7430. Pimefylline

Nomenclature

CAS number: 10001-43-1
3,7-Dihydro-1,3-dimethyl-7-[2-[(3-pyridinylmethyl)amino]ethyl]-1H-purine-2,6-dione; 7-[2-[(3-pyridylmethyl)amino]ethyl]theophylline; 7-(β-3′-picolylaminoethyl)theophylline; pimephylline; ES-771.
C15H18N6O2; mol wt 314.34.
C 57.31%, H 5.77%, N 26.74%, O 10.18%.

Description and references

Prepn: NL 6600250; Suter, Zutter, US 3350400 (1966, 1967 both to Eprova). Structure determn, properties and chemistry: eidem, Pharm. Acta Helv. 48, 133 (1973). Pharmacology: Ciaceri, Attaguile, Gazz. Med. Ital. 132, 36, 108 (1973). Metabolism: Pitrè, Farmaco Ed. Prat. 29, 46 (1974).

Chemical structure

Properties

Crystals from isopropyl acetate, mp 111-112°. uv max (water): 270 nm. Readily sol in cold water, chloroform; sol in acetone, ethanol. LD50 in mice (mg/kg): 1900 orally, 402 i.v. (Suter, Zutter, 1973).

Derivative

Nicotinate.

Nomenclature

CAS number: 10058-07-8
ES-902; Teonicon (Neopharmed).
C15H18N6O2.C6H5NO2; mol wt 437.45.
C 57.66%, H 5.30%, N 22.41%, O 14.63%.

Properties

Colorless, odorless powder from ethanol, mp 159-160°. uv max (water): 267 nm. Very sol in water (40% soln can be prepd); slightly sol in methanol; very slightly sol in acetone, chloroform. LD50 in mice (mg/kg): 2530 orally, 470 i.v. (Suter, Zutter, 1973).

Therapeutic Category

Vasodilator (coronary).

Keywords

Vasodilator (Coronary)