Description
Cas:510-77-0
Product Information:
(-)-Narwedine is a cholinesterase (AChE) inhibitor for the treatment of mild to moderate Alzheimer's disease.
Chemical Formula: C17H19NO3
Exact Mass: 285.136
Molecular Weight: 285.343
Elemental Analysis: C, 71.56; H, 6.71; N, 4.91; O, 16.82
Synonym:
Galanthaminone
(-)-Narwedine
Narwedine
3-Deoxy-3-oxo-galanthamine
Chemical Name: (4aS,8aS)-4a,5,9,10,11,12-Hexahydro-3-methoxy-11-methyl-6H-benzofuro[3a,3,2-ef][2]benzazepin-6-one
InChi Key:
QENVUHCAYXAROT-YOEHRIQHSA-N
InChi Code: InChI=1S/C17H19NO3/c1-18-8-7-17-6-5-12(19)9-14(17)21-16-13(20-2)4-3-11(10-18)15(16)17/h3-6,14H,7-10H2,1-2H3/t14-,17-/m0/s1
Smiles Code:
O=C1C=C[C@@]23CCN(C)CC4=CC=C(OC)C(O[C@@]3([H])C1)=C24
Technical Data:
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
In Vitro:
Galanthaminone reduces the action of AChE and therefore tends to increase the concentration of acetylcholine in the brain. is also an allosteric ligand at nicotinic acetylcholine receptors. It has shown activity in modulating the nicotinic cholinergic receptors on cholinergic neurons to increase acetylcholine release.
In Vivo:
Absorption of Galanthaminone is rapid and complete and shows linear pharmacokinetics. It is well absorbed with absolute oral bioavailability between 80 and 100%. It has a half-life of seven hours. Peak effect of inhibiting acetylcholinesterase was achieved about one hour after a single oral dose of 8 mg in some healthy volunteers.
References:
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Bickel U, Thomsen T, Weber W, Fischer JP, Bachus R, Nitz M, Kewitz H.Pharmacokinetics of galanthamine in humans and corresponding cholinesterase inhibition. Clin Pharmacol Ther. 1991 Oct;50(4):420-8. PubMed PMID: 1914378.
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Thomsen T, Bickel U, Fischer JP, Kewitz H. Stereoselectivity of cholinesterase inhibition by galanthamine and tolerance in humans. Eur J Clin Pharmacol.1990;39(6):603-5. PubMed PMID: 2095347.
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Mihailova D, Yamboliev I, Zhivkova Z, Tencheva J, Jovovich V. Pharmacokinetics of galanthamine hydrobromide after single subcutaneous and oral dosage in humans. Pharmacology. 1989;39(1):50-8. PubMed PMID: 2587617.
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Mihailova D, Velkov M, Zhivkova Z. In vitro metabolism of galanthamine hydrobromide (Nivalin) by rat and rabbit liver homogenate. Eur J Drug MetabPharmacokinet. 1987 Jan-Mar;12(1):25-30. PubMed PMID: 3609070.
Products are for research use only. Not for human use.
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