E3888
[D-Pen2,5]-Enkephalin hydrate
≥95% (HPLC)
别名:
DPDPE
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关于此项目
经验公式（希尔记法）:
C30H39N5O7S2 · xH2O
分子量:
645.79 (anhydrous basis)
NACRES:
NA.32
PubChem Substance ID:
UNSPSC Code:
12352209
MDL number:
InChI
1S/C30H39N5O7S2/c1-29(2)23(34-25(38)20(31)14-18-10-12-19(36)13-11-18)27(40)32-16-22(37)33-21(15-17-8-6-5-7-9-17)26(39)35-24(28(41)42)30(3,4)44-43-29/h5-13,20-21,23-24,36H,14-16,31H2,1-4H3,(H,32,40)(H,33,37)(H,34,38)(H,35,39)(H,41,42)/t20-,21-,23-,24-/m0/s1
SMILES string
CC1(C)SSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc3ccccc3)C(=O)N[C@H]1C(O)=O
InChI key
MCMMCRYPQBNCPH-WMIMKTLMSA-N
assay
≥95% (HPLC)
storage temp.
−20°C
Quality Level
General description
[D-Pen2,5]-Enkephalin hydrate, also called DPDPE, is a peptide and acts as a δ1-opioid receptor agonist. Opioid receptors are divided into three types called, μ, κ and δ, depending upon their ligands. These ligands are peptides and are classified as enkephalins, endorphins and dynorphins.
Application
[D-Pen2,5]-Enkephalin hydrate (DPDPE) has been used to study the pharmacodynamic and pharmacokinetic capabilities of polyethylene glycol (PEG) conjugate of DPDPE in rodents. It has been used to study the tendency of opiate self-administration in male Long-Evans rats, in ventral tegmental area (VTA).
Biochem/physiol Actions
Antinociceptive activity mediated through the δ1 receptor while the modulatory activity is mediated through the δ2 receptor. Tritiated [D-Pen2,5]-enkephalin is used as a δ1 ligand.
Other Notes
Lyophilized from 0.1% TFA in H2O
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)
法规信息
新产品
此项目有
K Akiyama et al.
Proceedings of the National Academy of Sciences of the United States of America, 82(8), 2543-2547 (1985-04-01)
Specific binding properties of the tritium-labeled delta opiate receptor agonist [3H][2-D-penicillamine, 5-D-penicillamine]enkephalin [( 3H][D-Pen2, D-Pen5]enkephalin) were characterized in the rat brain and in a mouse neuroblastoma-rat glioma hybrid cell line (NG 108-15). Saturation isotherms of [3H][D-Pen2, D-Pen5]enkephalin binding to rat
Yu-Hua Wang et al.
Scientific reports, 8(1), 14087-14087 (2018-09-22)
Dezocine is becoming dominated in China market for relieving moderate to severe pain. It is believed that Dezocine's clinical efficacy and little chance to provoke adverse events during the therapeutic process are mainly attributed to its partial agonist activity at
D P Devine et al.
The Journal of neuroscience : the official journal of the Society for Neuroscience, 14(4), 1978-1984 (1994-04-01)
Intracranial self-administration of mu- and delta-opioid agonists was demonstrated in male Long-Evans rats. Independent groups were allowed to lever-press for ventral tegmental area (VTA) microinfusions of morphine, the selective mu agonist [D-Ala2,N-Me-Phe4-Gly5-ol]-enkephalin (DAMGO), the selective delta-agonist [D-Pen2,D-Pen5]-enkephalin (DPDPE), or ineffective
K A Witt et al.
The Journal of pharmacology and experimental therapeutics, 298(2), 848-856 (2001-07-17)
Poly(ethylene glycol), or PEG, conjugation to proteins and peptides is a growing technology used to enhance efficacy of therapeutics. This investigation assesses pharmacodynamic and pharmacokinetic characteristics of PEG-conjugated [D-Pen2,D-Pen5]-enkephalin (DPDPE), a met-enkephalin analog, in rodent (in vivo, in situ) and
B Gao et al.
The Journal of pharmacology and experimental therapeutics, 294(1), 73-79 (2000-06-28)
Organic anion-transporting polypeptides (Oatps) are a rapidly growing gene family of polyspecific membrane transporters. In rat brain, Oatp1 (gene symbol Slc21a1) and Oatp2 (Slc21a5) are localized at the apical and basolateral domains, respectively, of the choroid plexus epithelium. Furthermore, Oatp2
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