Detection of multiple H3 receptor affinity states utilizing [3H]A-349821, a novel, selective, non-imidazole histamine H3 receptor inverse agonist radioligand (Q24675612)

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Language	Label	Description	Also known as
English	Detection of multiple H3 receptor affinity states utilizing [3H]A-349821, a novel, selective, non-imidazole histamine H3 receptor inverse agonist radioligand	scientific article

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scholarly article

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Detection of multiple H3 receptor affinity states utilizing [3H]A-349821, a novel, selective, non-imidazole histamine H3 receptor inverse agonist radioligand (English)

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author name string

David G Witte

1

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Betty Bei Yao

2

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Thomas R Miller

3

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Tracy L Carr

4

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Steven Cassar

5

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Rahul Sharma

6

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Ramin Faghih

7

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Bruce W Surber

8

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Timothy A Esbenshade

9

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Arthur A Hancock

10

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Kathleen M Krueger

11

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language of work or name

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publication date

July 2006

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British Journal of Pharmacology

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148

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5

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657-70

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Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction

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7 April 2017

Measurement of protein using bicinchoninic acid

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G protein-dependent pharmacology of histamine H3 receptor ligands: evidence for heterogeneous active state receptor conformations

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Pharmacological properties of ABT-239 [4-(2-{2-[(2R)-2-Methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile]: I. Potent and selective histamine H3 receptor antagonist with drug-like properties

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Use of novel, non-imidazole inverse agonist radioligands to define histamine H3 receptor pharmacology

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N-substituted piperidinyl alkyl imidazoles: discovery of methimepip as a potent and selective histamine H3 receptor agonist

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28 September 2017

Pharmacological and behavioral properties of A-349821, a selective and potent human histamine H3 receptor antagonist

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Antiobesity effects of A-331440, a novel non-imidazole histamine H3 receptor antagonist

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An efficient multigram synthesis of the potent histamine H3 antagonist GT-2331 and the reassessment of the absolute configuration

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Protean agonism at histamine H3 receptors in vitro and in vivo

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28 September 2017

Molecular modeling and pharmacological analysis of species-related histamine H(3) receptor heterogeneity

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Synthesis and SAR of aminoalkoxy-biaryl-4-carboxamides: novel and selective histamine H3 receptor antagonists

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28 September 2017

Characteristics of recombinantly expressed rat and human histamine H3 receptors

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28 September 2017

High constitutive activity of native H3 receptors regulates histamine neurons in brain.

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28 September 2017

Selective ligands as tools to study histamine receptors

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=1751875

28 September 2017

Characterization of the binding of [3H]-clobenpropit to histamine H3-receptors in guinea-pig cerebral cortex membranes

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28 September 2017

Highly potent and selective ligands for histamine H3-receptors

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28 September 2017

Identification of two H3-histamine receptor subtypes

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Membrane reconstitution of high-affinity alpha 2 adrenergic agonist binding with guanine nucleotide regulatory proteins

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A new class of histamine H(3)-receptor antagonists: synthesis and structure-activity relationships of 7,8,9,10-tetrahydro-6H-cyclohepta[b]quinolines

1 reference

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30 May 2018

Two novel and selective nonimidazole histamine H3 receptor antagonists A-304121 and A-317920: I. In vitro pharmacological effects

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30 May 2018

Coordination of histamine H3 receptor antagonists with human adrenal cytochrome P450 enzymes

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30 May 2018

Characterisation of the specific binding of the histamine H3 receptor antagonist radioligand [3H]GR168320.

1 reference

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30 May 2018

[3H]-thioperamide as a radioligand for the histamine H3 receptor in rat cerebral cortex

1 reference

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30 May 2018

Potencies of antagonists chemically related to iodoproxyfan at histamine H3 receptors in mouse brain cortex and guinea-pig ileum: evidence for H3 receptor heterogeneity?

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=1751875

30 May 2018

Evaluation of the receptor selectivity of the H3 receptor antagonists, iodophenpropit and thioperamide: an interaction with the 5-HT3 receptor revealed

1 reference

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30 May 2018

Guanine nucleotides and pertussis toxin reduce the affinity of histamine H3 receptors on AtT-20 cells

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3H-dopamine binding to rat striatal D-2 and D-3 sites: enhancement by magnesium and inhibition by guanine nucleotides and sodium

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30 May 2018

Modification of guanine nucleotide-regulatory components in brain membranes. II. Relationship of guanosine 5'-triphosphate effects on opiate receptor binding and coupling receptors with adenylate cyclase

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30 May 2018

Biexponential kinetics of (R)-alpha-[3H]methylhistamine binding to the rat brain H3 histamine receptor.

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30 May 2018

Magnesium-Dependent Enhancement of Endogenous Agonist Binding to A1Adenosine Receptors: A Complicating Factor in Quantitative Autoradiography

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30 May 2018

Histamine H3 receptor binding sites in rat brain membranes: modulations by guanine nucleotides and divalent cations

1 reference

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30 May 2018

Characterisation of the binding of the histamine H3 receptor agonist [3H] (R)-alpha methyl histamine to homogenates of rat and guinea-pig cortex.

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30 May 2018

The first radiolabeled histamine H3 receptor antagonist, [125I]iodophenpropit: saturable and reversible binding to rat cortex membranes

1 reference

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30 May 2018

H3 receptor antagonist, thioperamide, inhibits adrenal steroidogenesis and histamine binding to adrenocortical microsomes and binds to cytochrome P450

1 reference

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30 May 2018

Use of an inverse agonist radioligand [3H]A-317920 reveals distinct pharmacological profiles of the rat histamine H3 receptor

1 reference

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28 November 2018

D-alanine piperazine-amides: novel non-imidazole antagonists of the histamine H3 receptor

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=1751875

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Aminoalkoxybiphenylnitriles as histamine-3 receptor ligands

1 reference

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28 November 2018

Constitutive activity of histamine h(3) receptors stably expressed in SK-N-MC cells: display of agonism and inverse agonism by H(3) antagonists

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=1751875

28 November 2018

Identification of rat H3 receptor isoforms with different brain expression and signaling properties.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=1751875

28 November 2018

Effects of iodoproxyfan, a potent and selective histamine H3 receptor antagonist, on alpha 2 and 5-HT3 receptors

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=1751875

28 November 2018

Binding characteristics of a histamine H3-receptor antagonist, [3H]S-methylthioperamide: comparison with [3H](R)alpha-methylhistamine binding to rat tissues

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=1751875

28 November 2018

Further concerns over Cheng-Prusoff analysis

1 reference

https://pubmed.ncbi.nlm.nih.gov/16715122

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

[125I]iodoproxyfan, a new antagonist to label and visualize cerebral histamine H3 receptors

1 reference

https://pubmed.ncbi.nlm.nih.gov/16715122

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Identifiers

10.1038/SJ.BJP.0706752

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