Synonym
Lorcainide hydrochloride; EINECS 261-504-6; Lopantrol; Lorcainide HCl; Ro 13-1042; R 15889; R-15889; R15889
IUPAC/Chemical Name
N-(4-chlorophenyl)-N-(1-isopropylpiperidin-4-yl)-2-phenylacetamide hydrochloride
InChi Key
FSFSWNBDCJVFGI-UHFFFAOYSA-N
InChi Code
InChI=1S/C22H27ClN2O.ClH/c1-17(2)24-14-12-21(13-15-24)25(20-10-8-19(23)9-11-20)22(26)16-18-6-4-3-5-7-18;/h3-11,17,21H,12-16H2,1-2H3;1H
SMILES Code
O=C(N(C1=CC=C(Cl)C=C1)C2CCN(C(C)C)CC2)CC3=CC=CC=C3.[H]Cl
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
Biological target:
Lorcainide hydrochloride is a antiarrhythmic agent with local anaesthetic activity.
In vivo activity:
The inhibitory action of lorcainide on the myocardial Na(+)-K(+)-ATPase (EC 3.6.1.3) activity was studied in guinea-pig heart preparations at medium K+ concentrations of 2.5, 5.0 and 10 mM. Lorcainide exhibited characteristically similar concentration-dependent inhibitory effects at all three K+ concentrations tested.
Reference: Br J Pharmacol. 1991 Dec;104(4):793-6. https://pubmed.ncbi.nlm.nih.gov/1667285/
Preparing Stock Solutions
The following data is based on the
product
molecular weight
407.38
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 |
Formulation protocol:
1. Almotrefi AA, Dzimiri N. Variations in potassium concentration modify the inhibitory effect of lorcainide on myocardial Na(+)-K(+)-ATPase activity. Br J Pharmacol. 1991 Dec;104(4):793-6. doi: 10.1111/j.1476-5381.1991.tb12508.x. PMID: 1667285; PMCID: PMC1908833.
In vivo protocol:
1. Almotrefi AA, Dzimiri N. Variations in potassium concentration modify the inhibitory effect of lorcainide on myocardial Na(+)-K(+)-ATPase activity. Br J Pharmacol. 1991 Dec;104(4):793-6. doi: 10.1111/j.1476-5381.1991.tb12508.x. PMID: 1667285; PMCID: PMC1908833.
1: Luo X, Zeng FD. [HPLC method for determination of lorcainide hydrochloride in human serum]. Yao Xue Xue Bao. 1995;30(8):605-9. Chinese. PubMed PMID: 8571780.
2: Somberg JC, Laux B, Wynn J, Keefe D, Miura DS. Lorcainide therapy in a cardiac arrest population. Am Heart J. 1986 Apr;111(4):648-53. PubMed PMID: 3953387.
3: Lauwers WF, Meuldermans WE, Bracke JO. Mass spectral investigation of the metabolites of lorcainide in man. Eur J Drug Metab Pharmacokinet. 1983 Oct-Dec;8(4):351-62. PubMed PMID: 6673972.
4: Shita A, Bernard R, Mostinckx R, Debacker M. Haemodynamic reactions after intravenous injection of lorcainide hydrochloride in acute myocardial infarction. Eur J Cardiol. 1981;12(5):237-42. PubMed PMID: 7250167.
5: Amery WK, Heykants JJ, Xhonneux R, Towse G, Oettel P, Gough DA, Janssen PA. Lorcainide (R 15 889), a first review. Acta Cardiol. 1981;36(3):207-34. Review. PubMed PMID: 7020313.
6: Woestenborghs R, Michiels M, Heykants J. Simultaneous gas chromatographic determination of lorcainide hydrochloride and three of its principal metabolites in biological samples. J Chromatogr. 1979 Oct 11;164(2):169-76. PubMed PMID: 541407.
7: Carmeliet E, Janssen PA, Marsboom R, Van Nueten JM, Xhonneux R. Antiarrhythmic, electrophysiologic and hemodynamic effects of lorcainide. Arch Int Pharmacodyn Ther. 1978 Jan;231(1):104-30. PubMed PMID: 637616.
