Search Results - "SCHOEFFTER, Philippe"
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Functional activity of the multiligand analog SOM230 at human recombinant somatostatin receptor subtypes supports its usefulness in neuroendocrine tumors
Published in Neuroendocrinology (2004)“…Functional gastroenteropancreatic tumors express all 5 somatostatin receptor subtypes (sst) in different quantities. Octreotide and lanreotide treat patients…”
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Differential inverse agonist efficacies of SB-258719, SB-258741 and SB-269970 at human recombinant serotonin 5-HT7 receptors
Published in European journal of pharmacology (14-07-2004)“…Recombinant 5-hydroxytryptamine 5-HT7 receptors are known to express constitutive, i.e., agonist-independent activity. Nonselective ligands, like methiothepin,…”
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NGD 94-1 as an agonist at human recombinant dopamine D4.4 receptors expressed in HEK293 cells
Published in European journal of pharmacology (21-05-1999)“…The atypical antipsychotic, clozapine has some selectivity for dopamine D4 receptors and is a silent antagonist at these receptors. NGD 94-1…”
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Functional expression of the serotonin 5‐HT 7 receptor in human glioblastoma cell lines
Published in British journal of pharmacology (17-02-2009)“…Serotonin 5‐HT 7 receptors are present in astrocytes. Understanding their role in this type of cell would greatly benefit from the identification of astroglial…”
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Decahydroisoquinoline derivatives as novel non-peptidic, potent and subtype-selective somatostatin sst(3) receptor antagonists
Published in Bioorganic & medicinal chemistry letters (01-03-2010)“…Starting from non-peptidic sst(1)-selective somatostatin receptor antagonists, first compounds with mixed sst(1)/sst(3) affinity were identified by directed…”
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Distinct functional properties of native somatostatin receptor subtype 5 compared with subtype 2 in the regulation of ACTH release by corticotroph tumor cells
Published in American journal of physiology: endocrinology and metabolism (01-08-2005)“…In a series of human corticotroph adenomas, we recently found predominant mRNA expression of somatostatin (SS) receptor subtype 5 (sst5). After 72 h, the…”
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Modulatory role of the vascular endothelium in the contractility of human isolated internal mammary artery
Published in British journal of pharmacology (01-10-1988)“…1 Endothelium‐dependent relaxant responses and modulation of contractile responses were investigated in human isolated internal mammary artery (HIMA), a vessel…”
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Pharmacological and endocrinological characterisation of stress-induced hyperthermia in singly housed mice using classical and candidate anxiolytics (LY314582, MPEP and NKP608)
Published in European journal of pharmacology (25-01-2002)“…The stress-induced hyperthermia test is a paradigm developed several years ago to model the expression of autonomic hyperactivity in anxiety. Whereas in the…”
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Discovery of novel non-peptidic beta-alanine piperazine amide derivatives and their optimization to achiral, easily accessible, potent and selective somatostatin sst1 receptor antagonists
Published in Bioorganic & medicinal chemistry letters (01-03-2009)“…Structural simplification of the core moieties of obeline and ergoline somatostatin sst(1) receptor antagonists, followed by systematic optimization, led to…”
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Serotonin 5-HT7 receptors coupled to induction of interleukin-6 in human microglial MC-3 cells
Published in Neuropharmacology (01-07-2005)“…Brain serotonin 5-HT(7) receptors are known to be expressed in neurons and astrocytes. We now report the presence of these receptors in a third type of cell,…”
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Decahydroisoquinoline derivatives as novel non-peptidic, potent and subtype-selective somatostatin sst sub(3) receptor antagonists
Published in Bioorganic & medicinal chemistry letters (01-03-2010)“…Starting from non-peptidic sst sub(1)-selective somatostatin receptor antagonists, first compounds with mixed sst sub(1)/sst sub(3) affinity were identified by…”
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13
Decahydroisoquinoline derivatives as novel non-peptidic, potent and subtype-selective somatostatin sst 3 receptor antagonists
Published in Bioorganic & medicinal chemistry letters (2010)“…Starting from non-peptidic sst 1-selective somatostatin receptor antagonists, first compounds with mixed sst 1/sst 3 affinity were identified by directed…”
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Functional characterization of the novel antipsychotic iloperidone at human D2, D3, α2C, 5-HT6, and 5-HT1A receptors
Published in Life sciences (1973) (18-07-2003)Get full text
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Ergoline derivatives as highly potent and selective antagonists at the somatostatin sst1 receptor
Published in Bioorganic & medicinal chemistry letters (01-02-2008)Get full text
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Toward Selective ERβ Agonists for Central Nervous System Disorders: Synthesis and Characterization of Aryl Benzthiophenes
Published in Journal of medicinal chemistry (28-03-2002)“…In an effort to identify selective ligands for the estrogen receptor subtype ERβ, a series of aryl benzthiophenes was synthesized. In a radioligand binding…”
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Functional characterisation of the putative somatostatin sst2 receptor antagonist CYN 154806
Published in Naunyn-Schmiedeberg's archives of pharmacology (01-01-2003)“…The two forms (DTyr8 and LTyr8) of the putative somatostatin sst2 receptor antagonist CYN 154806 (Ac-4NO2-Phe-c(DCys-Tyr-DTrp-Lys-Thr-Cys)-D/LTyr-NH2) were…”
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18
Discovery of novel non-peptidic β-alanine piperazine amide derivatives and their optimization to achiral, easily accessible, potent and selective somatostatin sst 1 receptor antagonists
Published in Bioorganic & medicinal chemistry letters (2009)“…Pharmacophore considerations based on obeline and ergoline somatostatin sst 1 receptor antagonists led to the design of an achiral β-alanine piperazine amide…”
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19
Functional expression of the serotonin 5‐HT7 receptor in human glioblastoma cell lines
Published in British journal of pharmacology (01-10-2004)“…Serotonin 5‐HT7 receptors are present in astrocytes. Understanding their role in this type of cell would greatly benefit from the identification of astroglial…”
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Journal Article -
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Age-related decrease of in vitro isoproterenol-induced cyclic AMP accumulation in rat aorta
Published in European journal of pharmacology (22-01-1982)“…Isoproterenol-induced accumulation of cyclic AMP was investigated in aorta rings from 7 to 18 weeks old rats. The effect of isoproterenol on cyclic AMP reached…”
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