Peripheral benzodiazepine receptors: on mice and human brain imaging

Weissman, Ben Avi; Raveh, Lily

doi:10.1046/j.1471-4159.2003.01568.x

Cited by 48 publications

(29 citation statements)

References 42 publications

(45 reference statements)

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“…For instance, radiolabeled PK11195 has been used in imaging of mitochondrial benzodiazepine receptor-rich cells by positron emission tomography scanning (47). PK11195 in FRhK4 cells increased the amount of HIV-1 cDNA being synthesized, but it had no apparent effect on its transport to the nucleus.…”

Section: Discussionmentioning

confidence: 99%

Lv1 Inhibition of Human Immunodeficiency Virus Type 1 Is Counteracted by Factors That Stimulate Synthesis or Nuclear Translocation of Viral cDNA

Berthoux

Sebastian²,

Sokolskaja³

et al. 2004

J Virol

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Section: Discussionmentioning

confidence: 99%

Lv1 Inhibition of Human Immunodeficiency Virus Type 1 Is Counteracted by Factors That Stimulate Synthesis or Nuclear Translocation of Viral cDNA

Berthoux

Sebastian²,

Sokolskaja³

et al. 2004

J Virol

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“…alpha arylation | heterocycle | isoquinoline-N-oxide | one-pot T he isoquinoline motif and its derivatives form the cores of numerous natural products (1,2), are the central components of a number of pharmaceutical agents (3)(4)(5), and can provide the scaffold for chiral ligands (6,7) and valuable organic materials (8). However, traditional isoquinoline syntheses such as the Bischler-Napieralski (9, 10), Pictet-Spengler (11,12), and Pomeranz-Fritsch reactions (13)(14)(15) all centre around the lynchpin of electrophilic aromatic substitution and are thus often limited to electron-rich carbocycles (Scheme 1A).…”

mentioning

confidence: 99%

Synthesis of substituted isoquinolines utilizing palladium-catalyzed α-arylation of ketones

Donohoe

Pilgrim

Jones

et al. 2012

Proc. Natl. Acad. Sci. U.S.A.

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The utilization of sequential palladium-catalyzed α-arylation and cyclization reactions provides a general approach to an array of isoquinolines and their corresponding N-oxides. This methodology allows the convergent combination of readily available precursors in a regioselective manner and in excellent overall yields. This powerful route to polysubstituted isoquinolines, which is not limited to electron rich moieties, also allows rapid access to analogues of biologically active compounds.T he isoquinoline motif and its derivatives form the cores of numerous natural products (1, 2), are the central components of a number of pharmaceutical agents (3-5), and can provide the scaffold for chiral ligands (6, 7) and valuable organic materials (8). However, traditional isoquinoline syntheses such as the Bischler-Napieralski (9, 10), 12), and Pomeranz-Fritsch reactions (13-15) all centre around the lynchpin of electrophilic aromatic substitution and are thus often limited to electron-rich carbocycles (Scheme 1A). It is also imperative to develop routes to highly-substituted isoquinolines to fully explore this chemical space, for example, for potential pharmaceutical targets. While recent synthetic efforts have greatly expanded the diversity of isoquinoline motifs available (16-29), new routes to isoquinolines are still highly desirable, particularly ones with the ability to directly access the isoquinoline moiety in a range of oxidation levels and which do not require highly-specialized starting materials.Originally reported by Palucki and Buchwald (30), Hamann and Hartwig (31), and Miura and coworkers (32), the palladiumcatalyzed α-arylation of enolates has recently emerged as a powerful new reaction in synthetic organic chemistry (33-35). Key to its success has been the design of appropriate ligands for palladium that have precisely engineered steric and electronic properties to enable the various steps in the catalytic cycle to proceed with maximum efficiency (36-39). The reaction's utility has also been greatly enhanced by the development of robust preformed palladium catalysts. Properties such as air stability and very high reactivity in a range of systems have greatly expanded the potential uses of these catalysts (40-43). However, the α-arylation reaction has seen limited use in the de novo construction of aromatic compounds (44-51) and is still greatly underused in this regard, especially because the bond forming abilities provided by this powerful reaction can greatly simplify the design of routes to heavily-substituted aromatic compounds. Hence, we decided to explore the scope of this new catalytic method in the synthesis of important heteroaromatic ring systems, beginning our investigations with the isoquinoline nucleus. ResultsIn our disconnection approach we envisaged that key pseudo-1,5-dicarbonyl intermediates 3 could be accessed via the palladiumcatalyzed α-arylation of ketones 1 with aryl halides 2 possessing a protected aldehyde or ketone in the ortho-position (52). Subsequent treatment of these inter...

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“…Regulation of CSR in B cells is coordinated with the germ line transcription (GLT) of CH genes, as well as the induction of activation-induced cytidine deaminaseMidazolam (MDZ), a benzodiazepine (BZD), is an intravenously administered anesthetic used for premedication, induction and maintenance of general anesthesia, as well as for sedation in the treatment of nervous dental patients. There are two types of BZD receptors, centraltype BZD receptors (CBRs) and peripheral-type BZD receptors (PBRs) (7,8). CBRs are expressed mainly in the central nervous system (7), while PBRs are detected in many peripheral tissues, cells and organs, such as the kidney, endocrine organs and monocytes (7,8).…”

Section: Introductionmentioning

confidence: 99%

“…There are two types of BZD receptors, centraltype BZD receptors (CBRs) and peripheral-type BZD receptors (PBRs) (7,8). CBRs are expressed mainly in the central nervous system (7), while PBRs are detected in many peripheral tissues, cells and organs, such as the kidney, endocrine organs and monocytes (7,8). PBRs are reportedly involved in regulation of cellular proliferation, immunomodulation, steroidogenesis, and oxidative processes, as well as programmed cell death (7,8).…”

Section: Introductionmentioning

confidence: 99%

“…CBRs are expressed mainly in the central nervous system (7), while PBRs are detected in many peripheral tissues, cells and organs, such as the kidney, endocrine organs and monocytes (7,8). PBRs are reportedly involved in regulation of cellular proliferation, immunomodulation, steroidogenesis, and oxidative processes, as well as programmed cell death (7,8). MDZ has also been shown to inhibit IL-6 mRNA expression in human peripheral blood mononuclear cells (9), and to suppress lipopolysaccharide (LPS)-induced release of nitric oxide and TNF-α from rat microglia via PBRs (10).…”

Section: Introductionmentioning

confidence: 99%

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Midazolam inhibits IgE production in mice via suppression of class switch recombination

2014

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Anaphylactic shock is characterized by increased capillary permeability and a decline in blood pressure due to excessive production of IgE. Midazolam (MDZ) is reported to have immunomodulatory properties. However, little is known about the effect of MDZ on the production of IgE antibody. We examined whether MDZ can suppress antigenspecific and total IgE production followed by IgE class switch recombination (CSR). MDZ was administered intraperitoneally to mice prior to ovalbumin (OVA) plus native cholera toxin (nCT) immunization. Serum OVA-specific and total IgE responses, and surface IgE-positive B cells were analyzed by ELISA and flow cytometry. Furthermore, expression levels of CSRassociated molecules such as germ-line transcript ε (εGLT), germ-circle tanscript ε (εCT), AID, and Id2 in the spleen were compared. The levels of interferongamma (IFN-γ) and interleukin (IL)-4 mRNA and protein were also examined in the spleen and serum. MDZ significantly suppressed OVA-specific and total IgE levels in plasma and surface IgE-positive B cells in the spleen. Moreover, MDZ-treated mice had significantly reduced levels of εGLT and εCT. Furthermore, although the levels of IFN-γ mRNA and protein were significantly elevated, those of IL-4 were reduced in MDZ-treated mice. Therefore, MDZ may be an important modulator of allergic responses through its ability to downregulate IgE production. (J Oral Sci 56, 77-83, 2014)

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Peripheral benzodiazepine receptors: on mice and human brain imaging

Cited by 48 publications

References 42 publications

Lv1 Inhibition of Human Immunodeficiency Virus Type 1 Is Counteracted by Factors That Stimulate Synthesis or Nuclear Translocation of Viral cDNA

Lv1 Inhibition of Human Immunodeficiency Virus Type 1 Is Counteracted by Factors That Stimulate Synthesis or Nuclear Translocation of Viral cDNA

Synthesis of substituted isoquinolines utilizing palladium-catalyzed α-arylation of ketones

Midazolam inhibits IgE production in mice via suppression of class switch recombination

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