Search Results - "DAZA, Anthony"
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Breast cancer cell-secreted miR-199b-5p hijacks neurometabolic coupling to promote brain metastasis
Published in Nature communications (29-05-2024)“…Breast cancer metastasis to the brain is a clinical challenge rising in prevalence. However, the underlying mechanisms, especially how cancer cells adapt a…”
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2
Indol-3-ylcycloalkyl Ketones: Effects of N1 Substituted Indole Side Chain Variations on CB2 Cannabinoid Receptor Activity
Published in Journal of medicinal chemistry (14-01-2010)“…Several 3-acylindoles with high affinity for the CB2 cannabinoid receptor and selectivity over the CB1 receptor have been prepared. A variety of 3-acyl…”
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3
Characterization of a cannabinoid CB2 receptor-selective agonist, A-836339 [2,2,3,3-tetramethyl-cyclopropanecarboxylic acid [3-(2-methoxy-ethyl)-4,5-dimethyl-3H-thiazol-(2Z)-ylidene]-amide], using in vitro pharmacological assays, in vivo pain models, and pharmacological magnetic resonance imaging
Published in The Journal of pharmacology and experimental therapeutics (01-01-2009)“…Studies demonstrating the antihyperalgesic and antiallodynic effects of cannabinoid CB(2) receptor activation have been largely derived from the use of…”
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4
Indol-3-yl-tetramethylcyclopropyl Ketones: Effects of Indole Ring Substitution on CB2 Cannabinoid Receptor Activity
Published in Journal of medicinal chemistry (27-03-2008)“…A series of potent indol-3-yl-tetramethylcyclopropyl ketones have been prepared as CB2 cannabinoid receptor ligands. Two unsubstituted indoles (5, 32) were the…”
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5
Spontaneous phasic activity of the pig urinary bladder smooth muscle: characteristics and sensitivity to potassium channel modulators
Published in British journal of pharmacology (01-02-2002)“…A hallmark for unstable bladder contractions is hyperexcitability and changes in the nature of spontaneous phasic activity of the bladder smooth muscle. In…”
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6
Synthesis and evaluation of 2-amido-3-carboxamide thiophene CB2 receptor agonists for pain management
Published in Bioorganic & medicinal chemistry letters (01-04-2012)“…SAR studies on a series of thiophene amide derivatives provided CB2 receptor agonists. The activity of the compounds was characterized by radioligand binding…”
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7
Characterization of human cannabinoid CB2 receptor coupled to chimeric Gαqi5 and Gαqo5 proteins
Published in European journal of pharmacology (28-01-2009)Get full text
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8
Effects of Substitution on 9-(3-Bromo-4-fluorophenyl)-5,9-dihydro-3H,4H-2,6-dioxa-4- azacyclopenta[b]naphthalene-1,8-dione, a Dihydropyridine ATP-Sensitive Potassium Channel Opener
Published in Journal of medicinal chemistry (16-11-2006)“…Structure−activity relationships were investigated on the tricyclic dihydropyridine (DHP) KATP openers…”
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9
Functional characterization of large conductance calcium-activated K+ channel openers in bladder and vascular smooth muscle
Published in Naunyn-Schmiedeberg's archives of pharmacology (01-05-2004)“…Calcium activated K(+) channels (K(Ca) channels) are found in a variety of smooth muscle tissues, the most characterized of which are the large conductance…”
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10
Synthesis and Structure−Activity Relationships of a Novel Series of Tricyclic Dihydropyridine-Based KATP Openers That Potently Inhibit Bladder Contractions in Vitro
Published in Journal of medicinal chemistry (03-06-2004)“…Structure−activity relationships were investigated on a novel series of tricyclic dihydropyridine-containing KATP openers. This diverse group of analogues,…”
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11
(-)-(9S)-9-(3-Bromo-4-fluorophenyl)-2,3,5,6,7,9-hexahydrothieno[3,2-b]quinolin-8(4H)-one 1,1-dioxide (A-278637): a novel ATP-sensitive potassium channel opener efficacious in suppressing urinary bladder contractions. I. In vitro characterization
Published in The Journal of pharmacology and experimental therapeutics (01-10-2002)“…Alterations in the myogenic activity of the bladder smooth muscle are thought to serve as a basis for the involuntary detrusor contractions associated with the…”
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12
Pharmacological and molecular analysis of ATP-sensitive K + channels in the pig and human detrusor
Published in European journal of pharmacology (21-07-2000)“…The pharmacological and molecular properties of ATP-sensitive K + channels present in pig detrusor smooth muscle were investigated. In isolated pig detrusor…”
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13
ABT-866, a novel α1A-adrenoceptor agonist with antagonist properties at the α1B- and α1D-adrenoceptor subtypes
Published in European journal of pharmacology (02-08-2002)“…N-[3-(1H-Imidazol-4-ylmethyl)phenyl]ethanesulfonamide, maleate (ABT-866) is a novel α1-adrenoceptor agent with mixed pharmacological properties in vitro…”
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14
Synthesis and Structure−Activity Studies on N-[5-(1H-Imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an Imidazole-Containing α1A-Adrenoceptor Agonist
Published in Journal of medicinal chemistry (03-06-2004)“…Structure−activity studies were performed on the α1A-adrenoceptor (AR) selective agonist…”
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15
In vitro and in vivo characterization of a novel naphthylamide ATP‐sensitive K+ channel opener, A‐151892
Published in British journal of pharmacology (01-09-2004)“…Openers of ATP‐sensitive K+ channels are of interest in several therapeutic indications including overactive bladder and other lower urinary tract disorders…”
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N-[3-(1H-Imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1), a Novel α1-Adrenoceptor Ligand with an Enhanced in Vitro and in Vivo Profile Relative to Phenylpropanolamine and Midodrine
Published in Journal of medicinal chemistry (26-09-2002)“…N-[3-(1H-Imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1) is a novel α1 agent having the unique profile of α1A (rabbit urethra, EC50 = 0.60 μM)…”
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17
Structure–activity relationship of a novel class of naphthyl amide KATP channel openers
Published in Bioorganic & medicinal chemistry letters (19-05-2003)“…We have discovered a novel series of N-[2-(2,2,2-trifluoro-1-hydroxy-1-trifluoromethyl-ethyl)-naphthalen-1-yl] amides that are potent openers of K ATP channels…”
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18
Synthesis and Structure−Activity Relationships of a Novel Series of 2,3,5,6,7,9-Hexahydrothieno[3,2-b]quinolin-8(4H)-one 1,1-Dioxide KATP Channel Openers: Discovery of (−)-(9S)-9-(3-Bromo-4-fluorophenyl)-2,3,5,6,7,9- hexahydrothieno[3,2-b]quinolin-8(4H)-one 1,1-Dioxide (A-278637), a Potent KATP Opener That Selectively Inhibits Spontaneous Bladder Contractions
Published in Journal of medicinal chemistry (03-06-2004)“…Structure−activity relationships were investigated on a novel series of sulfonyldihydropyridine-containing KATP openers. Ring sizes, absolute stereochemistry,…”
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19
Species comparison and pharmacological characterization of rat and human CB 2 cannabinoid receptors
Published in European journal of pharmacology (28-11-2004)“…Pharmacological effects of cannabinoid ligands are thought to be mediated through cannabinoid CB 1 and CB 2 receptor subtypes. Sequence analysis revealed that…”
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20
Species comparison and pharmacological characterization of rat and human CB2 cannabinoid receptors
Published in European journal of pharmacology (28-11-2004)“…Pharmacological effects of cannabinoid ligands are thought to be mediated through cannabinoid CB1 and CB2 receptor subtypes. Sequence analysis revealed that…”
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