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. After oral admin of the drug, peak plasma concns occur within 1 hr and persist for about 3 hr. ...Isoxsurprine crosses the placenta. The drug is partially conjugated in the body and is excreted in the urine. Fecal excretion of the drug is negligible.

---

Biological Half-Life
Mean plasma half-life of the drug is 1.25 hr.

Interactions
Concurrent heavy use /of tobacco smoking/ may interfere with the therapeutic effects of isoxsuprine because nicotine constricts blood vessels.

---

Non-Human Toxicity Values
LD50 Rat oral 1750 mg/kg
LD50 Rat intraperitoneal 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.
Isoxsuprine Hydrochloride is the hydrochloride salt of isoxsuprine, a benzyl alcohol derivative with vasodilator activity. The mechanism of action of isoxsuprine hydrochloride is controversial because this drug has beta-adrenergic agonist activities that are not reversed by beta-adrenergic blockers. Although stimulation of the beta adrenergic receptor increases blood flow to produce vasodilatation, this drug may also have direct effects on the contractility of smooth muscle. Isoxsuprine hydrochloride also causes relaxation of uterine smooth muscle and may also produce positive inotropic and chronotropic effects on the myocardium.
A beta-adrenergic agonist that causes direct relaxation of uterine and vascular smooth muscle. Its vasodilating actions are greater on the arteries supplying skeletal muscle than on those supplying skin. It is used in the treatment of peripheral vascular disease and in premature labor.
See also: Isoxsuprine (has active moiety).

---

Mechanism of Action
Isoxsuprine produces peripheral vasodilation by a direct effect on vascular smooth muscle, primarily within skeletal muscle with little effect on cutaneous blood flow. Its effects were once thought to be due to beta-adrenergic receptor stimulation but are not reversed by beta-adrenergic blocking agents.

---

Therapeutic Uses
Adrenergic beta-Agonists; Sympathomimetics; Tocolytic Agents; Vasodilator Agents
Isoxsuprine is also used for management of threatened premature labor in pregnancies of 20 or more weeks' gestation. Use in not recommended prior to the 20th week of pregnancy. For isoxsuprine to be most effective, it is recommended that therapy be started as soon as the diagnosis of preterm labor is confirmed. Efficacy in advanced labor has not been established. Use in patients with ruptured membranes must be weighed against the risk of intrauterine infection. /NOT included in US product labeling/
Isoxsuprine has been used in the treatment of dysmenorrhea. /NOT included in US product labeling/
FDA has classified isoxsuprine as being possibly effective for its labeled indications, which include relief of symptoms associated with cerebrovascular insufficiency and peripheral vascular disease, ie, arteriosclerosis obliterans, thromboangiitis obliterans (Buerger's disease), and Raynaud's disease. This classification requires the submission of adequate and well-controlled studies in order to provide substantial evidence of effectiveness. /Included in US product labeling/
For more Therapeutic Uses (Complete) data for ISOXSUPRINE HYDROCHLORIDE (7 total), please visit the HSDB record page.

---

Drug Warnings
Except under special circumstances, this medication /isoxsuprine hydrochloride/ should not be used immediately postpartum or when the following medical problems exist: For use in management of premature labor only: Cardiac disorders, especially those associated with arrhythmias, or maternal hyperthyroidism (isoxsuprine may precipitate arrhythmias or heart failure; occult cardiac disease may be unmasked) or chorioamnionitis (intrauterine infection) or hemorrhage or intrauterine fetal death or known abnormality (immediate delivery required) or eclampsia (toxemia) and severe pre-eclampsia or pulmonary hypertension.
Isoxsuprine has both beta-1 and beta-2 adrenergic activity. Maternal hypotension and tachycardia are common side effects. Hypocalcemia, hypoglycemia, hypotension, ileus, and neonatal death are increased after isoxsuprine administration.
...When injected sc in human beings causes several mm of mercury transient elevation of ocular pressure, max in an hr or two, associated with edema and hyperemia of episcleral tissues.
Adverse effects of isoxsuprine include trembling, nervousness, weakness, dizziness, flushing, transient palpitation, tachycardia, chest pain, hypotension, abdominal distress, nausea, vomiting, intestinal distention, and severe rash.
For more Drug Warnings (Complete) data for ISOXSUPRINE HYDROCHLORIDE (8 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.)