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| 5mg |
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| Targets |
Rapacuronium Bromide targets the muscarinic acetylcholine receptor (mAChR), a G protein-coupled receptor that mediates the effects of acetylcholine. It is an allosteric modulator of mAChR. It binds to all muscarinic receptor subtypes at physiologically relevant concentrations and displays micromolar affinity and slight selectivity towards the M2 receptor. By modulating mAChR, Rapacuronium Bromide affects various physiological processes, including smooth muscle contraction and neurotransmission.
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| ln Vitro |
Rapacuronium has a micromolar affinity and a small degree of selectivity for the M2 receptor. It binds to all muscarinic receptor subtypes at physiologically relevant dosages. The kinetics of ACh binding and subsequent receptor activation, as measured by the stimulation of [35S]GTPγS binding, are intricately affected by rapacuronium. With an EC50 ranging from 28 μM for M2 receptors to 76 μM for M3 receptors, rapacuronium alone concentration-dependently lowers [35S]GTPγS binding to membranes, with a maximum impact of roughly 25% for odd isoforms and 15% for even isoforms. While there was a correlation (R2 = 0.76) between the EC50 values for rapacuronium's inhibition of [35S]GTPηS binding for each isoform and the affinities determined in [3H]ACh binding tests, these EC50 values were lower for all isoforms. minimal (4–12 times). Assessing the impact of 0.1, 1, and 10 μM rapacuronium on ACh-stimulated [35S]GTPγS binding revealed the compound's influence on the activation of distinct receptor subtypes by orthotopic agonists. distinct effects. Within the even subtype, rapacuronium at 1 μM and 10 μM considerably raised ACh EC50, although rapacuronium at 10 μM reduced EMAX. In this subtype, 0.1 and 1 μM rapacuronium caused an increase in EMAX of roughly 60% and 35%, respectively, and a significant 2-fold drop in ACh EC50. At 10 μM, rapacuronium bromide increased ACh EC50 by about three times without significantly altering EMAX. Rapacurium (0.1 - 10 μM) lowered the EC50 of ACh stimulation of [35S]GTPηS binding by 1.5 and 4 times at concentrations of 0.1 and 1 μM, respectively, but had no influence on the ACh effectiveness of M1 and M5 isoforms. At 10 μM rapacuronium, however, this impact was not noticeable [1].
In vitro, Rapacuronium Bromide binds to all muscarinic receptor subtypes and displays micromolar affinity and slight selectivity towards the M2 receptor. Its activity is typically measured using receptor binding assays and functional assays. Receptor binding assays determine the compound's affinity for mAChR subtypes. Functional assays measure the compound's ability to modulate mAChR-mediated signaling. |
| ln Vivo |
After administering a dose of 2×ED90, the neuromuscular effects of rapacuronium were observed in rats and guinea pigs over a period of time. The corresponding ED90 values were 5953±199 and 187±16 µg/kg, respectively [2].
In vivo, Rapacuronium Bromide was used as a neuromuscular blocking agent. It was first approved in 1999 but was later withdrawn in at least one region. Its use was limited by side effects, including bronchospasm. It is a research compound used to study muscarinic receptor pharmacology. |
| Enzyme Assay |
In vitro receptor binding assays for Rapacuronium Bromide measure its affinity for muscarinic acetylcholine receptor subtypes. Membranes from cells expressing mAChR subtypes are incubated with a radiolabeled mAChR ligand and varying concentrations of Rapacuronium Bromide. The Ki is determined from competition binding curves.
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| Cell Assay |
In vitro cell-based assays for Rapacuronium Bromide are used to study its effects on mAChR-mediated signaling. Cells expressing mAChR subtypes are treated with Rapacuronium Bromide, and downstream signaling is measured. The compound's ability to modulate mAChR-mediated responses is assessed.
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| Animal Protocol |
In vivo animal experiments for Rapacuronium Bromide were conducted to study its neuromuscular blocking effects. In a typical study, the compound was administered to animals, and muscle relaxation was measured. The compound's onset and duration of action were assessed. These studies supported its clinical use as a neuromuscular blocking agent.
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| ADME/Pharmacokinetics |
Rapacuronium Bromide has a molecular weight of 677.80 g/mol and a molecular formula of C37H61BrN2O4. It has a CAS number of 156137-99-4. It is a solid compound. For storage, it is recommended to keep the powder at -20°C. Pharmacokinetic properties such as absorption, distribution, metabolism, and excretion (ADME) have been characterized.
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| Toxicity/Toxicokinetics |
Rapacuronium Bromide is a neuromuscular blocking agent and its safety profile has been established. It was withdrawn in at least one region due to side effects, including bronchospasm. As with all research chemicals, standard laboratory safety precautions should be followed when handling Rapacuronium Bromide.
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| References | |
| Additional Infomation |
See also: Lapacuronium bromide (with active moiety).
Rapacuronium Bromide is a research compound and a pharmaceutical agent that was first approved in 1999 but was later withdrawn in at least one region. It is an allosteric modulator of the muscarinic acetylcholine receptor (mAChR). It binds to all muscarinic receptor subtypes and displays micromolar affinity and slight selectivity towards the M2 receptor. Rapacuronium Bromide is a valuable research tool for studying muscarinic receptor pharmacology. |
| Molecular Formula |
C37H61BRN2O4
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| Molecular Weight |
677.809
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| Exact Mass |
676.381
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| CAS # |
156137-99-4
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| Related CAS # |
156137-99-4 (bromide);465499-11-0 (cation);
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| PubChem CID |
5311398
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3.812
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
44
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| Complexity |
1030
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| Defined Atom Stereocenter Count |
10
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| SMILES |
CCC(=O)O[C@H]1[C@H](C[C@@H]2[C@@]1(CC[C@H]3[C@H]2CC[C@@H]4[C@@]3(C[C@@H]([C@H](C4)OC(=O)C)N5CCCCC5)C)C)[N+]6(CCCCC6)CC=C.[Br-]
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| InChi Key |
LVQTUXZKLGXYIU-GWSNJHLMSA-M
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| InChi Code |
InChI=1S/C37H61N2O4.BrH/c1-6-20-39(21-12-9-13-22-39)32-24-30-28-15-14-27-23-33(42-26(3)40)31(38-18-10-8-11-19-38)25-37(27,5)29(28)16-17-36(30,4)35(32)43-34(41)7-2;/h6,27-33,35H,1,7-25H2,2-5H3;1H/q+1;/p-1/t27-,28+,29-,30-,31-,32-,33-,35-,36-,37-;/m0./s1
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| Chemical Name |
[(2S,3S,5S,8R,9S,10S,13S,14S,16S,17R)-3-acetyloxy-10,13-dimethyl-2-piperidin-1-yl-16-(1-prop-2-enylpiperidin-1-ium-1-yl)-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl] propanoate;bromide
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| Synonyms |
Org-9487; Rapacuronium Bromide; Org 9487; Org9487; brand name Raplon;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 125 mg/mL (~184.42 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.07 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.07 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (3.07 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.4753 mL | 7.3767 mL | 14.7534 mL | |
| 5 mM | 0.2951 mL | 1.4753 mL | 2.9507 mL | |
| 10 mM | 0.1475 mL | 0.7377 mL | 1.4753 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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