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Central nervous system drug disposition: the relationship between in situ brain permeability and brain free fraction

The Journal of pharmacology and experimental therapeutics, 2007-07, Vol.322 (1), p.205-213

2007

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Receptor occupancy and brain free fraction

Drug metabolism and disposition, 2009-04, Vol.37 (4), p.753-760

2009

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Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders

Bioorganic & medicinal chemistry letters, 2011-09, Vol.21 (18), p.5562-5567

2011

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Pharmacological characterisation of the GlyT-1 glycine transporter using two novel radioligands

Neuropharmacology, 2010-11, Vol.59 (6), p.558-565

2010

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Characterisation of the binding of [3H]‐SB‐674042, a novel nonpeptide antagonist, to the human orexin‐1 receptor

British journal of pharmacology, 2004-01, Vol.141 (2), p.340-346

2004

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Glycine transporter 1 (GlyT1) inhibitors exhibit anticonvulsant properties in the rat maximal electroshock threshold (MEST) test

Brain research, 2010-05, Vol.1331, p.105-113

2010

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Orexin A Activates Locus Coeruleus Cell Firing and Increases Arousal in the Rat

Proceedings of the National Academy of Sciences - PNAS, 1999-09, Vol.96 (19), p.10911-10916

1999

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Evidence that orexin-A-evoked grooming in the rat is mediated by orexin-1 (OX1) receptors, with downstream 5-HT2C receptor involvement

Psychopharmacologia, 2001-01, Vol.153 (2), p.203-209

2001

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Effects of centrally administered orexin-B and orexin-A: a role for orexin-1 receptors in orexin-B-induced hyperactivity

Psychopharmacologia, 2001-01, Vol.153 (2), p.210-218

2001

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Amyloid β synaptotoxicity is Wnt-PCP dependent and blocked by fasudil

Alzheimer's & dementia, 2018-03, Vol.14 (3), p.306-317

2018

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Abstract 4135: Novel dual A2A A2B adenosine receptor antagonists for cancer immunotherapy: in vitro and in vivo characterization

Cancer research (Chicago, Ill.), 2019-07, Vol.79 (13_Supplement), p.4135-4135

2019

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Stereocontrolled Formation of Epoxy Peroxide FunctionalityAppended to a Lactam Ring

Journal of organic chemistry, 2001-07, Vol.66 (14), p.4771-4775

2001

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Construction of functionalised medium rings by stereospecific expansions of 2,3-epoxy alcohols under mild conditions

Tetrahedron letters, 2002-09, Vol.43 (37), p.6637-6640

2002

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N-1 substituted pyrimidin-4-ones: Novel, orally active inhibitors of lipoprotein-associated phospholipase A2

Bioorganic & medicinal chemistry letters, 2000-11, Vol.10 (22), p.2557-2561

2000

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New quinoline NK3 receptor antagonists with CNS activity

Bioorganic & medicinal chemistry letters, 2009-02, Vol.19 (3), p.837-840

2009

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Design and discovery of 3-aryl-5-substituted-isoquinolin-1-ones as potent tankyrase inhibitors

MedChemComm, 2015-01, Vol.6 (9), p.1687-1692

2015

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Design and discovery of 3-aryl-5-substituted-isoquinolin-1-ones as potent tankyrase inhibitorsElectronic supplementary information (ESI) available: For complete experimental details for the TNKS homology model generation and virtual screen, chemical synthesis, biological assays and X-ray crystallography see ESI. The PDB accession codes for the X-ray co-crystal structure of TNKS + 12, TNKS + 21 and TNKS + 23 are 4UW1, 4U6A and 4UUH, respectively. See DOI: 10.1039/c5md00210a

2015-09

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New quinoline NK 3 receptor antagonists with CNS activity

Bioorganic & medicinal chemistry letters, 2009, Vol.19 (3), p.837-840

2009

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Orexin receptors in GtoPdb v.2023.1

IUPHAR/BPS Guide to Pharmacology CITE, 2023-04, Vol.2023 (1)

2023

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Orexin receptors in GtoPdb v.2021.3

IUPHAR/BPS Guide to Pharmacology CITE, 2021-01, Vol.2021 (3)

2021

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Orexin receptors (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database

IUPHAR/BPS Guide to Pharmacology CITE, 2019-09, Vol.2019 (4)

2019

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SYNTHESIS OF EXOCYCLIC ENAMIDES VIA STEREOCONTROLLED ALLYLIC ISOMERIZATION AND 1,3-TRANSPOSITION

Synthetic communications, 2001-01, Vol.31 (11), p.1753-1764

2001

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Evidence that orexin-A-evoked grooming in the rat is mediated by orexin-1 (OX 1 ) receptors, with downstream 5-HT 2C receptor involvement

Psychopharmacology, 2001-01, Vol.153 (2), p.203-209

2001

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Tin (IV)-Mediated Stereoselective Synthesis of Epoxides with Concomitant Alkyl Peroxide Formation

Tetrahedron letters, 1995-08, Vol.36 (33), p.5979-5982

Hursthouse, M

1995

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N-1 substituted pyrimidin-4-ones: novel, orally active inhibitors of lipoprotein-associated phospholipase A 2

Bioorganic & medicinal chemistry letters, 2000, Vol.10 (22), p.2557-2561

2000

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Central nervous system drug disposition: the relationship between in situ brain permeability and brain free fraction

Receptor occupancy and brain free fraction

Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders

Pharmacological characterisation of the GlyT-1 glycine transporter using two novel radioligands

Characterisation of the binding of [3H]‐SB‐674042, a novel nonpeptide antagonist, to the human orexin‐1 receptor

Glycine transporter 1 (GlyT1) inhibitors exhibit anticonvulsant properties in the rat maximal electroshock threshold (MEST) test

Orexin A Activates Locus Coeruleus Cell Firing and Increases Arousal in the Rat

Evidence that orexin-A-evoked grooming in the rat is mediated by orexin-1 (OX1) receptors, with downstream 5-HT2C receptor involvement

Effects of centrally administered orexin-B and orexin-A: a role for orexin-1 receptors in orexin-B-induced hyperactivity

Amyloid β synaptotoxicity is Wnt-PCP dependent and blocked by fasudil

Abstract 4135: Novel dual A2A A2B adenosine receptor antagonists for cancer immunotherapy: in vitro and in vivo characterization

Stereocontrolled Formation of Epoxy Peroxide FunctionalityAppended to a Lactam Ring

Construction of functionalised medium rings by stereospecific expansions of 2,3-epoxy alcohols under mild conditions

N-1 substituted pyrimidin-4-ones: Novel, orally active inhibitors of lipoprotein-associated phospholipase A2

New quinoline NK3 receptor antagonists with CNS activity

Design and discovery of 3-aryl-5-substituted-isoquinolin-1-ones as potent tankyrase inhibitors

New quinoline NK 3 receptor antagonists with CNS activity

Orexin receptors in GtoPdb v.2023.1

Orexin receptors in GtoPdb v.2021.3

Orexin receptors (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database

SYNTHESIS OF EXOCYCLIC ENAMIDES VIA STEREOCONTROLLED ALLYLIC ISOMERIZATION AND 1,3-TRANSPOSITION

Evidence that orexin-A-evoked grooming in the rat is mediated by orexin-1 (OX 1 ) receptors, with downstream 5-HT 2C receptor involvement

Tin (IV)-Mediated Stereoselective Synthesis of Epoxides with Concomitant Alkyl Peroxide Formation

N-1 substituted pyrimidin-4-ones: novel, orally active inhibitors of lipoprotein-associated phospholipase A 2

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