Rats' systemic circulation is more affected by methylamine hydrochloride (0.025 mg/kg; femoral vein) on peripheral resistance vessels than Winkessel vessels [2].

Animal/Disease Models: Male Wistar-Kyoto rat, body weight 320-47 g (based on exponential tapered T-tube model) [2]
Doses: 0.025 mg/kg
Route of Administration: Femoral vein
Experimental Results: The effect on peripheral resistance vessels is greater than that on peripheral blood vessels Effects of resistance vessels on the Winksel vessels in the rat systemic circulation.

Interactions
Methoxamineine may cause arrhythmias when used in combination with general anesthetics. /Methoxamineine/
Methoxamineine hydrochloride was previously used as a 2% eye drop in patients with thyrotoxicosis, and it was found to cause mydriasis and widening of the palpebral fissure. Guanethidine can enhance this effect.
When vagal nerve action is blocked by atropine, Methoxamineine hydrochloride usually slightly slows the heart rate. This may be due to its direct action on alpha receptors. Injecting the drug into the artery leading to the sinoatrial node slows the heart rate, while phentolamine blocks this effect.
Concomitant use of alpha-adrenergic blockers (e.g., doxazosin, labetalol, phenoxybenzamine, phentolamine, prazosin, terazosin, tolazoline) or other drugs with alpha-adrenergic blocking effects (e.g., haloperidol, loxapine, phenothiazines, thioxanthates) may antagonize the peripheral vasoconstrictive effects of sympathomimetic drugs; however, phentolamine can still be used for treatment. /Sympathomimetic Drugs/
For more complete data on interactions of methoxyamine hydrochloride (17 drugs in total), please visit the HSDB record page.

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Non-human toxicity values
Intraperitoneal LD50 in mice: 92 mg/kg
Intravenous LD50 in mice: 5030 μg/kg

[1]. Sanders AB. The roles of methoxamine and norepinephrine in electromechanical dissociation. Ann Emerg Med. 1984;13(9 Pt 2):835-839.

[2]. Chang KC. Hypertensive effects of methoxamine on arterial mechanics in rats: analysis based on exponentially tapered T-tube model. Eur J Pharmacol. 1998;350(2-3):195-202.

[3]. Methoxamine-induced release of endogenous ATP from rabbit pulmonary artery. Eur J Pharmacol. 1994;254(3):287-290.

Methoxamine hydrochloride is a dimethoxybenzene compound. It is an α1-adrenergic agonist that induces sustained peripheral vasoconstriction. Mechanism of Action: Because it acts directly on α-receptors, its pharmacological properties are almost entirely characteristic of α-receptor stimulation. …Its most significant effect is increased blood pressure, which is entirely due to vasoconstriction. Intravenous or intramuscular injection of Methoxamine increases systolic and diastolic blood pressure, lasting for 60 to 90 minutes. The pressor effect is almost entirely due to increased peripheral resistance. Cardiac output decreases or remains unchanged. Methoxamine has a relatively higher selectivity for postsynaptic receptors in the pulmonary artery than for presynaptic receptors; both systems have similar sensitivities to norepinephrine and epinephrine. Tritium-labeled Methoxamine can cross the blood-brain barrier in rats. Therefore, Methoxamine is a centrally active α-adrenergic agonist, supporting the view that hypothalamic adrenergic mechanisms are involved in electroencephalography and behavioral arousal.

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Therapeutic Uses
Alpha-adrenergic agonist; sympathomimetic; vasoconstrictor
Methoxamineine can be administered intravenously to treat hypotension or relieve paroxysmal atrial tachycardia, especially when accompanied by hypotension. /Methoxamineine/
Methoxamineine…does not increase ventricular rate in patients with cardiac conduction block. Reflex bradycardia is common; therefore, this drug is used clinically to relieve paroxysmal atrial tachycardia. /Methoxamineine/
This drug can be used to treat hypotension when it is necessary to raise blood pressure without stimulating the heart. However, Methoxamineine has little effect on venous volume, thus its efficacy is limited, especially in the treatment of various types of shock.
For more complete data on the therapeutic uses of Methoxamineine hydrochloride (9 types), please visit the HSDB record page.

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Drug Warnings
Methoxamineine should be used with caution in patients with hyperthyroidism, bradycardia, partial atrioventricular block, myocardial disease, or severe arteriosclerosis. Caution should be exercised to avoid Methoxamineine overdose, as it may cause adverse hypertension and/or bradycardia. Methoxamineine can cause premature ventricular contractions or severe bradycardia and a decrease in cardiac output. Decreased cardiac output may be particularly harmful in elderly patients and/or those with a history of poor cerebral or coronary circulation. Bradycardia can be treated with atropine. Methoxamineine also increases cardiac workload by increasing peripheral arterial resistance and may induce or worsen heart failure associated with impaired myocardial function. Some clinicians consider this drug contraindicated in shock caused by myocardial infarction. High doses of Methoxamineine, especially after repeated injections, may lead to cardiac depression and hypotension. Methoxamineine can cause severe peripheral and visceral vasoconstriction, reducing blood flow to vital organs and decreasing renal perfusion; it may also cause decreased glomerular filtration rate, urine output, and sodium excretion, as well as metabolic acidosis. These effects are most likely to occur in patients with hypovolemia. In addition, prolonged use of this drug may lead to a decrease in plasma volume, resulting in a persistent state of shock, or a recurrence of hypotension after discontinuation of Methoxamineine. Methoxamineine may cause agitation, anxiety, nervousness, weakness, dizziness, precordial pain, tremor, dyspnea, sweating, or pallor. Sometimes, paresthesia or chills may occur in the extremities after injection. Urination urges, piloerection, and/or nausea and vomiting (usually projectile vomiting) may also occur, especially at high doses. Furthermore, high doses of Methoxamineine can cause severe, persistent hypertension and severe headache. It may also cause seizures and cerebral hemorrhage. For more complete data on drug warnings for Methoxamineine hydrochloride (8 in total), please visit the HSDB record page.

C11H17NO3.HCL

247.72

247.098

61-16-5

Methoxamine;390-28-3

6081

White to off-white solid powder

368.4ºC at 760 mmHg

212-216ºC

176.6ºC

1.5204

2.586

3

4

4

16

189

0

YGRFXPCHZBRUKP-UHFFFAOYSA-N

InChI=1S/C11H17NO3.ClH/c1-7(12)11(13)9-6-8(14-2)4-5-10(9)15-3;/h4-7,11,13H,12H2,1-3H3;1H

2-amino-1-(2,5-dimethoxyphenyl)propan-1-ol;hydrochloride

2934.99.9001

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.

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

DMSO : ~135 mg/mL (~544.97 mM)

Solubility in Formulation 1: ≥ 2 mg/mL (8.07 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 20.0 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 mg/mL (8.07 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 20.0 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.)