Search Results - "Brad D. Manion"
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A synthetic 18-norsteroid distinguishes between two neuroactive steroid binding sites on GABAA receptors
Published in The Journal of pharmacology and experimental therapeutics (01-05-2010)“…In the absence of GABA, neuroactive steroids that enhance GABA-mediated currents modulate binding of [35S]t-butylbicyclophosphorothionate in a biphasic manner,…”
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2
Activation and modulation of recombinant glycine and GABA A receptors by 4-halogenated analogues of propofol
Published in British journal of pharmacology (01-11-2016)“…Glycine receptors are important players in pain perception and movement disorders and therefore important therapeutic targets. Glycine receptors can be…”
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3
Neurosteroid Analogues. 18. Structure–Activity Studies of ent-Steroid Potentiators of γ‑Aminobutyric Acid Type A Receptors and Comparison of Their Activities with Those of Alphaxalone and Allopregnanolone
Published in Journal of medicinal chemistry (09-01-2014)“…A model of the alignment of neurosteroids and ent-neurosteroids at the same binding site on γ-aminobutyric acid type A (GABAA) receptors was evaluated for its…”
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4
11-trifluoromethyl-phenyldiazirinyl neurosteroid analogues: potent general anesthetics and photolabeling reagents for GABAA receptors
Published in Psychopharmacology (01-09-2014)“…Rationale While neurosteroids are well-described positive allosteric modulators of gamma-aminobutyric acid type A (GABA A ) receptors, the binding sites that…”
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5
Neurosteroid Analogues. 17. Inverted Binding Orientations of Androsterone Enantiomers at the Steroid Potentiation Site on γ-Aminobutyric Acid Type A Receptors
Published in Journal of medicinal chemistry (09-02-2012)“…The enantiomer pair androsterone and ent-androsterone are positive allosteric modulators of γ-aminobutyric acid (GABA) type A receptors. Each enantiomer was…”
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Neurosteroid Analogues. 16. A New Explanation for the Lack of Anesthetic Effects of Δ16-Alphaxalone and Identification of a Δ17(20) Analogue with Potent Anesthetic Activity
Published in Journal of medicinal chemistry (09-06-2011)“…This study addresses the hypothesis that the lack of anesthetic activity for (3α,5α)-3-hydroxypregn-16-ene-11,20-dione (Δ16-alphaxalone) is explained by the…”
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Neurosteroid analogues. 16. A new explanation for the lack of anesthetic effects of δ(16)-alphaxalone and identification of a δ(17(20)) analogue with potent anesthetic activity
Published in Journal of medicinal chemistry (09-06-2011)“…This study addresses the hypothesis that the lack of anesthetic activity for (3α,5α)-3-hydroxypregn-16-ene-11,20-dione (Δ(16)-alphaxalone) is explained by the…”
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Neurosteroid analogues. 12. Potent enhancement of GABA-mediated chloride currents at GABAA receptors by ent-androgens
Published in European journal of medicinal chemistry (2008)“…Allopregnanolone (1) and pregnanolone (2), steroids containing a 17beta-acetyl group, are potent enhancers of GABA (gamma-aminobutyric acid) action at GABAA…”
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9
Photoaffinity labeling with a neuroactive steroid analogue. 6-azi-pregnanolone labels voltage-dependent anion channel-1 in rat brain
Published in The Journal of biological chemistry (11-04-2003)“…Neuroactive steroids modulate the function of gamma-aminobutyric acid, type A (GABA(A)) receptors in the central nervous system by an unknown mechanism. In…”
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10
Neurosteroid Analogues. 14. Alternative Ring System Scaffolds: GABA Modulatory and Anesthetic Actions of Cyclopenta[b]phenanthrenes and Cyclopenta[b]anthracenes
Published in Journal of medicinal chemistry (13-03-2008)“…Although the structural features of binding sites for neuroactive steroids on γ-aminobutryic acid type A (GABAA) receptors are still largely unknown,…”
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11
Neurosteroid analogues. 15. A comparative study of the anesthetic and GABAergic actions of alphaxalone, Δ16-alphaxalone and their corresponding 17-carbonitrile analogues
Published in Bioorganic & medicinal chemistry letters (15-11-2010)“…Alphaxalone, a neuroactive steroid containing a 17β-acetyl group, has potent anesthetic activity in humans. This pharmacological activity is attributed to this…”
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12
Anticonvulsant and anesthetic effects of a fluorescent neurosteroid analog activated by visible light
Published in Nature neuroscience (01-04-2007)“…Most photoactivatable compounds suffer from the limitations of the ultraviolet wavelengths that are required for activation. We synthesized a neuroactive…”
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13
Neurosteroid Analogues. 11. Alternative Ring System Scaffolds: γ-Aminobutyric Acid Receptor Modulation and Anesthetic Actions of Benz[f]indenes
Published in Journal of medicinal chemistry (27-07-2006)“…Benz[f]indenes are tricyclic compounds with a linear 6-6-5 fused carbocyclic ring system. When properly substituted, benz[f]indenes can satisfy the…”
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14
Neurosteroid Analogues. 10. The Effect of Methyl Group Substitution at the C-6 and C-7 Positions on the GABA Modulatory and Anesthetic Actions of (3α,5α)- and (3α,5β)-3-Hydroxypregnan-20-one
Published in Journal of medicinal chemistry (21-04-2005)“…The planar 5α-reduced steroid (3α,5α)-3-hydroxypregnan-20-one and the nonplanar 5β-reduced steroid (3α,5β)-3-hydroxypregnan-20-one act at GABAA receptors to…”
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15
Neurosteroid Analogues. 9. Conformationally Constrained Pregnanes: Structure−Activity Studies of 13,24-Cyclo-18,21-dinorcholane Analogues of the GABA Modulatory and Anesthetic Steroids (3α,5α)- and (3α,5β)-3-Hydroxypregnan-20-one
Published in Journal of medicinal chemistry (04-12-2003)“…The hydrogen-bond-acceptor properties of the carbonyl moiety in the 17β-acetyl group on the D-ring of the anesthetic steroids (3α,5α)- and…”
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16
Neuroactive steroid interactions with voltage-dependent anion channels: lack of relationship to GABA(A) receptor modulation and anesthesia
Published in The Journal of pharmacology and experimental therapeutics (01-02-2004)“…Neuroactive steroids modulate the function of gamma-aminobutyric acid type A (GABA(A)) receptors in brain; this is the presumed basis of their action as…”
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17
Photoaffinity Labeling with a Neuroactive Steroid Analogue
Published in The Journal of biological chemistry (11-04-2003)“…Neuroactive steroids modulate the function of γ-aminobutyric acid, type A (GABA A ) receptors in the central nervous system by an unknown mechanism. In this…”
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18
Activation and modulation of recombinant glycine and GABA sub(A) receptors by 4-halogenated analogues of propofol
Published in British journal of pharmacology (01-11-2016)“…Background and Purpose Glycine receptors are important players in pain perception and movement disorders and therefore important therapeutic targets. Glycine…”
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19
Activation and modulation of recombinant glycine and GABAA receptors by 4‐halogenated analogues of propofol
Published in British journal of pharmacology (01-11-2016)“…Background and Purpose Glycine receptors are important players in pain perception and movement disorders and therefore important therapeutic targets. Glycine…”
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20
11-trifluoromethyl-phenyldiazirinyl neurosteroid analogues: potent general anesthetics and photolabeling reagents for [GABA.sub.A] receptors
Published in Psychopharmacology (01-09-2014)“…Rationale While neurosteroids are well-described positive allosteric modulators of gamma-aminobutyric acid type A ([GABA.sub.A]) receptors, the binding sites…”
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