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(D-Ala2)-Leu-Enkephalin-Arg trifluoroacetate salt

Names

[ CAS No. ]:
81733-79-1

[ Name ]:
(D-Ala2)-Leu-Enkephalin-Arg trifluoroacetate salt

[Synonym ]:
Dalargin
H-Tyr-D-Ala-Gly-Phe-Leu-Arg-OH
(D-Ala2)-Leucine Enkephalin-Arg

Biological Activity

[Description]:

Dalargin is a potent δ-opioid receptor agonist. Dalargin mitigates Gentamicin (HY-A0276)-induced cell death. Dalargin shows nephroprotective effects on Gentamicin-induced kidney injury. Dalargin shows antiulcer activity[1][2][3].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Opioid Receptor
Signaling Pathways >> Neuronal Signaling >> Opioid Receptor
Research Areas >> Neurological Disease

[Target]

δ Opioid Receptor/DOR


[In Vitro]

Dalargin (100 µg/mL; 1 h) 在体外减轻庆大霉素诱导的肾上皮细胞死亡[2]。 Cell Viability Assay[2] Cell Line: Kidney cells Concentration: 100 µg/mL Incubation Time: 1 h (prior to treatment with 1.2–2.5 mg/ml gentamicin for 24 h) Result: Reduced kidney cells death.

[In Vivo]

Dalargin (25, 50 µg/kg; i.p.) 对庆大霉素诱导的大鼠肾损伤显示出肾脏保护作用[2]。 Animal Model: 290-350 g, White male rats[2] Dosage: 25, 50 µg/kg Administration: I.p. (3 h before each gentamicin injection) Result: Mitigated gentamicin-induced acutekidney injury, attenuated ROS generation and oxidative stress, alleviated histopathological changes in a renal tissue.

[References]

[1]. Titov MI, et al. Dalargin--a peptidnyĭ preparat s tsitoprotektivnym deĭstviem [Dalargin--a peptide preparation with cytoprotective action]. Biull Vsesoiuznogo Kardiol Nauchn Tsentra AMN SSSR. 1985;8(2):72-6.  

[2]. Plotnikov EY, et al. Nephroprotective effect of GSK-3β inhibition by lithium ions and δ-opioid receptor agonist dalargin on gentamicin-induced nephrotoxicity. Toxicol Lett. 2013 Jul 18;220(3):303-8.  

[3]. Polonskiĭ VM, et al. Mesto prilozheniia (tsentral'noe ili perifericheskoe) protivoiazvennogo deĭstviia sinteticheskogo analoga éndogennykh opioidov dalargina v éksperimental'noĭ modeli tsisteaminovykh duodenal'nykh iazv u krys [The site (central or peripheral) of the anti-ulcer action of dalargin, a synthetic analog of endogenous opioids in an experimental model of cysteamine-induced duodenal ulcer in rats]. Biull Eksp Biol Med. 1987 Apr;103(4):433-4.  

Chemical & Physical Properties

[ Density]:
1.363g/cm3

[ Molecular Formula ]:
C35H51N9O8

[ Molecular Weight ]:
725.83500

[ Exact Mass ]:
725.38600

[ PSA ]:
308.40000

[ LogP ]:
5.06670

Related Compounds