Progress in Neuro-Psychopharmacology and Biological Psychiatry
Critical reviews and theoretical articlesA review of recently-developed ligands for neuronal benzodiazepine receptors and their pharmacological activities
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Cited by (29)
Procognitive effect of AC-3933 in aged mice, and synergistic effect of combination with donepezil in scopolamine-treated mice
2014, European Journal of PharmacologyCitation Excerpt :Benzodiazepine receptor inverse agonists, such as β-carbolines, decrease the gating of GABA-linked chloride ion channels and attenuate GABAergic inhibition. They consequently facilitate cholinergic transmission and augment cognitive function, and as such, have good potential in the treatment of senile dementia, including Alzheimer׳s disease (Chorvat et al., 1998; Gardner, 1992). However, benzodiazepine receptor inverse agonists with high intrinsic activity (i.e. full inverse agonists) strongly attenuate GABAergic inhibition, thereby inducing undesirable effects like anxiety and convulsion (Contó et al., 2005; Evans and Lowry, 2007).
Pharmacological properties of AC-3933, a novel benzodiazepine receptor partial inverse agonist
2014, NeuroscienceCitation Excerpt :Conversely, BzR inverse agonists, such as β-carboline, reduce GABA effects and hence increase the overall excitability of neurons. Since BzR inverse agonists with high intrinsic activity, (i.e. full inverse agonists) strongly attenuate GABAergic inhibition, they induce undesirable effects, including anxiety and convulsion (Gardner, 1992; Contó et al., 2005). On the other hand, BzR inverse agonists with low intrinsic activity (i.e. partial inverse agonist) are expected to exert modest excitability of neurons and hence produce minimal side effects.
High affinity central benzodiazepine receptor ligands. Part 2: Quantitative structure-activity relationships and comparative molecular field analysis of pyrazolo[4,3-c]quinolin-3-ones
2001, Bioorganic and Medicinal ChemistryCitation Excerpt :In this context, research based on traditional binding affinity and intrinsic efficacy studies can still play a role to improve our knowledge on the main structural requirements necessary for a high binding affinity and possibly a well defined intrinsic activity.9–14 Indeed, several pharmacophore models proved useful for the design of new and potent BzR ligands.15 In this field, a significant contribution also came from 2-D and 3-D QSAR studies16,17 on a new class of BzR ligands, the 2-aryl-2,5-dihydropyridazino[4,3-b]indol-3(3H)-ones and from a preliminary 2-D QSAR study18 on a structurally related class of ligands, the well known 2-aryl-2,5-dihydropyrazolo[4,3-c]quinoline-3(3H)-ones (PQs).19
Molecular modeling and QSAR analysis of the interaction of flavone derivatives with the benzodiazepine binding site of the GABA<inf>A</inf> receptor complex
2001, Bioorganic and Medicinal ChemistryCitation Excerpt :Furthermore, the regional heterogeneity of the GABAA–BDZ-bs complex has been suggested as another reason for the multiplicity of pharmacological properties of BDZ-bs ligands. The enormous amount of structure–activity relationship (SAR) data available for a diversity of ligands has resulted in the formulation of several pharmacophore models for the BDZ-bs.9–18 The common feature of these models is the attempt to explain ligand efficacy as a function of ligand–receptor interaction at a molecular level.
Synthesis and BZR affinity of pyrazolo[1,5-a]pyrimidine derivatives. Part 1: Study of the structural features for BZR recognition
1999, Bioorganic and Medicinal ChemistrySynthesis and structure-affinity relationships at the central benzodiazepine receptor of pyridazino[4,3-b]indoles and Indeno[1,2-c]pyridazines
1999, Bioorganic and Medicinal Chemistry