Showing papers in "Annual Reports in Medicinal Chemistry in 2002"

Chapter 16. Therapeutic applications of non-peptidic δ-opioid agonists graham

Abstract: A number of ligands for the δ-opioid receptor have been disclosed over the past few years. The majority of research has focused on compounds derived from the piperazine derivative, BW373U86 ( 9 ). To date, several compounds combining subnanomolar potency and excellent selectivity have been identified. Much effort has been directed towards the optimisation of physicochemical and pharmacokinetic properties, which has led to the identification of compounds with improved properties. However, there is as yet no reported clinical data to support pre-clinical experiments implicating the activation of the δ-opioid receptor for the treatment of pain or motility impairment. It therefore remains to be seen whether selective activation of S-opioid receptors will indeed have clinical benefit.

Chapter 8. Purine and pyrimidine nucleotide (P2) receptors

Abstract: There is rapidly growing interest in receptors for ATP, ADP, UTP, UDP and other nucleotides. The P2 receptor family comprises both metabotropic (P2Y) and ionotropic (P2X) receptors, at which ATP acts as a fast neurotransmitter, and at least one subtype of P2 receptors is found on nearly every cell. The future challenge for medicinal chemists lies in how to develop subtype-selective agonists and antagonists that are biovailable and stable in vivo. The discovery of such agents is relevant to treatment of disorders of the autonomic nervous system, central nervous system, respiratory system and the cardiovascular and renal systems.