Comparative effects of SCH 19927 and timolol on intraocular pressure of conscious rabbits and relative systemic beta-blockade resulting from topical administration. 1985

R W Watkins, and D P Cummins, and G Vander Vliet, and J Glennon, and T Baum
Department of Pharmacology, Schering-Plough Research Division, Bloomfield, New Jersey.

SCH 19927, the RR isomer of labetalol, has been shown to possess beta-blocking and vasodilator properties. It was compared to timolol for ability to lower intraocular pressure (IOP) in conscious rabbits. Its potential for systemic beta-blockade after topical administration was also assessed. Dose-related reductions in IOP followed topically applied SCH 19927 (0.1-1.0%). Timolol in concentrations less than 0.5% was not effective in lowering IOP. Timolol (0.1 and 0.5%) strongly inhibited tachycardia induced by iv isoproterenol. A 1.0% concentration of SCH 19927 was less effective than 0.5% timolol in inhibiting the isoproterenol-induced tachycardia; 0.1% SCH 19927 caused only minor inhibitory actions. Thus, not only is SCH 19927 at least as potent in lowering IOP in conscious rabbits, its topical administration results in less systemic beta-blockade than does timolol.

UI MeSH Term Description Entries
D007741 Labetalol A salicylamide derivative that is a non-cardioselective blocker of BETA-ADRENERGIC RECEPTORS and ALPHA-1 ADRENERGIC RECEPTORS. AH-5158,Albetol,Apo-Labetalol,Dilevalol,Labetalol Hydrochloride,Labetalol, (R,R)-Isomer,Labetolol,Normodyne,Presolol,R,R-Labetalol,SCH-19927,Trandate,AH 5158,AH5158,Apo Labetalol,ApoLabetalol,Hydrochloride, Labetalol,R,R Labetalol,SCH 19927,SCH19927
D009883 Ophthalmic Solutions Sterile solutions that are intended for instillation into the eye. It does not include solutions for cleaning eyeglasses or CONTACT LENS SOLUTIONS. Eye Drop,Eyedrop,Eyedrops,Ophthalmic Solution,Eye Drops,Drop, Eye,Drops, Eye,Solution, Ophthalmic,Solutions, Ophthalmic
D011817 Rabbits A burrowing plant-eating mammal with hind limbs that are longer than its fore limbs. It belongs to the family Leporidae of the order Lagomorpha, and in contrast to hares, possesses 22 instead of 24 pairs of chromosomes. Belgian Hare,New Zealand Rabbit,New Zealand Rabbits,New Zealand White Rabbit,Rabbit,Rabbit, Domestic,Chinchilla Rabbits,NZW Rabbits,New Zealand White Rabbits,Oryctolagus cuniculus,Chinchilla Rabbit,Domestic Rabbit,Domestic Rabbits,Hare, Belgian,NZW Rabbit,Rabbit, Chinchilla,Rabbit, NZW,Rabbit, New Zealand,Rabbits, Chinchilla,Rabbits, Domestic,Rabbits, NZW,Rabbits, New Zealand,Zealand Rabbit, New,Zealand Rabbits, New,cuniculus, Oryctolagus
D011943 Receptors, Adrenergic, beta One of two major pharmacologically defined classes of adrenergic receptors. The beta adrenergic receptors play an important role in regulating CARDIAC MUSCLE contraction, SMOOTH MUSCLE relaxation, and GLYCOGENOLYSIS. Adrenergic beta-Receptor,Adrenergic beta-Receptors,Receptors, beta-Adrenergic,beta Adrenergic Receptor,beta-Adrenergic Receptor,beta-Adrenergic Receptors,Receptor, Adrenergic, beta,Adrenergic Receptor, beta,Adrenergic beta Receptor,Adrenergic beta Receptors,Receptor, beta Adrenergic,Receptor, beta-Adrenergic,Receptors, beta Adrenergic,beta Adrenergic Receptors,beta-Receptor, Adrenergic,beta-Receptors, Adrenergic
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D013999 Timolol A beta-adrenergic antagonist that is similar in action to PROPRANOLOL; the levo-isomer is more active. Timolol has been proposed as an anti-hypertensive, anti-arrhythmic, anti-angina, and anti-glaucoma agent. It is also used in the treatment of MIGRAINE DISORDERS and tremor. (S)-1-((1,1-Dimethylethyl)amino)-3-((4-(4-morpholinyl)-1,2,5-thiadazol-3-yl)oxy)-2-propanol,2-Propanol, 1-((1,1-dimethylethyl)amino)-3-((4-(4-morpholinyl)-1,2,5-thiadiazol-3-yl)oxy)-, (S)-,Blocadren,L-714,465,MK-950,Optimol,Timacar,Timolol Hemihydrate,Timolol Maleate,Timolol Maleate, (1:1) Salt,Timoptic,Timoptol,L 714,465,L714,465,MK 950,MK950

Related Publications

R W Watkins, and D P Cummins, and G Vander Vliet, and J Glennon, and T Baum
February 1982, Acta ophthalmologica,
R W Watkins, and D P Cummins, and G Vander Vliet, and J Glennon, and T Baum
July 1996, Naunyn-Schmiedeberg's archives of pharmacology,
R W Watkins, and D P Cummins, and G Vander Vliet, and J Glennon, and T Baum
May 1991, Methods and findings in experimental and clinical pharmacology,
R W Watkins, and D P Cummins, and G Vander Vliet, and J Glennon, and T Baum
March 1991, American journal of veterinary research,
R W Watkins, and D P Cummins, and G Vander Vliet, and J Glennon, and T Baum
March 1991, American journal of veterinary research,
R W Watkins, and D P Cummins, and G Vander Vliet, and J Glennon, and T Baum
January 1988, Journal of ocular pharmacology,
R W Watkins, and D P Cummins, and G Vander Vliet, and J Glennon, and T Baum
March 1993, General pharmacology,
R W Watkins, and D P Cummins, and G Vander Vliet, and J Glennon, and T Baum
January 1993, Journal of ocular pharmacology,
R W Watkins, and D P Cummins, and G Vander Vliet, and J Glennon, and T Baum
October 1980, Acta ophthalmologica,
R W Watkins, and D P Cummins, and G Vander Vliet, and J Glennon, and T Baum
June 1991, Archives of ophthalmology (Chicago, Ill. : 1960),
Copied contents to your clipboard!