Нилидрин

Description

Nilidrin (bufenine) is a beta-adrenergic agonist and vasodilator. Structurally, it is an amino alcohol: a 4-hydroxyphenyl fragment with a side chain bearing a secondary amino group substituted by a 1-methyl-3-phenylpropyl residue. Acts primarily on beta-2 adrenergic receptors. Known as Buphenine, Nilidrine, Arlidin, Dilatal; found in the literature as phenyl-sec-butylnorsuprifen and suprifen-psb. Dosage form: hydrochloride.

Basic Attributes

• CAS No: 447-41-6 (additional number 33374-68-4)
• Chemical formula: C19H25NO2
• Molecular Weight: 299.4073
• Exact weight: 299.41
• EU number: 207-182-2
• UNII: 695DKH33EI
• DSSTox ID: DTXSID4023387
• ATC code: C - cardiovascular system; G - genitourinary system and sex hormones
• PSA Specifications: 52.5
• XLogP3: 3.3 (calculation)

Physico-chemical characteristics

• Appearance: White powder
• Color and shape: methanol crystals
• Smell: odorless
• Taste: tasteless
• Density: 1.101 g/cm³
• Melting point: 111-112 °C
• Boiling point: 476 °C at 760 mm Hg. Art.
• Flash point: 127.3 °C
• Refractive index: 1.579
• Solubility in water: 1.1 × 10³ mg/l at 25 °C (calculation)
• Vapor pressure: 4.1 × 10⁻⁹ mm Hg. Art. at 25 °C (calculation)
• Henry's law constant: 1.7 × 10⁻¹⁵ atm m³/mol at 25 °C (calculation)
• pH: from 4.5 to 6.5 (1% solution)

Pharmacological group and mechanism of action

Beta-adrenergic receptor agonist. Excitation of beta-2 receptors of vascular smooth muscles dilates the arterioles of skeletal muscles, blood flow increases, and peripheral resistance decreases. At the same time, a positive inotropic effect appears: in experiments on anesthetized dogs and cats and in humans without anesthesia, nilidrine increased cardiac output. An increase in the volume of gastric juice was also noted. Nylidrine hydrochloride inhibits the release of histamine from mast cells through a non-adrenergic mechanism that is not associated with an increase in cAMP levels.

Scope of application

• peripheral vascular diseases: the drug Arlidin increased walking distance and accelerated the healing of trophic ulcers
• threat of premature birth - tocolytic effect through beta-2 receptors of the uterus, which is reflected in the ATC code of group G
• reference substance in pharmacological and analytical studies

Regulatory status: The FDA recognized nilidrine as having insufficient evidence of effectiveness in cerebral ischemia, cerebral atherosclerosis and other cerebrovascular insufficiency and withdrew the drug from the US market.

Storage and transportation conditions

Store below 40°C (104°F), preferably between 15 and 30°C (59 and 86°F), unless otherwise indicated by the manufacturer. The container is sealed. The volatility of the substance is negligible - the vapor pressure is about 10⁻⁹ mm Hg. Art., Henry's constant is 10⁻¹⁵ atm m³/mol, therefore evaporation during storage and transportation is not considered a risk factor.