Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1995-06-22
1997-10-14
Fay, Zohreh
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514913, A61K 31415
Patent
active
056773277
ABSTRACT:
The present invention provides a method for identifying a compound having muscarinic agonist activity that will lower intraocular pressure without causing miosis which comprises measuring the activity of the compound at the m.sub.3 and m.sub.5 muscarinic receptors and determining from the activity measurement a compound having at least twice the agonist activity at the m.sub.5 receptor as compared to the m.sub.3 receptor. Preferably, the method of measuring said muscarinic agonist activity comprises eliciting phosphoinositide hydrolysis in CHO-K1 cells stably expressing the m.sub.3 and m.sub.5 muscarinic receptor subtypes. The present invention also provides a method of lowering the intraocular pressure in a mammal which comprises administering to said mammal a compound that has been determined to have at least twice the agonist activity at the m.sub.5 receptor as compared to the m.sub.3 receptor.
REFERENCES:
patent: 5264449 (1993-11-01), Albaugh
Embase Abstract 93042625, (1993). Olianas et al.
Embase Abstract 93039765, (1993). Schwarz et al.
WPIDS 92-096799 (2), (1992). Mitch et al.
Gil Daniel W.
WoldeMussie Elizabeth
Allergan
Baran Robert J.
Fay Zohreh
Lambert Howard R.
Voet Martin A.
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