Synonym
LEK 8829; LEK-8829; LEK8829;
IUPAC/Chemical Name
(6aR,9R)-N,7-dimethyl-N-(prop-2-yn-1-yl)-4,6,6a,7,8,9-hexahydroindolo[4,3-fg]quinoline-9-carboxamide methanesulfonate
InChi Key
MZNFBRQGHUXNJH-KEZWHQCISA-N
InChi Code
InChI=1S/C20H21N3O.CH4O3S/c1-4-8-22(2)20(24)14-9-16-15-6-5-7-17-19(15)13(11-21-17)10-18(16)23(3)12-14;1-5(2,3)4/h1,5-7,9,11,14,18,21H,8,10,12H2,2-3H3;1H3,(H,2,3,4)/t14-,18-;/m1./s1
SMILES Code
[H][C@@]1(N(C)C[C@H](C(N(C)CC#C)=O)C=C12)CC3=CNC4=C3C2=CC=C4.CS(=O)(O)=O
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
>3 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
2934.99.03.00
Preparing Stock Solutions
The following data is based on the
product
molecular weight
415.50
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
1: Milivojevic N, Krisch I, Sket D, Zivin M. The dopamine D1 receptor agonist and D2 receptor antagonist LEK-8829 attenuates reinstatement of cocaine-seeking in rats. Naunyn Schmiedebergs Arch Pharmacol. 2004 Jun;369(6):576-82. Epub 2004 May 7. PubMed PMID: 15138661.
2: Zivin M, Sprah L, Sket D. Antiparkinsonian potential of interaction of LEK-8829 with bromocriptine. Eur J Pharmacol. 1998 May 22;349(2-3):151-7. PubMed PMID: 9671092.
3: Zivin M, Sprah L, Sket D. The D1 receptor-mediated effects of the ergoline derivative LEK-8829 in rats with unilateral 6-hydroxydopamine lesions. Br J Pharmacol. 1996 Nov;119(6):1187-96. PubMed PMID: 8937722; PubMed Central PMCID: PMC1915887.
4: Glavan G, Sket D, Zivin M. Modulation of neuroleptic activity of 9,10-didehydro-N-methyl-(2-propynyl)-6-methyl-8-aminomethylergoline bimaleinate (LEK-8829) by D1 intrinsic activity in hemi-parkinsonian rats. Mol Pharmacol. 2002 Feb;61(2):360-8. PubMed PMID: 11809861.
5: Krisch I, Bole-Vunduk B, Pepelnak M, Lavric B, Ocvirk A, Budihna MV, Sket D. Pharmacological studies with two new ergoline derivatives, the potential antipsychotics LEK-8829 and LEK-8841. J Pharmacol Exp Ther. 1994 Oct;271(1):343-52. PubMed PMID: 7965734.
6: Sprah L, Zivin M, Sket D. Ergoline derivative LEK-8829-induced turning behavior in rats with unilateral striatal ibotenic acid lesions: interaction with bromocriptine. J Pharmacol Exp Ther. 1999 Mar;288(3):1093-100. PubMed PMID: 10027846.
