1375. Brimonidine

Nomenclature

CAS number: 59803-98-4
5-Bromo-N-(4,5-dihydro-1H-imidazol-2-yl)-6-quinoxalinamine; 5-bromo-6-(2-imidazolin-2-ylamino)quinoxaline; UK-14304; AGN-190342.
C11H10BrN5; mol wt 292.13.
C 45.23%, H 3.45%, Br 27.35%, N 23.97%.

Description and references

α2-Adrenoceptor agonist. Prepn: J. C. Danielewicz et al., DE 2309160; eidem, US 3890319 (1973, 1975 both to Pfizer). HPLC determn in serum and aqueous humour of the eye: N. K. Karamanos et al., Biomed. Chromatogr. 13, 86 (1999). Clinical study in control of intraocular pressure: R. David et al., Arch. Ophthalmol. 111, 1387 (1993); L. J. Katz et al., Am. J. Ophthalmol. 127, 20 (1999). Review of pharmacology and mechanisms of action: J. C. Adkins, J. A. Balfour, Drugs Aging 12, 225-241 (1998); of pharmacotherapeutic profile: L. B. Cantor, Expert Opin. Pharmacother. 1, 815-834 (2000).

Chemical structure

Properties

Yellow crystals from ethanol, mp 252°.

Derivative

d-Tartrate.

Nomenclature

CAS number: 70359-46-5
UK-14304-18; AGN-190342-LF; Alphagan (Allergan).
C11H10BrN5.C4H6O6; mol wt 442.22.
C 40.74%, H 3.65%, Br 18.07%, N 15.84%, O 21.71%.

Properties

White crystals from acetone, mp 207.5°.

Therapeutic Category

Antiglaucoma.

Keywords

Antiglaucoma