E3148
Endomorphin 2
储存温度
−20°C
SMILES字符串
N[C@@H](Cc1ccc(O)cc1)C(=O)N2CCC[C@H]2C(=O)N[C@@H](Cc3ccccc3)C(=O)N[C@@H](Cc4ccccc4)C(N)=O
InChI
1S/C32H37N5O5/c33-25(18-23-13-15-24(38)16-14-23)32(42)37-17-7-12-28(37)31(41)36-27(20-22-10-5-2-6-11-22)30(40)35-26(29(34)39)19-21-8-3-1-4-9-21/h1-6,8-11,13-16,25-28,38H,7,12,17-20,33H2,(H2,34,39)(H,35,40)(H,36,41)/t25-,26-,27-,28-/m0/s1
InChI key
XIJHWXXXIMEHKW-LJWNLINESA-N
基因信息
human ... OPRM1(4988)
mouse ... OPRM1(18390)
rat ... OPRM1(25601)
Amino Acid Sequence
Tyr-Pro-Phe-Phe-NH2
一般描述
Endomorphin 2 is an endogenous ligand for μ-opioid receptor (MOR). It is a neuropeptide and has the sequence Tyr-Pro-Phe-Phe-NH2. It has a greater affinity for MOR1 receptor than MOR2. It resides in primary sensory afferent fibers, and might be the predominant ligand to regulate pain perception. In dynorphin-induced allodynia mice models, endomorphin has anti-allodynic effects. In tail flick test, it produces short-lived antinociception, which is naloxone-sensitive.
生化/生理作用
Potent, selective endogenous μ opioid receptor agonist.
法律信息
Sold under license to US patent number 6,303,578
储存分类代码
13 - Non Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
个人防护装备
Eyeshields, Gloves, type N95 (US)
法规信息
新产品
此项目有
Attila Keresztes et al.
Journal of medicinal chemistry, 51(14), 4270-4279 (2008-06-25)
Endomorphins were subjected to a number of structural modifications in a search for their bioactive conformations. The alicyclic beta-amino acids cis-(1 S,2 R)ACPC/ACHC, cis-(1 R,2 S)ACPC/ACHC, trans-(1 S,2 S)ACPC/ACHC, and trans-(1 R,2 R)ACPC/ACHC were introduced into endomorphins to examine the
Jakub Fichna et al.
Bioorganic & medicinal chemistry letters, 18(4), 1350-1353 (2008-01-22)
The mu-opioid agonists endomorphin-1 (Tyr-Pro-Trp-Phe-NH(2)) and endomorphin-2 (Tyr-Pro-Phe-Phe-NH(2)) exhibit an extremely high selectivity for the mu-opioid receptor and thus represent a potential framework for modification into mu-antagonists. Here we report on the synthesis and biological evaluation of novel [d-2-Nal(4)]endomorphin-2 analogs
Csaba Tömböly et al.
Journal of medicinal chemistry, 51(1), 173-177 (2007-12-08)
The constitutional similarity with different secondary structure preference between the Aba-Gly and the spiro-Aba-Gly scaffolds were exploited to design the novel endomorphin-2 analogs Tyr-spiro-( R/ S)-Aba-Gly-Phe-NH(2) ( 1 and 2) and Tyr-( R/ S)-Aba-Gly-Phe-NH(2) ( 3 and 4). The (
Steven Ballet et al.
Journal of medicinal chemistry, 49(13), 3990-3993 (2006-06-23)
The Aba-Gly scaffold, incorporated into Dmt-Tic ligands (H-Dmt-Tic-Gly-NH-CH2-Ph, H-Dmt-Tic-Gly-NH-Ph, H-Dmt-Tic-NH-CH2-Bid), exhibited mixed micro/delta or delta opioid receptor activities with micro agonism. Substitution of Tic by Aba-Gly coupled to -NH-CH2-Ph (1), -NH-Ph (2), or -Bid (Bid=1H-benzimidazole-2-yl) (3) shifted affinity (Ki(micro)=0.46, 1.48
L S Stone et al.
Neuroreport, 8(14), 3131-3135 (1997-10-23)
Two highly-selective mu-opioid receptor agonists, endomorphin-1 and -2, were recently purified from bovine brain and are postulated to be endogenous mu-opioid receptor ligands. We sought to determine the effects of these ligands at the spinal level in mice. Endomorphin-1 and
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