(D-Arg2,Lys4)-Dermorphin (1-4) amide

Modify Date: 2024-01-14 10:27:54

(D-Arg2,Lys4)-Dermorphin (1-4) amide Structure
(D-Arg2,Lys4)-Dermorphin (1-4) amide structure
Common Name (D-Arg2,Lys4)-Dermorphin (1-4) amide
CAS Number 118476-85-0 Molecular Weight 611.73600
Density N/A Boiling Point N/A
Molecular Formula C30H45N9O5 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of (D-Arg2,Lys4)-Dermorphin (1-4) amide


DALDA is a potent and highly selective μ-opioid receptor agonist with a Ki of 1.69 nM. DALDA shows antinociceptive and respiratory effects[1].

 Names

Name 6-amino-2-[[2-[[2-[[2-amino-3-(4-hydroxyphenyl)propanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-phenylpropanoyl]amino]hexanamide
Synonym More Synonyms

 (D-Arg2,Lys4)-Dermorphin (1-4) amide Biological Activity

Description DALDA is a potent and highly selective μ-opioid receptor agonist with a Ki of 1.69 nM. DALDA shows antinociceptive and respiratory effects[1].
Related Catalog
Target

μ Opioid Receptor/MOR:1.69 nM (Ki)

κ Opioid Receptor/KOR:4230 nM (Ki)

δ Opioid Receptor/DOR:19200 nM (Ki)

In Vitro DALDA 在生理 pH 值下携带净正电荷 (3+),因此是亲水的,比吗啡更极性[1]。
In Vivo DALDA (0-7 nmol/rat; i.t.; once) 在大鼠中表现出抗痛和呼吸作用[1]。 DALDA (0.1 and 1.0 μg/side; ICV; once) 在大鼠中产生双相效应,初始抑制,中间显著抑制,接着是水平运动、饲养和刻板印象次数的激活[2]。 Animal Model: Male Sprague-Dawley rats (300–350 g)[1] Dosage: 0.24, 0.7 and 7 nmol/rat Administration: Intrathecal injection, once Result: Showed antinociceptive effects with an ED50 of 237 pmol/rat in the rat tail-flick test. Inhibited the uptake of NE in spinal cord synaptosomes in a dose-dependent manner. Had no effect on 5-HT uptake. Produced depression in minute ventilation. Animal Model: Male Long-Evans rats, weighing 200-225 g[2] Dosage: 0, 0.1 and 1.0 μg/side, 0.5 μL Administration: Lateral cerebral ventricle injection, once Result: Elicited a significant biphasic effect with an initial suppression, an intermediate marked inhibition, followed by significant activation for horizontal movement time, rearing time, and stereotypy time.
References

[1]. Shimoyama M, et al. Antinociceptive and respiratory effects of intrathecal H-Tyr-D-Arg-Phe-Lys-NH2 (DALDA) and [Dmt1] DALDA. Journal of Pharmacology and Experimental Therapeutics, 2001, 297(1): 364-371.  

[2]. Meyer ME, et al. DALDA (H-Tyr-D-Arg-Phe-Lys-NH2), a potent mu-opioid peptide agonist, affects various patterns of locomotor activities. Pharmacol Biochem Behav. 1995 May;51(1):149-51.  

 Chemical & Physical Properties

Molecular Formula C30H45N9O5
Molecular Weight 611.73600
Exact Mass 611.35400
PSA 264.56000
LogP 3.30120

 Safety Information

Risk Phrases 20-35-52/53
Safety Phrases 26-36/37/39-45-61
RIDADR UN 1759 8/PG 2

 Synonyms

[D-Arg2 (Lys4]-Dermorphin-(1-4)-amide
H-Tyr-D-Arg-Phe-Lys-NH2
DALDA
(D-Arg2,Lys4)-Dermorphin (1-4) amide