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Drug-Target Interaction

Drug

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PubChem ID:16130933
Structure:
Synonyms:
142569-99-1
Endothelin-1 (8-21), succinyl-(glu(9),ala(11,15))-
Irl 1620
Irl-1620
L-Tryptophan,
L-Tryptophan, N-(3-carboxy-1-oxopropyl)-L-alanyl-L-alpha-glutamyl-L-alpha-glutamyl-L-alanyl-L-valyl-L-tyrosyl-L-tyrosyl-L-alanyl-L-histidyl-L-leucyl-L-alpha-aspartyl-L-isoleucyl-L-isoleucyl-
LS-184750
NCGC00167326-01
Succinyl-(glu(9),ala(11,15))-endothelin-1 (8-21)
Succinyl-(glutamyl(9)-alanyl(11,15))-endothelin-1 (8-21)

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:
----

References:

9771913
Endothelin ET(B) receptors counteract venoconstrictor effects of endothelin-1 in anesthetized rats.. B Palacios; S L Lim; C C Pang (1998) Life sciences display abstract
The inhibitory effects of BQ 788 (3 mg/kg, i.v., ET(B)-receptor antagonist) on endothelin-1 (ET-1)- or IRL 1620 (ET(B)-receptor agonist)-induced changes in mean arterial pressure (MAP), mean circulatory filling pressure (MCFP, driving force of venous return), arterial resistance (RA), venous resistance (RV) and cardiac output (CO) were characterized in 6 groups of pentobarbital-anesthetized rats. ET-1 or IRL 1620 (0.5, 1 and 2 nmol/kg, i.v.) dose-dependently increased MAP, RA, RV and MCFP and decreased CO. Maximum changes in RA, RV and CO elicited by ET-1 were greater than those by IRL 1620. Equimolar doses of ET-1 and IRL 1620 also caused similar initial transient decreases in MAP. BQ 788 alone slightly elevated MCFP, but did not alter other variables. The ET(B)-blocker abolished all changes elicited by IRL 1620, but only partially inhibited its responses on MCFP, showing the presence of BQ 788-insensitive receptors. BQ 788 also abolished ET-1's depressor response, partially inhibited its effect on MCFP, and markedly augmented its effects on RA, RV and CO. Thus, ET(B)-receptors counteract the sustained constrictor effects of ET-1 on arterial and venous resistance vessels Our results indicate a substantial arterial and venous dilator role for ET(B) receptors.