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经验公式(希尔记法):
C26H25NO4 · CH4O3S · xH2O
化学文摘社编号:
分子量:
511.59 (anhydrous basis)
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
产品名称
Naltriben methanesulfonate hydrate, ≥98% (HPLC), solid
SMILES string
O.CS(O)(=O)=O.Oc1ccc2C[C@H]3N(CC[C@@]45[C@@H](Oc1c24)c6oc7ccccc7c6C[C@@]35O)CC8CC8
InChI key
VAGWKZSGWSRENH-HIAJFTJMSA-N
InChI
1S/C26H25NO4.CH4O3S.H2O/c28-18-8-7-15-11-20-26(29)12-17-16-3-1-2-4-19(16)30-22(17)24-25(26,21(15)23(18)31-24)9-10-27(20)13-14-5-6-14;1-5(2,3)4;/h1-4,7-8,14,20,24,28-29H,5-6,9-13H2;1H3,(H,2,3,4);1H2/t20-,24+,25+,26-;;/m1../s1
assay
≥98% (HPLC)
form
solid
drug control
regulated under CDSA - not available from Sigma-Aldrich Canada
color
off-white
solubility
DMSO: 14 mg/mL at ~60 °C
storage temp.
−20°C
Quality Level
Application
Naltriben methanesulfonate hydrate has been used in the assessment of parasite growth and evaluation of growth inhibition. It has also been used to understand the action of deltorphin-II in exhibiting its antimalarial effect.
Biochem/physiol Actions
Naltriben methanesulfonate is a highly selective δ2 opioid receptor antagonist. The relative ability of the delta antagonists benzylidenenaltrexone and naltriben to inhibit DPDPE-stimulated [35S]GTPgammaS binding suggests that the opioid receptor is of the delta-2 subtype. Ligand binding assays demonstrates biphasic binding of the antagonist to the single receptor type. [35S]GTPgammaS binding is also stimulated by [D-Ser2,Leu5,Thr6]enkephalin > deltorphin II = DPDPE = etorphine > levallorphan = diprenorphine = nalorphine = naltrindole.
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
A E Takemori et al.
Life sciences, 50(20), 1491-1495 (1992-01-01)
The pharmacological profile of naltrindole (NTI) and three of its analogues, N-methyl-NTI (N-Me-NTI), oxymorphindole (OMI) and naltriben (NTB) were studied in antinociceptive assays. The compounds were found to have agonist activities that appear to be mediated mainly by kappa opioid
Profiling molecular factors associated with pyknosis and developmental arrest induced by an opioid receptor antagonist and dihydroartemisinin in Plasmodium falciparum
Asahi H, et al.
Testing, 12(9), e0184874-e0184874 (2017)
Liliana Matos et al.
Orphanet journal of rare diseases, 9, 180-180 (2014-12-11)
Mutations affecting RNA splicing represent more than 20% of the mutant alleles in Sanfilippo syndrome type C, a rare lysosomal storage disorder that causes severe neurodegeneration. Many of these mutations are localized in the conserved donor or acceptor splice sites
Inhibitory effect of deltorphin-II on development of malaria in Plasmodium berghei-infected mice
Ajitbhai GA, et al.
MalariaWorld journal, 6, 3-3 (2017)
Carla Martins et al.
Human mutation, 40(8), 1084-1100 (2019-06-23)
Mucopolysaccharidosis type IIIC (MPSIIIC) is a severe, rare autosomal recessive disorder caused by variants in the heparan-α-glucosaminide N-acetyltransferase (HGSNAT) gene which result in lysosomal accumulation of heparan sulfate. We analyzed clinical presentation, molecular defects and their haplotype context in 78
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