H4904
(+)-Himbacine
~98% (GC), powder, muscarinic receptor antagonist
别名:
(3S,3aR,4R,4aS,8aR,9aS)-4-[(1E)-2-[(2R,6S)-1,6-dimethyl-2-piperdinyl]ethenyl]decahydro-3-methyl-naphtho[2,3-c]furan-1(3H)-one
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关于此项目
经验公式（希尔记法）:
C22H35NO2
化学文摘社编号:
分子量:
345.52
UNSPSC Code:
12352200
PubChem Substance ID:
MDL number:
SMILES string
[H][C@]12CCCC[C@]1([H])[C@@H](\C=C\[C@@H]3CCC[C@@H](C)N3C)[C@@]4([H])[C@H](C)OC(=O)[C@@]4([H])C2
assay
~98% (GC)
form
powder
optical activity
[α]/D +51.4°, c = 1.01 in chloroform(lit.)
color
off-white
solubility
ethanol: 50 mg/mL, H2O: insoluble
Gene Information
rat ... Chrm1(25229), Chrm2(81645)
Biochem/physiol Actions
Selective M2/M4 muscarinic acetylcholine receptor antagonist.
Disclaimer
Hygroscopic
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
J H Miller et al.
The Journal of pharmacology and experimental therapeutics, 263(2), 663-667 (1992-11-01)
The binding potencies for the putative M2-selective antagonist himbacine were determined in radioligand binding and in functional response assays in neuronal tissue and Chinese hamster ovary cells containing transfected muscarinic receptors. Himbacine was shown to bind to all five cloned
Yoshito Takahashi et al.
Brain research, 1339, 26-40 (2010-04-14)
Cholinergic modulation of spontaneous GABAergic currents (mIPSC) was studied using whole-cell patch methods in mouse accessory olfactory bulb slices. Carbachol (above 100 microM) administration produced an increase in the mIPSC frequency in mitral cells, but did not affect the responses
Samuel Chackalamannil et al.
Journal of medicinal chemistry, 48(19), 5884-5887 (2005-09-16)
Structurally novel thrombin receptor (protease activated receptor 1, PAR-1) antagonists based on the natural product himbacine are described. The prototypical PAR-1 antagonist 55 showed a Ki of 2.7 nM in the binding assay, making it the most potent PAR-1 antagonist
Mariappan V Chelliah et al.
Journal of medicinal chemistry, 50(21), 5147-5160 (2007-09-15)
Pursuing our earlier efforts in the himbacine-based thrombin receptor antagonist area, we have synthesized a series of compounds that incorporate heteroatoms in the C-ring of the tricyclic motif. This effort has resulted in the identification of several potent heterocyclic analogs
Mariappan V Chelliah et al.
Bioorganic & medicinal chemistry letters, 22(7), 2544-2549 (2012-03-13)
Discovery of a novel nor-seco himbacine analog as potent thrombin receptor (PAR-1) antagonist is described. Despite low plasma level, these new analogs showed excellent ex vivo efficacy in the monkey platelet aggregation assay. A potent hydroxy metabolite generated in vivo
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