Stereochemistry | ABSOLUTE |
Molecular Formula | C32H44N2O8.BrH |
Molecular Weight | 665.612 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 12 / 12 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Br.[H][C@@]12C[C@H]3[C@H](OC)[C@]1(O)[C@](O)(C[C@@H]3OC)[C@H]4C[C@H]5[C@@]26[C@H](CC[C@]5(CN(CC)[C@]46[H])OC(=O)C7=C(NC(C)=O)C=CC=C7)OC
InChI
InChIKey=CFFYROOPXPKMEQ-IPZKEBFRSA-N
InChI=1S/C32H44N2O8.BrH/c1-6-34-16-29(42-28(36)18-9-7-8-10-21(18)33-17(2)35)12-11-25(40-4)31-23(29)14-20(26(31)34)30(37)15-22(39-3)19-13-24(31)32(30,38)27(19)41-5;/h7-10,19-20,22-27,37-38H,6,11-16H2,1-5H3,(H,33,35);1H/t19-,20+,22+,23-,24+,25+,26-,27+,29-,30+,31+,32+;/m1./s1
Lappaconitine is an alkaloid isolated from the root of Aconltitum sinomantanum Nakai. It has a strong analgesic activity that does not involve the opioid receptor. It was shown to have class-I antiarrhythmic action and irreversibly blocks cloned human heart (hH1) channels by binding to the site 2 receptor.
CNS Activity
Originator
Approval Year
PubMed
Patents
Sample Use Guides
Lappaconitine (8 mg) was intravenously dripped to patients in the lappaconitine group 30 min before ending the operation. PCIA started as soon as the end of the surgery and the total dose of lappaconitine was 36 mg.
Route of Administration:
Intravenous
Right isolated guinea-pig atria became
bradycardic at 3 uM lappaconitine, and at 4.5 uM one of
six right atria ceased contracting. Asystolia was also observed
in left atria at concentrations about 600 nM, but all
of the asystolic atria resumed contraction as the stimulation
current was increased, indicating an elevation of the
excitation threshold.