-1 in the continued presence of S6c caused an additional [Ca(2+)](i) peak of 225 nM. Neither nicotinamide or 8-bromo- (8-Br) cADPR nor apocynin decreased the [Ca(2+)](i) response to S6c, but inhibited the subsequent [Ca(2+)](i) response to ET-1. The ET(B)R blockers BQ-788 and A-192621 prevented the S6c [Ca(2+)](i) peak and reduced the ET-1 response by more than one-half, suggesting an ET(B)R/ET(A)R interaction. In contrast, the ET(A)R blocker BQ-123 had no effect on the S6c [Ca(2+)](i) peak and obliterated the subsequent ET-1 response. ET-1 immediately stimulated superoxide formation (measured with TEMPO-9-AC, 68 arbitrary units) that was inhibited 95% by apocynin or diphenyl iodonium. S6c or IRL-1620 increased superoxide by 8% of that caused by subsequent ET-1 addition. We conclude that ET(A)R activation of afferent arterioles increases the formation of superoxide that accounts for approximately 60% of subsequent Ca(2+) signaling. ET(B)R activation appears to result in only minor increases in superoxide production. Nicotinamide and 8-Br-cADPR results suggest that ET-1 (and primarily ET(A)R) causes the activation of vascular smooth muscle cell-ADPR cyclase.