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Insights into Structure-Activity Relationships and CNS Therapeutic Applications of NR2B Selective Antagonists

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Excessive stimulation of NMDA receptors is involved in various CNS pathologies such as Parkinson's disease, acute and chronic pain and cerebral ischaemia. The use of NMDA antagonists as therapeutic agents has been restricted as a result of unwanted side effects including hallucinations and loss of co-ordination. NR2B subtype selective antagonists have previously shown a therapeutic effect without causing the side effects of broad spectrum NMDA antagonists. Considerable research has since been devoted to the development of orally bioavailable, selective NR2B antagonists and their applications in various neurological diseases. The improved therapeutic index of these compounds is expected to be the result of the subtype selectivity and cellular location of the NR2B receptors within the CNS. This review describes recent advances in the development of NR2B antagonists as well as their therapeutic applications.

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Keywords: 3,4-difluoro-substitution; 4-dihydroquinolinon; 4-methylsulfonamide; 4-trifluoromethoxy; 7-hydroxy analogue; Affinities; Alzheimer's Disease; Aminoheterocycle Derivatives; Aniline; Antagonist; CNS; Cyclohexanol Phenols; Enantiomeric Propanolamines; Ethylenediamine; Heterocycles; Heterocyclic; Huntington's Disease; Ifenprodil; Immunocytochemical; Kynurenic Acid Amides; L-DOPA therapy; NEUROLOGICAL; NMDA antagonists; NMDA receptors; NR2B; NR2B Selective Antagonists; Neurological disease; Pharmacokinetic Data; Propanolamines; SAfiRs; Structure-activity relationships; Tahirovic; Various Cinnamidines; aforementioned; allodynia; anti-Parkinsonian effects; anti-nociceptive effects; antinociceptive; autoradiography; carageenan-induced; cinnamidine-based NR2B; cinnamidines; cyclohexane; cyclohexane derivatives; discriminate; discrimination; dysphoria; enantiomeric propranolamines; enantioselectivity; epileptiform; excitotoxicity; extrasynaptic NR2B; extrasynaptically; glutamate; homopiperidine; hydroxyl group; hyperalgesia; ifenprodil pharmacophore; in vivo evaluation; intraperitoneal; isobutyl; lipophilic; metabotropic glutamate; mousepartial-sciatic-nerve-ligation; naphthamidine; neurodegeneration; neuroprotective effects; noradrenalin; paroxysmal disorder; pharmacokinetic; pharmacokinetics; phenylpropyl subunit; piperidines; polycyclic units; propanolamines; psychomimetic; repolarization; rigidification; sensorimotor; thiadiazolyl; thiosemicarbazide; trifluoromethoxyphenyl

Document Type: Research Article

Publication date: 01 December 2010

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