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Discovery of histamine H3 antagonists for the treatment of cognitive disorders and Alzheimer's disease

The Journal of pharmacology and experimental therapeutics, 2011-01, Vol.336 (1), p.38

2011

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An 80-amino acid deletion in the third intracellular loop of a naturally occurring human histamine H3 isoform confers pharmacological differences and constitutive activity

The Journal of pharmacology and experimental therapeutics, 2007-12, Vol.323 (3), p.888

2007

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Structure–activity relationships of arylbenzofuran H3 receptor antagonists

Bioorganic & medicinal chemistry letters, 2005-05, Vol.15 (10), p.2559-2563

2005

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Antagonism of supraspinal histamine H3 receptors modulates spinal neuronal activity in neuropathic rats

The Journal of pharmacology and experimental therapeutics, 2012-10, Vol.343 (1), p.13

2012

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Design of a New Histamine H3 Receptor Antagonist Chemotype: (3aR,6aR)-5-Alkyl-1-aryl-octahydropyrrolo[3,4-b]pyrroles, Synthesis, and Structure−Activity Relationships

Journal of medicinal chemistry, 2009-08, Vol.52 (15), p.4640-4649

2009

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In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists : Trends across multiple chemical series

Bioorganic & medicinal chemistry letters, 2008, Vol.18 (1), p.355-359

2008

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H4 receptor antagonism exhibits anti-nociceptive effects in inflammatory and neuropathic pain models in rats

Pharmacology, biochemistry and behavior, 2010-03, Vol.95 (1), p.41-50

2010

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Pharmacological properties and procognitive effects of ABT-288, a potent and selective histamine H3 receptor antagonist

The Journal of pharmacology and experimental therapeutics, 2012-10, Vol.343 (1), p.233

2012

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Rotationally Constrained 2,4-Diamino-5,6-disubstituted Pyrimidines: A New Class of Histamine H4 Receptor Antagonists with Improved Druglikeness and in Vivo Efficacy in Pain and Inflammation Models

Journal of medicinal chemistry, 2008-10, Vol.51 (20), p.6547-6557

2008

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Structure−Activity Studies on a Series of a 2-Aminopyrimidine-Containing Histamine H4 Receptor Ligands

Journal of medicinal chemistry, 2008-10, Vol.51 (20), p.6571-6580

2008

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Antinociceptive effects of histamine H3 receptor antagonist in the preclinical models of pain in rats and the involvement of central noradrenergic systems

Brain research, 2010-10, Vol.1354, p.74-84

2010

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The Alkaloid Conessine and Analogues as Potent Histamine H3 Receptor Antagonists

Journal of medicinal chemistry, 2008-09, Vol.51 (17), p.5423-5430

2008

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Diaryldiamines with Dual Inhibition of the Histamine H3 Receptor and the Norepinephrine Transporter and the Efficacy of 4-(3-(Methylamino)-1-phenylpropyl)-6-(2-(pyrrolidin-1-yl)ethoxy)naphthalen-1-ol in Pain

Journal of medicinal chemistry, 2010-11, Vol.53 (21), p.7869-7873

2010

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Lack of efficacy of melanin-concentrating hormone-1 receptor antagonists in models of depression and anxiety

European journal of pharmacology, 2006-07, Vol.540 (1), p.115-120

2006

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In vitro studies on a class of quinoline containing histamine H3 antagonists

Bioorganic & medicinal chemistry letters, 2010-06, Vol.20 (11), p.3295-3300

2010

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In Vitro Preclinical Cardiac Assessment of Tolterodine and Terodiline: Multiple Factors Predict the Clinical Experience

Journal of cardiovascular pharmacology, 2006-11, Vol.48 (5), p.199-206

2006

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Synthesis, Potency, and In Vivo Profiles of Quinoline Containing Histamine H3 Receptor Inverse Agonists

Journal of medicinal chemistry, 2007-11, Vol.50 (22), p.5439-5448

2007

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Molecular recognition in aqueous media. Conformationally restricted water-soluble cyclophanes derived from 6H,12H-5,11-methanodibenzo[b,f][1,5]diazocine

Journal of the American Chemical Society, 1988-08, Vol.110 (18), p.6204-6210

1988

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Dopamine D4 Ligands and Models of Receptor Activation: 2-(4-Pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole and Related Heteroarylmethylarylpiperazines Exhibit a Substituent Effect Responsible for Additional Efficacy Tuning

Journal of medicinal chemistry, 2004-04, Vol.47 (9), p.2348-2355

2004

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In vitro Optimization of Structure Activity Relationships of Analogues of A‐331440 Combining Radioligand Receptor Binding Assays and Micronucleus Assays of Potential Antiobesity Histamine H3 Receptor Antagonists

Basic & clinical pharmacology & toxicology, 2004-09, Vol.95 (3), p.144-152

2004

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Adenosine kinase inhibitors: polar 7-Substitutent of pyridopyrimidine derivatives improving their locomotor selectivity

Bioorganic & medicinal chemistry letters, 2003-09, Vol.13 (18), p.3041-3044

2003

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Discovery of histamine H3 antagonists for the treatment of cognitive disorders and Alzheimer's disease

Pharmacological properties of ABT-239 [4-(2-{2-[(2R)-2-Methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile]: II. Neurophysiological characterization and broad preclinical efficacy in cognition and schizophrenia of a potent and selective histamine H3 receptor antagonist

An 80-amino acid deletion in the third intracellular loop of a naturally occurring human histamine H3 isoform confers pharmacological differences and constitutive activity

Structure–activity relationships of arylbenzofuran H3 receptor antagonists

Antagonism of supraspinal histamine H3 receptors modulates spinal neuronal activity in neuropathic rats

Design of a New Histamine H3 Receptor Antagonist Chemotype: (3aR,6aR)-5-Alkyl-1-aryl-octahydropyrrolo[3,4-b]pyrroles, Synthesis, and Structure−Activity Relationships

In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists : Trends across multiple chemical series

Synthesis and Pharmacology of (Pyridin-2-yl)methanol Derivatives as Novel and Selective Transient Receptor Potential Vanilloid 3 Antagonists

H4 receptor antagonism exhibits anti-nociceptive effects in inflammatory and neuropathic pain models in rats

Pharmacological properties and procognitive effects of ABT-288, a potent and selective histamine H3 receptor antagonist

Rotationally Constrained 2,4-Diamino-5,6-disubstituted Pyrimidines: A New Class of Histamine H4 Receptor Antagonists with Improved Druglikeness and in Vivo Efficacy in Pain and Inflammation Models

Structure−Activity Studies on a Series of a 2-Aminopyrimidine-Containing Histamine H4 Receptor Ligands

Antinociceptive effects of histamine H3 receptor antagonist in the preclinical models of pain in rats and the involvement of central noradrenergic systems

The Alkaloid Conessine and Analogues as Potent Histamine H3 Receptor Antagonists

Diaryldiamines with Dual Inhibition of the Histamine H3 Receptor and the Norepinephrine Transporter and the Efficacy of 4-(3-(Methylamino)-1-phenylpropyl)-6-(2-(pyrrolidin-1-yl)ethoxy)naphthalen-1-ol in Pain

Lack of efficacy of melanin-concentrating hormone-1 receptor antagonists in models of depression and anxiety

In vitro studies on a class of quinoline containing histamine H3 antagonists

In Vitro Preclinical Cardiac Assessment of Tolterodine and Terodiline: Multiple Factors Predict the Clinical Experience

Synthesis, Potency, and In Vivo Profiles of Quinoline Containing Histamine H3 Receptor Inverse Agonists

5-(3-Bromophenyl)-7-(6-morpholin-4-ylpyridin-3-yl)pyrido[2,3-d]pyrimidin-4-ylamine: structure–activity relationships of 7-substituted heteroaryl analogs as non-nucleoside adenosine kinase inhibitors

Discovery of 3-Methyl-N-(1-oxy-3‘,4‘,5‘,6‘-tetrahydro-2‘H-[2,4‘-bipyridine]-1‘-ylmethyl)benzamide (ABT-670), an Orally Bioavailable Dopamine D4 Agonist for the Treatment of Erectile Dysfunction

Molecular recognition in aqueous media. Conformationally restricted water-soluble cyclophanes derived from 6H,12H-5,11-methanodibenzo[b,f][1,5]diazocine

Dopamine D4 Ligands and Models of Receptor Activation: 2-(4-Pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole and Related Heteroarylmethylarylpiperazines Exhibit a Substituent Effect Responsible for Additional Efficacy Tuning

In vitro Optimization of Structure Activity Relationships of Analogues of A‐331440 Combining Radioligand Receptor Binding Assays and Micronucleus Assays of Potential Antiobesity Histamine H3 Receptor Antagonists

Adenosine kinase inhibitors: polar 7-Substitutent of pyridopyrimidine derivatives improving their locomotor selectivity

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