[D-Ala2]-Deltorphin II (Synonyms: [D-Ala2]-Deltorphin II) |
| Katalog-Nr.GC11848 |
[D-Ala2]-Deltorphin II ist ein selektiver Peptidagonist fÜr δ Opioid-Rezeptor.
Products are for research use only. Not for human use. We do not sell to patients.
![[D-Ala2]-Deltorphin II Chemische Struktur](/media/struct/GC1/GC11848.png "[D-Ala2]-Deltorphin II Chemische Struktur")
Cas No.: 122752-16-3
Sample solution is provided at 25 µL, 10mM.
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[D-Ala2]-deltorphin II (DADELT II) is a natural agonist of δ opioid receptor with Ki or IC50 value of 0.41 nM [1, 2].
Opioid receptors are most abundant in the central nervous system, but are also localized in many peripheral tissues in mammalian organisms. there are three types of opioid receptors that are well-defined; the µ, δ and κ receptors [2].
[D-Pen2, D-Pen5]enkephalin (DPDPE) is a second highly selective agonist of δ [3]. Treatment with DPDPE at 1 M for as short as 3 min significantly diminished the inhibition of the opioid receptor in NG108-15 cells to cyclic AMP production. That means neuronal delta opioid receptor underwent acute desensitization. This desensitization was temporally parallel to the phosphorylation of delta opioid receptor 3 min. after agonist stimulation [4].
I.c.v. administration of DADELT II from 0.38-12.78 nM resulted in a dose- and time-related antinociception. 10 min after the administration of DADELT II, the maximal antinociceptive response was seen. Until 60 min after the administration of DADELT II, effects were detected. These antinociceptive effects of i.c.v. DADELT II were antagonized by the selective δ antagonist, ICI 174,864 [3]. After supraspinal and spinal administration in rats intracerebroventricularly, DADELT II at 0.2, 1, 10 μg/rat in a dose-related fashion inhibited diarrhea and colonic bead expulsion but did not show any effect on the rate of small intestine transit. Spinal administration of DADELT II at the same dose produced similar results. Naltrindole is a selective antagonist of the δ opioid receptor. Subcutaneous pretreatment with naltrindole at 1 and 10 mg/kg antagonized effects of DADELT II partially and completely, respectively [1].
References:
[1]. Broccardo M, Improta G. Antidiarrheal and colonic antipropulsive effects of spinal and supraspinal administration of the natural δ opioid receptor agonist,[D-Ala2] deltorphin II, in the rat. European journal of pharmacology, 1992, 218(1): 69-73.
[2]. Janecka A, Fichna J, Janecki T. Opioid receptors and their ligands. Current topics in medicinal chemistry, 2004, 4(1): 1-17.
[3]. Jiang Q, Mosberg HI, Porreca F. Antinociceptive effects of [D-Ala2] deltorphin II, a highly selective δ agonist in vivo. Life sciences, 1990, 47(11): PL43-PL47.
[4]. Cai Y, Zhang Y, Wu Y, et al. δ opioid receptor in neuronal cells undergoes acute and homologous desensitization. Biochemical and biophysical research communications, 1996, 219(2): 342-347.
| Cas No. | 122752-16-3 | SDF | |
| Überlieferungen | [D-Ala2]-Deltorphin II | ||
| Chemical Name | (S)-5-(((R)-1-(((S)-1-((2-amino-2-oxoethyl)amino)-3-methyl-1-oxobutan-2-yl)amino)-3-methyl-1-oxobutan-2-yl)amino)-4-((S)-2-((R)-2-((S)-2-amino-3-(4-hydroxyphenyl)propanamido)propanamido)-3-phenylpropanamido)-5-oxopentanoic acid | ||
| Canonical SMILES | O=C([C@@H](C(C)C)NC([C@H](CCC(O)=O)NC([C@H](CC1=CC=CC=C1)NC([C@@H](C)NC([C@H](CC(C=C2)=CC=C2O)N)=O)=O)=O)=O)N[C@H](C(NCC(N)=O)=O)C(C)C | ||
| Formula | C38H54N8O10 | M.Wt | 782.89 |
| Löslichkeit | Soluble to 1 mg/ml in 10% acetonitrile | Storage | Desiccate at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.2773 mL | 6.3866 mL | 12.7732 mL |
| 5 mM | 0.2555 mL | 1.2773 mL | 2.5546 mL |
| 10 mM | 0.1277 mL | 0.6387 mL | 1.2773 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 17 reference(s) in Google Scholar.)
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