mAChr

MAJOR ACTION OF ANTIMUSCARINIC AGENTS IS COMPETITIVE ANTAGONISM OF ACTIONS OF ACETYLCHOLINE & OTHER MUSCARINIC AGONISTS.

Antidote and Emergency Treatment
/SRP:/ Immediate First Aid: Ensure adequate decontamination has been performed. If the patient stops breathing, begin artificial respiration immediately, preferably using a demand ventilator, bag-valve-mask, or simple breathing mask (if trained). Perform cardiopulmonary resuscitation if necessary. Immediately flush contaminated eyes with running water. Do not induce vomiting. If vomiting occurs, tilt the patient forward or place them in the left lateral decubitus position (head down if possible) to maintain an open airway and prevent aspiration. Keep the patient calm and maintain normal body temperature. Seek medical attention. /Class A and Class B Poisoning/
/SRP:/ Basic Treatment: Establish an open airway (using an oropharyngeal or nasopharyngeal airway if necessary). Suction if necessary. Observe for signs of respiratory failure and provide assisted ventilation if necessary. Administer oxygen using a non-invasive breathing mask at a flow rate of 10 to 15 liters per minute. Monitor for pulmonary edema and treat as necessary… Monitor for shock and treat as necessary… Anticipate seizures and treat as necessary… If eyes become contaminated, rinse immediately with water. During transport, continuously rinse each eye with 0.9% normal saline (NS)... Do not use emetics. If swallowed, rinse mouth; if the patient is able to swallow, has a strong gag reflex, and does not drool, administer 5 mL/kg to 200 mL of water to dilute... After cleansing, cover skin burns with a dry, sterile dressing... /Class A and B Poisons/
/SRP:/ Advanced Treatment: For patients with altered mental status, severe pulmonary edema, or severe respiratory distress, consider oropharyngeal or nasopharyngeal endotracheal intubation to control the airway. Positive pressure ventilation using a bag-valve-mask may be effective. Consider medical treatment for pulmonary edema... For severe bronchospasm, consider the use of β-receptor agonists, such as salbutamol... Monitor heart rhythm and treat arrhythmias if necessary... Initiate intravenous infusion of 5% glucose solution (D5W) /SRP: "Maintain patency", minimum flow rate/. If signs of hypovolemia appear, administer 0.9% normal saline (NS) or lactated Ringer's solution. For hypotension accompanied by signs of hypovolemia, administer fluids with caution. Be aware of signs of fluid overdose… Treat seizures with diazepam or lorazepam… Use promecaine hydrochloride as an adjunct to eye irrigation… /Toxins A and B/

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Excerpt of Human Toxicity
/Signs and Symptoms/ Approximately 10–36 tablets of sominex, equivalent to 2.5–9 mg of scopolamine hydrobromide, were ingested. The reaction was very similar to atropine poisoning, presenting with disorientation, mydriasis, and blurred vision, presumably due to cycloplegia. No permanent ocular damage occurred. Grant, WM, Ocular Toxicology, 2nd ed., Springfield, Illinois: Charles C. Thomas Press, 1974, p. 902.

Mechanism of Action
The main action of antimuscarinic drugs is to competitively antagonize the effects of acetylcholine and other muscarinic agonists. /Antimuscarinic Drugs/

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Therapeutic Uses Anticholinergic drugs
Over-the-counter sleeping pills (previously used)

C₁₇H₂₂BRNO₅

400.26

319.141

6106-81-6

6419978

Prisms from water

137ºC

-0.49

2

5

5

24

460

5

C[N+]1([C@@H]2CC(C[C@H]1[C@H]3[C@@H]2O3)OC(=O)[C@H](CO)C4=CC=CC=C4)[O-].Br

MGNNYKWRWHQLCR-RDYQINQZSA-N

InChI=1S/C17H21NO5.BrH/c1-18(21)13-7-11(8-14(18)16-15(13)23-16)22-17(20)12(9-19)10-5-3-2-4-6-10;/h2-6,11-16,19H,7-9H2,1H3;1H/t11?,12-,13-,14+,15-,16+,18?;/m1./s1

[(1S,2S,4R,5R)-9-methyl-9-oxido-3-oxa-9-azoniatricyclo[3.3.1.02,4]nonan-7-yl] (2S)-3-hydroxy-2-phenylpropanoate;hydrobromide

Hyoscine N-oxide hydrobromide; Hyoscine N-oxide hydrobromide; Genoscopolamine HydrobroMide Monohydrate; Scopolamine N-Oxide HydrobroMide Monohydrate; Scopolamine N-oxide hydrobromide; Hyoscine N-oxide HydrobroMide Monohydrate; Scopolamine aminoxide hydrobromide; Hyoscine N-oxide hydrobomide; HSDB 6105; AMINOXYSCOPOLAMINE HYDROBROMIDE; EINECS 228-066-8; NSC 61807; SCOPOLAMINE, N-OXIDE,HYDROBROMIDE; ...; 6106-81-6;

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)

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

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.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*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).

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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)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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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).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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