Elsevier S & T

Excitatory Amino Acids: Clinical Results with Antagonists

Herrling, Paul L.

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Table of contents
  • Cover
  • Contentsv
  • Contributorsix
  • Prefacexi
  • Acknowledgmentsxiii
  • Chapter 1. Selfotel (CGS 19755)1
  • 1. Summary1
  • 2. Overview of the pharmacology2
  • 3. Rationale for clinical testing4
  • 4. Human results4
  • 5. Conclusions6
  • Chapter 2. D-CPPene (SDZ EAA-494)„A Competitive NMDA Antagonist: Pharmacology and Results in Human7
  • 1. Summary7
  • 2. Structure-activity relationships8
  • 3. General pharmacology11
  • 4. Human studies17
  • 5. Discussion20
  • 6. Conclusion21
  • Chapter 3. Intrathecal Administration of a Competitive NMDA Receptor Antagonist for Pain Treatment23
  • 1. Summary23
  • 2. Overview of the pharmacology23
  • 3. Rationale for clinical testing24
  • 4. Human results25
  • 5. Discussion26
  • Chapter 4. Clinical Experience with the NMDA Ion Channel Blocker, Aptiganel Hydrochloride (CERESTAT?31
  • 1. Summary31
  • 2. Pharmacology32
  • 3. Clinical studies in normal male volunteers34
  • 4. Clinical studies in patients34
  • 5. Discussion41
  • Chapter 5. Development of ACPC, A Partial Agonist of the Glycine Site on the NMDA Receptor43
  • 1. Introduction43
  • 2. Partial agonism as a therapeutic approach43
  • 3. ACPC – pharmacology and mechanism of action44
  • 4. Efficacy of ACPC in animal models of neuroprotection44
  • 5. Efficacy of ACPC in animal models of depression and anxiety48
  • 6. Prevention of opiate tolerance and toxicity by ACPC49
  • 7. Pharmacokinetics50
  • 8. Safety profiles of ACPC in animal models52
  • 9. PCP-like effects53
  • 10. Phase I clinical trials of ACPC54
  • Chapter 6. Ifenprodil and Eliprodil: Neuroprotective NMDA Receptor Antagonists and Calcium Channel B57
  • 1. Introduction57
  • 2. The NMDA receptor complex and its regulation59
  • 3. Actions of ifenprodil and eliprodil at different sites of the NMDA receptor59
  • 4. Other sites of action of ifenprodil and eliprodil71
  • 5. Neuroprotective effects73
  • 6. Behavioral pharmacology and side-effect profile75
  • 7. Pharmacokinetics78
  • 8. Clinical trials79
  • 9. Conclusions79
  • Chapter 7. (3S,4aR,6R,8aR)-6-[2-(1(2)H-Tetrazole-5-yl)ethyl]decahydroisoquinoline-3-carboxylic Acid81
  • 1. Summary81
  • 2. LY293558 as a novel neuroprotectant compound81
  • 3. In vitro glutamate receptor profile82
  • 4. In vivo AMPA receptor antagonism83
  • 5. Effects of LY293558 on CNS excitability83
  • 6. In vivo neuroprotection against AMPA-induced excitotoxicity84
  • 7. Neuroprotectant activity in animal models of cerebral ischemia85
  • 8. Overview and discussion86
  • Chapter 8. The NBQX Story89
  • 1. Summary89
  • 2. Pharmacology89
  • 3. Human pharmacology96
  • 4. Discussion97
  • Chapter 9. Riluzole in Amyotrophic Lateral Sclerosis99
  • 1. Summary99
  • 2. Introduction99
  • 3. Chemical structure100
  • 4. Neuroprotective properties100
  • 5. Mechanism(s) of action101
  • 6. Rationale of clinical testing101
  • 7. Clinical results102
  • 8. Conclusion108
  • Chapter 10. Preclinical and Clinical Aspects of Remacemide Hydrochloride109
  • 1. Preclinical efficacy studies109
  • 2. Clinical studies117
  • 3. Conclusions120
  • Glossary121
  • Summary Table of Compounds and Their Clinical Status125
  • References129
  • Index153
Book details
  • Vendor Elsevier S & T
  • SKU 9780125468206
  • ISBN-13 9780080531342
  • Author Herrling, Paul L.
  • Category Medical
  • Subject Biochemistry

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Glutamate is the major excitatory neurotransmitter in the brain and dysfunction of glutamate transmission is the likely cause of a variety of diseases including neurodegeneration following cerebral ischemia, Huntington's chorea, amyotrophic lateral sclerosis, epilepsy, spasticity, emesis, chronic pain, and schizophrenia. Excitatory amino acid receptor agonists and antagonists are therefore of major interest as potential drugs for central nervous system disorders. Excitatory Amino Acids is the first book entirely dedicated to the results of human testing of modulators of excitatory amino acid neurotransmitters.

Features include:
* Coverage of the field of excitatory amino acids from synaptic function to preclinical and clinical pharmacology
* Description of the development of NMDA (Nmethyl-d-aspartate) and non-NMDA antagonists
* Reports of potential drugs in early and late clinical stages of development.