Structure‐activity studies on the potentiation of benzodiazepine receptor binding by ethylenediamine analogues and derivatives

Morgan, Page W.; Stone, T.W.

doi:10.1111/j.1476-5381.1983.tb10543.x

Cited by 15 publications

(6 citation statements)

References 30 publications

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“…The polyamines comprise agmatine, putrescine, spermidine, and spermine, and are involved in many cellular functions, including growth, division, and signaling cascades [Tabor and Tabor, 1984; Gilad and Gilad, 2003; Seiler and Raul, 2005]. Of particular importance to psychiatric disorders, the polyamines influence the properties of several neurotransmitter pathways, including the catecholamines [Deckardt et al, 1978; Hirsch et al, 1987; Bo et al, 1990; Ritz et al, 1994; Bastida et al, 2007], gamma amino‐butyric acid [Morgan and Stone, 1983; Brackley et al, 1990; Gilad et al, 1992; Seiler, 2004], nitric oxide [Galea et al, 1996], and glutamate [Lynch and Gallagher, 1996; Shim et al, 1999; Zomkowski et al, 2002, 2006; Li et al, 2003]. Numerous animal studies have demonstrated the antidepressant and anxiolytic effects of agmatine and putrescine [Zomkowski et al, 2002, 2004, 2005, 2006; Aricioglu and Altunbas, 2003; Lavinsky et al, 2003; Gong et al, 2006; Zeidan et al, 2007], and alterations in the levels of the polyamines and their metabolic enzymes have been observed in several psychiatric conditions, including suicide [Fiori and Turecki, 2008].…”

Section: Allelic Frequencies Of the In/del In Suicide Completers And mentioning

confidence: 99%

Anisotropic polyvinyl alcohol—Bacterial cellulose nanocomposite for biomedical applications

2008

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Compliance mismatch between the synthetic graft and the surrounding native tissue has been reported as a major factor in ultimate failure of the currently used cardiovascular graft replacements. Thus, developing biomaterials that display close mechanical properties as the tissue it is replacing is an important objective in biomedical devices design. Polyvinyl alcohol (PVA) is a biocompatible hydrogel with characteristics desired for biomedical applications. It can be crosslinked by a low temperature thermal cycling process. By using a novel thermal processing method under an applied strain and with the addition of a small amount of bacterial cellulose (BC) nanofibers, an anisotropic PVA-BC nanocomposite was created. The stress-strain tensile properties of porcine aorta were closely matched in both the circumferential and the axial directions by one type of anisotropic PVA-BC nanocomposite (10% PVA with 0.3% BC at 75% initial strain and cycle 2) within physiological range, with improved resistance to further stretch beyond physiological strains. The PVA-BC nanocomposite gives a broad range of mechanical properties, including anisotropy, by controlling material and processing parameters. PVA-BC nanocomposites with controlled degree of anisotropy that closely match the mechanical properties of the soft tissue it might replace, ranging from cardiovascular to other connective tissues, can be created.

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Section: Allelic Frequencies Of the In/del In Suicide Completers And mentioning

confidence: 99%

Anisotropic polyvinyl alcohol—Bacterial cellulose nanocomposite for biomedical applications

2008

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“…These attempts might be clinically helpful, if recovery time or residual effects have to be minimized. Conflicting data have been reported for physostigmine (Avant et al, 1979;Grote et al, 1981;Pandit et al, 1983) and the observed effects of theophylline (Arvidsson et al, 1982;Henauer et al, 1983) might be due to ethylenediamine which is part of the aminophylline preparation used and which is known to interact with the binding of [3H]-diazepam in cerebral cortical synaptosomal membranes (Morgan & Stone, 1983). The new imidazodiazepine Ro 15-1788 can reverse the sedative effects of 3-methylclonazepam (Darragh et al, 1981), diazepam (Darragh et al, 1982), flunitrazepam (Gaillard & Blois, 1983) and midazolam (Klotz et al, 1984a).…”

Section: Introductionmentioning

confidence: 99%

Flunitrazepam and lormetazepam do not affect the pharmacokinetics of the benzodiazepine antagonist Ro 15‐1788.

Klotz¹,

Duka²,

Dorow³

et al. 1985

Brit J Clinical Pharma

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Following a single intravenous dose of 0.1 mg/kg, the pharmacokinetics of Ro 15‐1788, a specific benzodiazepine antagonist, have been investigated in 20 healthy male volunteers. In random order injection of Ro 15‐1788 has been preceded (5 min) by intravenous dosing with 0.06 mg/kg of lormetazepam (n = 6), 0.03 mg/kg of flunitrazepam (n = 8) or placebo (n = 6). The rapid elimination of the antagonist could be characterized by an elimination half‐life between 0.9 to 1.4 h and a total plasma clearance of 727 to 1440 ml/min. These single dose studies indicate that the disposition of Ro 15‐1788 was not affected by the acute coadministration of both benzodiazepines.

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“…Of particular importance to psychiatric disorders, the polyamines influence the properties of several neurotransmitter pathways, including the catecholamines [Deckardt et al, 1978;Hirsch et al, 1987;Bo et al, 1990;Ritz et al, 1994;Bastida et al, 2007], gamma amino-butyric acid [Morgan and Stone, 1983;Brackley et al, 1990;Gilad et al, 1992;Seiler, 2004], nitric oxide [Galea et al, 1996], and glutamate [Lynch and Gallagher, 1996;Shim et al, 1999;Zomkowski et al, 2002Zomkowski et al, , 2006Li et al, 2003]. Numerous animal studies have demonstrated the antidepressant and anxiolytic effects of agmatine and putrescine [Zomkowski et al, 2002[Zomkowski et al, , 2004[Zomkowski et al, , 2005[Zomkowski et al, , 2006Aricioglu and Altunbas, 2003;Lavinsky et al, 2003;Gong et al, 2006;Zeidan et al, 2007], and alterations in the levels of the polyamines and their metabolic enzymes have been observed in several psychiatric conditions, including suicide [Fiori and Turecki, 2008].…”

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confidence: 99%

Association of the SAT1 in/del polymorphism with suicide completion

Fiori

Turecki

2009

American J of Med Genetics Pt B

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Several studies have observed decreased expression of spermidine/spermine N1-acetyltransferase (SAT1) in the brains of suicide completers, and we previously identified a single-nucleotide polymorphism in the promoter region of SAT1 which was associated with suicide completion and SAT1 expression in the brain. We recently characterized the haplotype structure of the SAT1 promoter region and identified an insertion/deletion (in/del) of 15 adenine residues. This variant appears to be a predictor of SAT1 expression, and we were thus interested in determining if the lower expressing deletion allele was found more frequently among suicide completers. To this end, we genotyped the in/del in a sample of 771 French-Canadian males, comprising 326 suicide completers and 445 non-suicide controls. We found no significant difference in the frequencies of the two alleles between suicide completers and controls in the entire sample. However, we observed a significantly higher frequency of the deletion in the depressed suicide completers compared to the depressed non-suicides. These results add support for a role of SAT1 in conferring a risk for suicide completion, in particular in the context of depressive disorders.

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Structure‐activity studies on the potentiation of benzodiazepine receptor binding by ethylenediamine analogues and derivatives

Cited by 15 publications

References 30 publications

Anisotropic polyvinyl alcohol—Bacterial cellulose nanocomposite for biomedical applications

Anisotropic polyvinyl alcohol—Bacterial cellulose nanocomposite for biomedical applications

Flunitrazepam and lormetazepam do not affect the pharmacokinetics of the benzodiazepine antagonist Ro 15‐1788.

Association of the SAT1 in/del polymorphism with suicide completion

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