118476-85-0

118476-85-0 structure

Name: (D-Arg2,Lys4)-Dermorphin (1-4) amide
Chemical Name: 6-amino-2-[[2-[[2-[[2-amino-3-(4-hydroxyphenyl)propanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-phenylpropanoyl]amino]hexanamide
CAS Number: 118476-85-0
Molecular Formula: C₃₀H₄₅N₉O₅
Molecular Weight: 611.73600
Catalog: Signaling Pathways GPCR/G Protein Opioid Receptor
Create Date: 2016-01-14 23:43:57
Modify Date: 2024-01-14 10:27:54
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].

Name	6-amino-2-[[2-[[2-[[2-amino-3-(4-hydroxyphenyl)propanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-phenylpropanoyl]amino]hexanamide
Synonyms	[D-Arg2 (Lys4]-Dermorphin-(1-4)-amide H-Tyr-D-Arg-Phe-Lys-NH2 DALDA (D-Arg2,Lys4)-Dermorphin (1-4) amide

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

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

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

118476-85-0	100304-60-7
90549-86-3	118476-87-2
1282514-63-9	130947-34-1
83397-56-2	87777-29-5
82802-96-8	87614-65-1