| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg | |||
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| 500mg | |||
| Other Sizes |
| Targets |
α1 adrenoceptor
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|---|---|
| ln Vivo |
Benoxathian hydrochloride (10 nM; paraventricular nucleus injection) totally reverses 2.5, 5.0, or 10.0 mg/kg phenylpropanolamine (IP)-induced anorexia in rats [1].
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| Animal Protocol |
Microinjection of the alpha-1 adrenergic receptor antagonist benoxathian (0, 2.5, 5.0 or 10.0 nmol) into the PVN was found to have no effect on baseline feeding behavior. Microinjection of 10.0 nmol benoxathian into the PVN completely reversed the anorexia induced by 2.5, 5.0 or 10.0 mg/kg PPA (IP), yet did not alter the hypodipsia produced by PPA. These data strongly suggest that PPA anorexia is mediated by an alpha-1 adrenergic satiety mechanism within the PVN.[1]
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| References |
[1]. Wellman PJ, et al. Reversal of phenylpropanolamine anorexia in rats by the alpha-1 receptor antagonist benoxathian. Pharmacol Biochem Behav. 1991 Apr;38(4):905-8.
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| Additional Infomation |
Adrenergic alpha receptor antagonists: These drugs bind to alpha adrenergic receptors without activating them, thus blocking the effects of endogenous or exogenous adrenergic agonists. Adrenergic alpha receptor antagonists are used to treat hypertension, vasospasm, peripheral vascular disease, shock, and pheochromocytoma. Antihypertensive drugs: These are drugs used to treat acute or chronic vascular hypertension, regardless of their pharmacological mechanism. Antihypertensive drugs include: diuretics (especially thiazide diuretics); adrenergic beta receptor antagonists; adrenergic alpha receptor antagonists; angiotensin-converting enzyme inhibitors; calcium channel blockers; ganglion blockers; and vasodilators. Phenylehrenololamine (PPA) is a phenethylamine anorexic drug that acts primarily as a direct agonist on alpha-1 adrenergic receptors and also possesses some alpha-2 adrenergic activity. Direct injection of PPA and the α1 receptor agonist 1-phenylephrine into the paraventricular nucleus (PVN) of rats inhibited feeding. This study aimed to verify whether systemic PPA inhibited feeding by acting on the α1 receptor population in the PVN. To this end, we performed unilateral PVN localization-guided cannulation in adult male rats. The results showed that microinjection of the α1 adrenergic receptor antagonist phenoxythiazide (0, 2.5, 5.0 or 10.0 nmol) into the PVN had no effect on the baseline feeding behavior of rats. Microinjection of 10.0 nmol of phenoxythiazide into the paraventricular nucleus (PVN) completely reversed the anorexia induced by 2.5, 5.0 or 10.0 mg/kg PPA (intraperitoneal injection), but did not change the PPA-induced reduction in water intake. These data strongly suggest that PPA-induced anorexia is mediated by an α-1 adrenergic satiety mechanism in the PVN. [1]
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| Molecular Formula |
C19H23NO4S.HCL
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|---|---|
| Molecular Weight |
397.91616
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| Exact Mass |
397.111
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| CAS # |
92642-97-2
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| PubChem CID |
10386130
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| Appearance |
Typically exists as solid at room temperature
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| Boiling Point |
500.7ºC at 760 mmHg
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| Flash Point |
256.6ºC
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| LogP |
4.418
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
26
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| Complexity |
374
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=C(C(=CC=C1)OC)OCCNCC2CSC3=CC=CC=C3O2.Cl
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| InChi Key |
OWRADFDDJVNMGL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H23NO4S.ClH/c1-21-16-7-5-8-17(22-2)19(16)23-11-10-20-12-14-13-25-18-9-4-3-6-15(18)24-14;/h3-9,14,20H,10-13H2,1-2H3;1H
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| Chemical Name |
N-(2,3-dihydro-1,4-benzoxathiin-2-ylmethyl)-2-(2,6-dimethoxyphenoxy)ethanamine;hydrochloride
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| Synonyms |
Benoxathian hydrochloride; 92642-97-2; Benoxathian HCl; Benoxathian (hydrochloride); BenoxathianHydrochloride; Benzoxathian hydrochloride; NIOSH/DM2930000; 2-[[[2-(2,6-Dimethoxyphenoxy)ethyl]-amino]-methyl]-1,4-benzoxathian hydrochloride;
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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 : ~250 mg/mL (~628.27 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.23 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 (5.23 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 (5.23 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 | 2.5131 mL | 12.5653 mL | 25.1307 mL | |
| 5 mM | 0.5026 mL | 2.5131 mL | 5.0261 mL | |
| 10 mM | 0.2513 mL | 1.2565 mL | 2.5131 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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