| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Incomplete, with 33–39% bioavailability via the capsule and suppository routes, relative to the intramuscular route. Metabolism / Metabolites BENZQUINAMIDE YIELDS 2-ACETOXY-3-(N,N-DIETHYLCARBOXAMI DO)-1,2,3,4,6,7-HEXAHYDRO-9-HYDROXY-10-METHOXY-11BH-BENZOQUINOLIZINE & 2-ACETOXY-3-(N-ETHYLCARBOXAMIDO)-1,2,3,4,6,7-HEXAHYDRO- 9,10-DIMETHOXY-11BH-BENZOQUINOLIZINE IN MAN & DOG: WISEMAN, EH ET AL, BIOCHEM PHARMAC 13, 1421 (1964). /FROM TABLE/ BENZQUINAMIDE YIELDS 3-(N,N-DIETHYLCARBOXAMIDO)-1,2,3, 4,6,7-HEXAHYDRO-2-HYDROXY-9,10-DIMETHOXY-11BH-BENZOQUINOLIZINE IN MAN & DOG: WISEMAN, EH ET AL, BIOCHEM PHARMAC 13, 1421 (1964). /FROM TABLE/ Biological Half-Life 1-1.6 hours (for all formulations) |
|---|---|
| References | |
| Additional Infomation |
Benzquinamide is a monocarboxylic acid amide. It has a role as an antiemetic, a sedative, a H1-receptor antagonist, a muscarinic antagonist and an antipsychotic agent.
Benzquinamide is a discontinued antiemetic compound with antihistaminic, mild anticholinergic, and sedative properties. The mechanism of action is not known, but presumably benzquinamide works via antagonism of muscarinic acetycholine receptors and histamine H1 receptors. Drug Indication Used to prevent and treat nausea and vomiting associated with anesthesia and surgery, administered intramuscularly or intravenously. Mechanism of Action The mechanism of action is not known, but presumably benzquinamide works via antagonism of muscarinic acetycholine receptors and histamine H1 receptors. LIKE PHENOTHIAZINES, IT APPARENTLY INHIBITS STIMULI @ CHEMORECEPTOR TRIGGER ZONE. HOWEVER, IN CONTRAST...INCR CARDIAC OUTPUT, BLOOD PRESSURE, & RESP HAVE BEEN NOTED BOTH EXPTL & CLINICALLY WITH BENZQUINAMIDE. /HCL/ Therapeutic Uses Antipsychotic Agents; Antiemetics ...BENZQUINAMIDE HAS BEEN SHOWN TO BE SUPERIOR TO PHENOTHIAZINES IN CONTROL OF NAUSEA & VOMITING... DEGREE OF SOMNOLENCE ASSOC WITH BENZQUINAMIDE IS EQUAL TO THAT OF PHENOTHIAZINES; THERE HAVE BEEN NO REPORTED HYPOTENSION OR EXTRAPYRAMIDAL REACTIONS. ...APPEARS TO BE EFFECTIVE NON-PHENOTHIAZINE ANTIEMETIC. ...BENZQUINAMIDE MAY BE USEFUL IN PT WITH CNS DEPRESSION (POSTOPERATIVE PT, THOSE WITH UREMIA OR KETOACIDOSIS, THOSE WHO HAVE RECEIVED SEDATIVE OR ANALGESIC DRUGS). IT APPEARS TO BE @ LEAST AS EFFECTIVE AS PHENOTHIAZINES. ... BENZQUINAMIDE PRODUCES FEWER SERIOUS ADVERSE REACTIONS THAN PHENOTHIAZINES. /HCL/ Drug Warnings IT SHOULD NOT BE USED EITHER IN PREGNANT WOMEN OR IN CHILDREN. /HCL/ Pharmacodynamics Benzquinamide is an antiemetic compound with antihistaminic, mild anticholinergic, and sedative properties. |
| 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
