Absorption, Distribution and Excretion
Easily absorbed from the gastrointestinal tract. Duration of action: 2 hours. Time to peak effect: 30 minutes. Onset of action: 10 minutes. Easily absorbed from the gastrointestinal tract. Biological half-life: Duration of action is 10 hours.

Interactions
Nilidene amines can enhance the effects of phenothiazines by displacing them from receptor sites and tissues, as well as through its cerebral vasodilatory effects. Although clinical literature is lacking, concomitant use of nilidene amines may enhance the activity of phenothiazines. Pretreatment of rats with nilidene amines protects them from acute sodium cyanide poisoning.

[1]. The cerebral peripheral circulatory action of nylidrin hydrochloride

Therapeutic Uses
MeSH Title: Adrenaline Beta Agonist, Sympathomimetic Drug, Tocolytic, Vasodilator
Nylidrin is only considered "possibly" effective for its labeled indications, including peripheral vascular spasmolytic diseases such as occlusive arteriosclerosis; thromboangiitis obliterans; diabetic vascular disease; nocturnal leg cramps; Raynaud's phenomenon and Raynaud's disease; frostbite; acrocyanosis; acrosensory disorders; thrombophlebitis; and cold hands and feet.
The FDA has listed nilideline as a drug with "lack of substantial evidence of efficacy" for the treatment of cerebral ischemia, cerebral arteriosclerosis, and other cerebral circulatory insufficiency. Therefore, the FDA has withdrawn nilideline from the U.S. market.
.../IT/ Used to treat limb vascular diseases that may involve skeletal muscle vessels, such as intermittent claudication, thrombophlebitis, and to a lesser extent, diabetic vascular disease. ...This product is only effective when vasospasm is present in these conditions...
For more complete data on the therapeutic uses of nylidrin (11 items), please visit the HSDB record page.
Drug Warnings
...This product should not be used in patients with angina or recent/past myocardial infarction.
Heavy smoking may interfere with the therapeutic effect of nylidrin because nicotine constricts blood vessels.
Studies on the relationship between age and the efficacy of nylidrin have not been conducted in elderly populations. However, the risk of hypothermia induced by nylidrin may be increased in elderly patients.
Caution should be exercised in patients with cardiomyopathy, thyrotoxicosis, or severe angina.
For more complete data on drug warnings (6 items) for nylidrin, please visit the HSDB record page.
Pharmacodynamics
...Nilidrin hydrochloride primarily works by stimulating β-receptors. The β-receptor stimulating effect of nelidene has been studied and confirmed in various isolated tissues of rabbits, guinea pigs, and dogs. This drug has been shown to dilate skeletal muscle arterioles and increase cardiac output in anesthetized dogs, cats, and unanesthetized humans. It has also been reported to increase cerebral blood flow and reduce vascular resistance. The combined effect of these mechanisms is to improve blood supply to ischemic tissues with minimal changes in blood pressure (normally). Nelidene causes peripheral vasodilation, positive inotropic effects, and increased gastric acid secretion. One study showed that intra-arterial administration of this drug has two main effects: firstly, reducing total peripheral resistance; and secondly, acting directly on myocardial tissue to increase cardiac output. It can also act directly on arteries and arterioles of skeletal muscle. Furthermore, it can inhibit uterine contractions, thereby preventing or stopping preterm labor.

C19H25NO2

299.414

299.189

447-41-6

849-55-8 (hydrochloride)

4567

Crystals from methanol

1.101 g/cm3

476ºC at 760 mmHg

111-112°

127.3ºC

7.23E-10mmHg at 25°C

1.579

3.815

3

3

7

22

296

0

OC1C=CC(C(C(NC(CCC2C=CC=CC=2)C)C)O)=CC=1

PTGXAUBQBSGPKF-UHFFFAOYSA-N

InChI=1S/C19H25NO2/c1-14(8-9-16-6-4-3-5-7-16)20-15(2)19(22)17-10-12-18(21)13-11-17/h3-7,10-15,19-22H,8-9H2,1-2H3

4-[1-hydroxy-2-(4-phenylbutan-2-ylamino)propyl]phenol

Buphenine; Nylidrin

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.)