Selective therapeutic applications

The possibility that 11-desoxyprostaglandins might exhibit tissue selectivity in therapeutic applications provided an incentive to develop a short synthetic route to this series (Ref. 1). 

Histamine produces its pharmacological actions by three subtypes of receptors the postsynaptic Hi and H2 receptors and the presynaptic H3 receptor. The H3 receptor is mainly located in the central nervous system (CNS), where it acts as an inhibitory autoreceptor in the central histaminergic neuronal pathways [176]. A number of therapeutic applications have been proposed for selective H3 receptor antagonists, including several CNS disorders such as Alzheimer s disease. Attention Deficit Hyperactivity Disorder, Schizophrenia, or for enhancing memory or obesity control. 

The Role of DPls in Therapy briefly discusses factors affecting the therapeutic profiles of drugs delivered by DPI devices. The article concludes with The Burgeoning DPI Industry, which surveys the DPI products on the market in 1999 and a selection of those known to be under development. Thoughts on the potential of the DPI dosage form in future therapeutic applications conclude the article. 

Amino-3-fluorobenzoic acid is an important intermediate in the synthesis of derivatives of indole, such as the potent and selective thromboxane/prostaglandin endoperoxide receptor antagonist L-670,596 or the anti-inflammatory agent Etodolac. Compounds of this type have therapeutic applications. 2-Amino-3-fluoro-benzoic add is aiso an important precursor for the synthesis of fluoroacridines, which can be converted to interesting tridentate ligands, such as Acriphos. ... 

The physiology and pathology of excitatory amino acid neurotransmission is described by C.G. Parsons, W. Danysz and W. ZieglgSnsberger. At present, there seems to be a consensus that competitive AMPA and N-methyl-o-aspar-tate (NMDA) receptor antagonists have a low chance of finding therapeutic applications. Antagonists showing moderate affinity and satisfactory selectivity for certain NMDA receptor subtypes seem to have a more favourable profile. 

Compston JE. Selective oestrogen receptor modulators potential therapeutic applications. Clin Endocrinol (Oxf) 1998 48(4) 389-91. 

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