The findings indicate that isoxsuprine salticide inhibits 12(S)-HETE synthesis as well as the generation of cyclic chemorepellent-induced defects (CCID) in a dose-dependent manner (5 to 60 μM). Moreover, only isoxosulin hydrochloride suppresses the induction of MYPT, paxillin, and MLC2, the other two migratory indicators [2].

The animals treated with vehicle had a total infarct volume of 279 ± 25 mm3, whereas the animals treated with isoxosulfonate had a total infarct volume of 137 ± 18 mm3 [3].

Absorption, Distribution and Excretion
Isoxsuprine hydrochloride is almost completely absorbed from the gastrointestinal tract. Peak plasma concentrations occur within 1 hour after oral administration and persist for approximately 3 hours. …Isoxsuprine can cross the placenta. The drug partially binds in the body and is excreted in the urine. Fecal excretion is negligible. Biological Half-Life The mean plasma half-life of this drug is 1.25 hours.

Interactions
Simultaneous heavy smoking may interfere with the therapeutic effect of isosuprine because nicotine constricts blood vessels. Non-human Toxicity Values Oral LD50 in rats: 1750 mg/kg Intraperitoneal LD50 in rats: 164 mg/kg

[1]. Affinity of tocolytic agents on human placental and myometrial beta-adrenergic receptors. J Perinat Med. 1986;14(2):109-13.

[2]. In vitro inhibition of breast cancer spheroid-induced lymphendothelial defects resembling intravasation into the lymphatic vasculature by acetohexamide, isoxsuprine, nifedipin and proadifen. Br J Cancer. 2013 Feb 19;108(3):570-8.

[3]. Identification of isoxsuprine hydrochloride as a neuroprotectant in ischemic stroke through cell-based high-throughput screening. PLoS One. 2014 May 7;9(5):e96761.

Isoxsuprine hydrochloride is an alkylbenzene compound. Isoxsuprine hydrochloride is the hydrochloride salt of Isoxsuprine, a benzyl alcohol derivative with vasodilatory activity. The mechanism of action of Isoxsuprine hydrochloride is controversial because it has β-adrenergic agonist activity that cannot be reversed by β-adrenergic blockers. Although stimulation of β-adrenergic receptors increases blood flow, thus producing a vasodilatory effect, the drug may also directly affect the contractility of smooth muscle. Isoxsuprine hydrochloride can also relax uterine smooth muscle and may have positive inotropic and chronotropic effects on the myocardium. It is a β-adrenergic agonist that directly relaxes uterine and vascular smooth muscle. Its vasodilatory effect on arteries supplying skeletal muscle is stronger than that on arteries supplying the skin. It is used to treat peripheral vascular disease and preterm birth. See also: Isoxsuprine (containing the active ingredient).

---

Mechanism of Action
Isosuprine acts directly on vascular smooth muscle (primarily skeletal muscle) to produce peripheral vasodilation, with minimal effect on skin blood flow. Its action was once thought to be due to stimulation of β-adrenergic receptors, but this effect cannot be reversed by β-adrenergic blockers.

---

Therapeutic Uses
β-adrenergic agonist; sympathomimetic; tocolytic; vasodilator
Isosuprine is also used to treat threatened preterm labor in women at 20 weeks of gestation and beyond. Use before 20 weeks of gestation is not recommended. For optimal efficacy, treatment is recommended to begin immediately after diagnosis of preterm labor. Its efficacy in late labor has not been established. For patients with premature rupture of membranes, the risk of intrauterine infection must be weighed. /Not included on US product label/
Isosuprine has been used to treat dysmenorrhea. /Not Included on US Product Labels/
The US Food and Drug Administration (FDA) has classified Isoxsuprine as potentially effective for its labeled indications, including the relief of symptoms associated with cerebrovascular insufficiency and peripheral vascular disease, such as occlusive arteriosclerosis, thromboangiitis obliterans (Burgh's disease), and Raynaud's disease. This classification requires the submission of adequate and well-controlled studies to provide strong evidence of efficacy. /Included on US Product Labels/
For more complete data on the therapeutic uses of Isoxsuprine hydrochloride (7 types), please visit the HSDB record page.

---

Drug Warning
Except in special circumstances, this drug (Isoxsuprine hydrochloride) should not be used immediately postpartum or in the presence of the following medical problems: for the management of preterm labor only: heart disease, especially heart disease with arrhythmias, or hyperthyroidism in pregnant women (Isoxsuprine may induce arrhythmias or heart failure; may induce occult heart disease), or chorioamnionitis (intrauterine infection), or hemorrhage, or intrauterine fetal death, or known abnormalities (requiring immediate delivery), or eclampsia (preeclampsia) and severe preeclampsia or pulmonary hypertension.
Isoxsuprine is a β1 and β2 receptor agonist. Adrenergic activity. Common side effects include hypotension and tachycardia in pregnant women. The risk of hypocalcemia, hypoglycemia, hypotension, intestinal obstruction, and neonatal death is increased after administration of Isoxsuprine.
...After subcutaneous injection, it causes a transient increase in intraocular pressure of several millimeters of mercury, reaching its peak within one to two hours, accompanied by scleral edema and congestion.
Adverse reactions of Isoxsuprine include tremor, nervousness, weakness, dizziness, flushing, transient palpitations, tachycardia, chest pain, hypotension, abdominal discomfort, nausea, vomiting, flatulence, and severe rash.
For more complete data on drug warnings for Isoxsuprine hydrochloride (8 in total), please visit the HSDB record page.

C18H23NO3.HCL

337.84

337.144

579-56-6

Isoxsuprine-d6 hydrochloride;2706004-35-3

11368

White to off-white solid powder

1.146g/cm3

484.2ºC at 760mmHg

203-204°

246.6ºC

4.064

4

4

7

23

299

0

QVPSGVSNYPRFAS-UHFFFAOYSA-N

InChI=1S/C18H23NO3.ClH/c1-13(12-22-17-6-4-3-5-7-17)19-14(2)18(21)15-8-10-16(20)11-9-15;/h3-11,13-14,18-21H,12H2,1-2H3;1H

4-[1-hydroxy-2-(1-phenoxypropan-2-ylamino)propyl]phenol;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 : ~140 mg/mL (~414.40 mM)
H2O : ~15.56 mg/mL (~46.06 mM)

Solubility in Formulation 1: ≥ 3.5 mg/mL (10.36 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 35.0 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.

---

Solubility in Formulation 2: ≥ 3.5 mg/mL (10.36 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 35.0 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.

---

View More

Solubility in Formulation 3: ≥ 3.5 mg/mL (10.36 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 35.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

---

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