Stereochemistry | ABSOLUTE |
Molecular Formula | C35H60N2O4.2Br |
Molecular Weight | 732.67 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 10 / 10 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
[Br-].[Br-].[H][C@@]12C[C@@H]([C@H](OC(C)=O)[C@@]1(C)CC[C@@]3([H])[C@@]2([H])CC[C@@]4([H])C[C@H](OC(C)=O)[C@H](C[C@]34C)[N+]5(C)CCCCC5)[N+]6(C)CCCCC6
InChI
InChIKey=NPIJXCQZLFKBMV-YTGGZNJNSA-L
InChI=1S/C35H60N2O4.2BrH/c1-24(38)40-32-21-26-13-14-27-28(35(26,4)23-31(32)37(6)19-11-8-12-20-37)15-16-34(3)29(27)22-30(33(34)41-25(2)39)36(5)17-9-7-10-18-36;;/h26-33H,7-23H2,1-6H3;2*1H/q+2;;/p-2/t26-,27+,28-,29-,30-,31-,32-,33-,34-,35-;;/m0../s1
Molecular Formula | BrH |
Molecular Weight | 80.912 |
Charge | 0 |
Count |
MOL RATIO
2 MOL RATIO (average) |
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Molecular Formula | C35H60N2O4 |
Molecular Weight | 572.8619 |
Charge | 2 |
Count |
MOL RATIO
1 MOL RATIO (average) |
Stereochemistry | MIXED |
Additional Stereochemistry | No |
Defined Stereocenters | 10 / 10 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
Pancuronium (trademarked as Pavulon) is an aminosteroid muscle relaxant with various medical uses. Pancuronium is a typical non-depolarizing curare-mimetic muscle relaxant. It competitively inhibits the nicotinic acetylcholine receptor at the neuromuscular junction by blocking the binding of acetylcholine. It has slight vagolytic activity, causing an increase in heart rate, but no ganglioplegic (i.e., blocking ganglions) activity. It is a very potent muscle relaxant drug, with an ED95 of only 60 µg/kg body weight. The onset of action is relatively slow compared to other similar drugs, in part due to its low dose - an intubating dose takes 3–6 minutes for full effect. Clinical effects (muscle activity lower than 25% of physiological) last for about 100 minutes. The time needed for full (over 90% muscle activity) recovery after single administration is about 120–180 minutes in healthy adults. Pancuronium is used with general anesthesia in surgery for muscle relaxation and as an aid to intubation or ventilation. It does not have sedative or analgesic effects. Side-effects include moderately raised heart rate and thereby arterial pressure and cardiac output, excessive salivation, apnea and respiratory depression, rashes, flushing, and sweating. The muscular relaxation can be dangerous for the seriously ill and it can accumulate leading to extended weakness. Pancuronium is not preferable to long-term use in ICU-ventilated patients. Pancuronium is also used as one component of a lethal injection in the administration of the death penalty in some parts of the United States.
CNS Activity
Originator
Approval Year
Doses
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as victim
Sourcing
PubMed
Patents
Sample Use Guides
Load: 0.04-0.1 mg/kg IV
Maintenance: 0.015-0.1 mg/kg IV q30-60min OR
Continuous infusion: 0.1 mg/kg/hr IV
Dose should be calculated based on ideal body weight
Monitoring of muscle twitch response to a peripheral nerve stimulator is advised
Route of Administration:
Intravenous
HEK293 cells were prepared for patch clamp recording by replacing the culture medium with an extracellular solution consisting of 150 mM NaCl, 5.6 mM KCl, 1.8 mM CaCl2, 1.0 mM MgCl2, and 10 mM HEPES, pH 7.3. Subsequently, 3−5 μl of polystyrene beads coated with a monoclonal antibody specific for the CD8 antigen (Dyna-beads; Dynal, Lake Success, NY) were added to the culture dish. Good expression of nAChR channels in excised patches was found for most cells having two or three beads attached. Patch pipettes, filled with a solution consisting of 140 mM KCl, 5 mM EGTA, 5 mM MgCl2, and 10 mM HEPES, pH 7.3, had resistances of 3−6 MΩ. An outside-out patch24 with a seal resistance of 5 GΩ or greater was excised from a cell and moved into position at the outflow of a HSSE-2 rapid perfusion device (ALA Scientific Instruments, Westbury, NY). The perfusion system consisted of solution reservoirs, manual switching valves, a solenoid-driven pinch valve, and two tubes inserted into the culture dish and had a time resolution of less than 100 μs. One tube contained extracellular solution without agonist (normal solution); the other contained extracellular solution with 300 μM acetylcholine (test solution). In the control protocol, the patch, initially perfused with normal solution, was exposed to a series of ten 0.25- s exposures to the test solution at 5-s intervals. Manual valves were used to connect to reservoirs containing a defined concentration of competitive antagonist (Pancuronium ) with or without acetylcholine. An equilibrium (+/+) protocol was performed by exposing the patch to acetylcholine plus antagonist for 0.25 s, with a 5-s interval of antagonist alone. After switching back to antagonist free solutions, the control protocol was repeated