E3273
Endomorphin 1
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](Cc3c[nH]c4ccccc34)C(=O)N[C@@H](Cc5ccccc5)C(N)=O
InChI
1S/C34H38N6O5/c35-26(17-22-12-14-24(41)15-13-22)34(45)40-16-6-11-30(40)33(44)39-29(19-23-20-37-27-10-5-4-9-25(23)27)32(43)38-28(31(36)42)18-21-7-2-1-3-8-21/h1-5,7-10,12-15,20,26,28-30,37,41H,6,11,16-19,35H2,(H2,36,42)(H,38,43)(H,39,44)/t26-,28-,29-,30-/m0/s1
InChI key
ZEXLJFNSKAHNFH-SYKYGTKKSA-N
基因信息
human ... OPRM1(4988)
mouse ... OPRM1(18390)
rat ... OPRM1(25601)
Amino Acid Sequence
Tyr-Pro-Trp-Phe-NH2
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
S Ide et al.
Japanese journal of pharmacology, 83(4), 306-311 (2000-09-23)
Endomorphin-1 is a novel endogenous peptide that is highly selective for the mu-opioid receptor over the delta- and kappa-opioid receptors. The structural basis of high selectivity of endomorphin-1 to the mu-opioid receptor was examined using chimeric receptors between mu- and
Gina F Marrone et al.
ACS chemical neuroscience, 7(12), 1717-1727 (2016-09-21)
The mu opioid receptor gene undergoes extensive alternative splicing. Mu opioids can be divided into three classes based on the role of different groups of splice variants. Morphine and methadone require only full length seven transmembrane (7TM) variants for analgesia
Sarah A Nickolls et al.
PloS one, 8(12), e83691-e83691 (2014-01-01)
Agonists at the µ-opioid receptor are known to produce potent analgesic responses in the clinical setting, therefore, an increased understanding of the molecular interactions of ligands at this receptor could lead to improved analgesics. As historically morphine has been shown
M G Paterlini et al.
Biophysical journal, 78(2), 590-599 (2000-02-02)
A series of diastereoisomers of endomorphin-1 (EM1, Tyr(1)-Pro(2)-Trp(3)-Phe(4)-NH(2)) have been synthesized and their potency measured using the guinea pig ileum assay. [D-Phe(4)]EM1 possessed 1/10 the potency of EM1, while potencies of [D-Tyr(1)]EM1 and [D-Trp(3)]EM1 were 50- and 100-fold lower, respectively.
Laura Pont et al.
Electrophoresis, 37(5-6), 795-808 (2015-12-20)
In this work, an untargeted metabolomic approach based on sensitive analysis by on-line solid-phase extraction capillary electrophoresis mass spectrometry (SPE-CE-MS) in combination with multivariate data analysis is proposed as an efficient method for the identification of biomarkers of Huntington's disease
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