Reference

Ophthalmic compositions containing R stereoisomeric b-adrenergic blocking agents for treating elevated intraocular pressure

Ophthalmic compositions containing R stereoisomeric b-adrenergic blocking agents for treating elevated intraocular pressure. Lotti, Victor J. (Merck and Co., Inc. , USA). Eur. Pat. Appl. EP 105996 A1 25 Apr 1984, 26 pp. DESIGNATED STATES: R: AT, BE, CH, DE, FR, GB, IT, LI, LU, NL, SE. (English). (European Patent Organization). CODEN: EPXXDW. CLASS: IC: A61K031-13; A61K031-41. APPLICATION: EP 82-401896 15 Oct 1982. DOCUMENT TYPE: Patent CA Section: 63 (Pharmaceuticals) Section cross-reference(s): 28 Topical compns. contg. R or R-enriched isomers of b-adrenergic blocking agents are effective in treating elevated intraocular pressure. (RS)-1-tert-Butylamino-2,3-dihydroxypropane (RS-I) [61915-26-2] was resolved with R-pyroglutamic acid and the resulting R-(+)-I [59207-70-4] treated with benzaldehyde [100-52-7] to give R-2-phenyl-3-tert-butyl-5-hydroxymethyloxazoline [91021-59-9]. This was treated with 3-morpholino-4-chloro-1,2,5-thiadiazole [30165-96-9] in the presence of KOCMe3 in tert-BuOH to give R-(+)-II [26839-76-9]. A no. of compns., e.g., solns., ointments, and ophthalmic inserts were prepd.Except for chemicals metioned above, 92007-66-4 is also used. contg. R-(+)-II hydrogen maleate [26839-77-0]. .

Are b-adrenergic mechanisms involved in ocular hypotensive actions of adrenergic drugs?

Are b-adrenergic mechanisms involved in ocular hypotensive actions of adrenergic drugs?. Chiou, George C. Y.; Watanabe, Kazuhito; McLaughlin, Marsha A.; Liu, Hsin K. (Coll. Med., Texas A and M Univ., College Station, TX 77843, USA). Ophthalmic Res., 17(1), 49-53 (English) 1985. CODEN: OPRSAQ. ISSN: 0030-3747. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Section cross-reference(s): 2 In cats, tazolol (I) [39832-48-9] (b1-agonist) reduced the formation of aq. humor more than the outflow, whereas metoprolol [37350-58-6] (b1-antagonist) reduced the outflow of aq. humor more than its formation. Both salbutamol [18559-94-9] (b2-agonist) and butoxamine [1937-89-9] (b2-antagonist) inhibited aq. humor formation and aq. humor outflow to an equal extent. Receptor binding expts. on the iris-ciliary body prepns. from rabbits clearly showed that there are 40-fold and 281-fold differences in binding affinity of d- [26839-77-0] and l-timolol maleate [26921-17-5] and d- [5051-22-9] and l-propranolol [4199-09-1], resp. Thus, adrenergic receptor mechanisms exist in the eye tissues, but do not control intraocular pressure significantly.