No changes were seen between groups in the significant conditioned place preference (CPP) produced by oxycodone (ip; 5, 10, and 15 mg/kg; days 4–11). Phentermine, the positive control group, only significantly increased CPP at 3 mg/kg, though[1]. ..Inhaling oxytropium bromide causes the force-frequency curve to shift higher two hours after inhalation and prevents endotoxin injection from causing the force-frequency curve to drop [1]. Acetylcholine (ACh)-induced drug resistance is potently and continuously inhibited by oxitropium bromide. The rise in resistance brought on by histamine, serotonin, leukotriene D4, or antigens is inhibited by oxytropium bromide [2]. The reduction in mucus scores brought on by intravenous histamine was considerably lessened by inhaled doses of the anticholinergic medication oxitropium bromide at 1.5 μg and above, but not by inhaled histamine [3].

Animal/Disease Models: Male Wistar rat [1]
Doses: 5, 10, 15 mg/kg; Administration on days 4-11: intraperitoneal (ip) injection
Experimental Results: Significant CPP was shown in vivo.

Absorption, Distribution and Excretion
A peak plasma concentration of oxetacaine of approximately 20 ng/ml is attained about one hour after oral administration. LEss than 1/3 of the administered dose is absorbed as it undergoes extensive metabolism.
Less than 0.1% of the amdinistered dose is recovered in urine within 24 hours in the form of unchanged oxetacaine or its metabolites.
This pharmacokinetic property has not been studied.
This pharmacokinetic property has not been studied.

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Metabolism / Metabolites
Oxetacaine is rapidly and extensively metabolized hepatically. After metabolism, there is a formation of primary metabolites such as beta-hydroxy-mephentermine and beta-hydroxy-phentermine. The major metabolites are found in the plasma in insignificant amounts.

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Biological Half-Life
Oxetacaine presents a very short half-life of approximately one hour.

Protein Binding
Due to the low half-life, it is thought that oxetacaine, when absorbed, presents a very low protein plasma binding.

[1]. Oxethazaine and related congeners: a series of highly potent local anesthetics. Proc Soc Exp Biol Med. 1962 Mar;109:664-8.

[2]. The abuse potential of oxethazaine: Effects of oxethazaine on drug-seeking behavior and analysis of its metabolites in plasma and hair in animal models. Pharmacology, Biochemistry and Behavior.

Oxethazaine is a white powder. (NTP, 1992)
Oxethazaine is an amino acid amide.
Oxetacaine, also called oxethazaince, is a potent surface analgesic with the molecular formula N, N-bis-(N-methyl-N-phenyl-t-butyl-acetamide)-beta-hydroxyethylamine that conserves its unionized form at low pH levels. Its actions have shown to relieve dysphagia, relieve pain due to reflux, chronic gastritis, and duodenal ulcer. Oxetacaine is approved by Health Canada since 1995 for its use as an antacid combination in over-the-counter preparations. It is also in the list of approved derivatives of herbal products by the EMA.

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Drug Indication
Oxetacaine is available as an over-the-counter antacid and it is used to alleviate pain associated with gastritis, peptic ulcer disease, heartburn, esophagitis, hiatus hernia, and anorexia.

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Mechanism of Action
Oxetacaine inhibits gastric acid secretion by suppressing gastrin secretion. Moreover, oxetacaine exerts a local anesthetic effect on the gastric mucosa. This potent local anesthetic effect of oxetacaine may be explained by its unique chemical characteristics in which, as a weak base, it is relatively non-ionized in acidic solutions whereas its hydrochloride salt is soluble in organic solvents and it can penetrate cell membranes. Oxetacaine diminishes the conduction of sensory nerve impulses near the application site which in order reduces the permeability of the cell membrane to sodium ions. This activity is performed by the incorporation of the unionized form into the cell membrane.

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Pharmacodynamics
Oxetacaine improves common gastrointestinal symptoms. Oxetacaine is part of the anesthetic antacids which increase the gastric pH while providing relief from pain for a longer period of duration at a lower dosage. This property has been reported to relieve the symptoms of hyperacidity. Oxetacaine is reported to produce a reversible loss of sensation and to provide a prompt and prolonged relief of pain. In vitro, oxetacaine was showed to produce an antispasmodic action on the smooth muscle and block the action of serotonin. The local efficacy of oxetacaine has been proven to be 2000 times more potent than lignocaine and 500 times more potent than cocaine. Its anesthetic action produces the loss of sensation which can be explained by its inhibitory activity against the nerve impulses and de decrease in permeability of the cell membrane.

C28H41N3O3

467.654

467.314

126-27-2

13930-31-9 (hydrochloride)

4621

White to off-white solid powder

1.1±0.1 g/cm3

630.4±55.0 °C at 760 mmHg

104-105°C

335.1±31.5 °C

0.0±1.9 mmHg at 25°C

1.558

4.94

1

4

12

34

585

0

FTLDJPRFCGDUFH-UHFFFAOYSA-N

InChI=1S/C28H41N3O3/c1-27(2,19-23-13-9-7-10-14-23)29(5)25(33)21-31(17-18-32)22-26(34)30(6)28(3,4)20-24-15-11-8-12-16-24/h7-16,32H,17-22H2,1-6H3

2-[2-hydroxyethyl-[2-[methyl-(2-methyl-1-phenylpropan-2-yl)amino]-2-oxoethyl]amino]-N-methyl-N-(2-methyl-1-phenylpropan-2-yl)acetamide

Wy-806; WY 806;Oxethazaine

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ≥ 50 mg/mL (~106.92 mM)

Solubility in Formulation 1: 2.5 mg/mL (5.35 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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.

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Solubility in Formulation 2: ≥ 2.5 mg/mL (5.35 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 25.0 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.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (5.35 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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 (Please use freshly prepared in vivo formulations for optimal results.)