| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Compared to intramuscular injection, the bioavailability of capsules and suppositories is 33-39%, indicating incomplete absorption. Metabolisms/Metabolites Benzoquinolamide metabolites in humans and dogs are 2-acetoxy-3-(N,N-diethylcarboxamide)-1,2,3,4,6,7-hexahydro-9-hydroxy-10-methoxy-11BH-benzoquinolazine and 2-acetoxy-3-(N-ethylcarboxamide)-1,2,3,4,6,7-hexahydro-9,10-dimethoxy-11BH-benzoquinolazine: WISEMAN, EH et al., BIOCHEM PHARMAC 13, 1421 (1964). /Excerpt from table/ Benzoquinolamines in humans and dogs form 3-(N,N-diethylcarboxamido)-1,2,3,4,6,7-hexahydro-2-hydroxy-9,10-dimethoxy-11BH-benzoquinolazine: WISEMAN, EH et al., BIOCHEM PHARMAC 13, 1421 (1964). /Excerpt from table/ Biological half-life 1–1.6 hours (all formulations) |
|---|---|
| References | |
| Additional Infomation |
Benzylquinamide is a monocarboxylic acid amide. It has antiemetic, sedative, H1 receptor antagonist, muscarinic receptor antagonist, and antipsychotic effects. Benzylquinamide is a discontinued antiemetic compound with antihistamine, mild anticholinergic, and sedative effects. The mechanism of action of benzoquinamide is unclear, but it is speculated to be through antagonism of muscarinic acetylcholine receptors and histamine H1 receptors. Drug Indications Used for the prevention and treatment of nausea and vomiting induced by anesthesia and surgery, administered intramuscularly or intravenously. Mechanism of Action The mechanism of action of benzoquinamide is unclear, but it is speculated to be through antagonism of muscarinic acetylcholine receptors and histamine H1 receptors. Similar to phenothiazines, benzoquinamide appears to inhibit stimulation of chemoreceptor trigger zones. However, unlike phenothiazines, both experimental and clinical studies have found that benzoquinamide can increase cardiac output, blood pressure, and respiratory function. /HCL/
Therapeutic Use Antipsychotic; Antiemetic ...Benzoquinalamide is superior to phenothiazines in controlling nausea and vomiting...Benzoquinalamide causes drowsiness comparable to phenothiazines; no reports of hypotension or extrapyramidal reactions have been observed. ...Appears to be an effective non-phenothiazine antiemetic. ...Benzoquinalamide may be effective in patients with central nervous system depression (postoperative patients, patients with uremia or ketoacidosis, patients who have received sedatives or analgesics). It appears to be at least as effective as phenothiazines. ...Benzoquinalamide causes fewer serious adverse reactions than phenothiazines. /HCL/ Drug Warnings Contraindicated in pregnant women and children. /HCL/ Pharmacodynamics Benzoquinalamide is an antiemetic compound with antihistamine, mild anticholinergic, and sedative effects. |
| Molecular Formula |
C22H32N2O5
|
|---|---|
| Molecular Weight |
404.49988
|
| Exact Mass |
404.231
|
| CAS # |
63-12-7
|
| Related CAS # |
Benzquinamide hydrochloride;113-69-9
|
| PubChem CID |
2342
|
| Appearance |
CRYSTALS FROM DIISOPROPYL ETHER
|
| Density |
1.2±0.1g/cm3
|
| Boiling Point |
531.0±50.0°C at 760 mmHg
|
| Melting Point |
130-131.5
130-131.5 °C 131 °C |
| Flash Point |
274.9±30.1°C
|
| LogP |
2.36
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
29
|
| Complexity |
582
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O=C(C1CN2CCC3=CC(OC)=C(OC)C=C3C2CC1OC(C)=O)N(CC)CC
|
| InChi Key |
JSZILQVIPPROJI-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C22H32N2O5/c1-6-23(7-2)22(26)17-13-24-9-8-15-10-20(27-4)21(28-5)11-16(15)18(24)12-19(17)29-14(3)25/h10-11,17-19H,6-9,12-13H2,1-5H3
|
| Chemical Name |
[3-(diethylcarbamoyl)-9,10-dimethoxy-2,3,4,6,7,11b-hexahydro-1H-benzo[a]quinolizin-2-yl] acetate
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4722 mL | 12.3609 mL | 24.7219 mL | |
| 5 mM | 0.4944 mL | 2.4722 mL | 4.9444 mL | |
| 10 mM | 0.2472 mL | 1.2361 mL | 2.4722 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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