141068-94-2Relevant articles and documents
Synthesis and evaluation of 2-[(5-methylbenz-1-ox-4-azin-6- yl)imino]imidazoline, a potent, peripherally acting α2 adrenoceptor agonist
Munk, Stephen A.,Harcourt, Dale,Ambrus, Gy?rgy,Denys, Lydia,Gluchowski, Charles,Burke, James A.,Kharlamb, Alexander B.,Manlapaz, Cynthia A.,Padillo, Edwin U.,Runde, Eileen,Williams, Linda,Wheeler, Larry A.,Garst, Michael E.
, p. 3533 - 3538 (1996)
We have synthesized 2-[(5-methylbenz-1-ox-4-azin-6- yl)imino]imidazoline, 3, a potent, peripherally acting α2 adrenoceptor agonist. The agent is conveniently prepared in five steps from 2-amino-m- cresol. The agent has demonstrated good selectivity for α2 adrenoceptors in binding and functional studies. When applied topically to eyes, the agent is efficacious for the reduction of intraocular pressure. The agent does not penetrate the blood-brain barrier and, as a consequence, does not lower blood pressure or induce sedation when administered topically or intravenously. We have determined the pK(a) and log P in water versus both octanol and dodecane of 3 and a set of related agents. The best physical parameter to explain its lack of central nervous system penetration appears to be log P measured in octanol versus water.
Compounds and method of treatment having agonist-like activity selective at alpha 2B or 2B/2C adrenergic receptors
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, (2008/06/13)
Methods and compounds for the treatment of conditions including pain, particularly chronic pain, glaucoma or elevated intraocular pressure with reduced cardiovascular or sedative side effects. Also included are methods of making and using such compounds.
