Výsledky vyhledávání - "M C Dubroeucq"

RP 73870, a gastrin/cholecystokinin-B receptor antagonist with potent anti-ulcer activity in the rat

Autor: C E, Pendley, L R, Fitzpatrick, A J, Capolino, M A, Davis, N J, Esterline, A, Jakubowska, P, Bertrand, C, Guyon, M C, Dubroeucq, G E, Martin

Publikováno v: The Journal of pharmacology and experimental therapeutics. 273(3)

RP 73870, the racemic potassium salt of (([N-(methoxy-3-phenyl)-N-(N-methyl-N-phenyl-carbamoylmethyl)- carbamoylmethyl]-3-ureido)-3-phenyl)-2-ethylsulfonate-(RS) is a potent, reversible antagonist of both gastrin and cholecystokinin-B receptors in gu

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::b3775b9c7be3e124aabe47d711048fbc
https://pubmed.ncbi.nlm.nih.gov/7791071

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Estimation of brain penetration of CCKB receptor antagonists by an ex-vivo binding assay

Autor: S. Dreisler, Bernadette Jeantaud, M. C. Dubroeucq, P. Lopez, A. Doble, Philippe Bertrand, C. Guyon

Publikováno v: Neuropeptides. 24:223

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::9be594c4271db7b5d9fd20906d597056
https://doi.org/10.1016/0143-4179(93)90217-x

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Peripheral benzodiazepine binding sites: effect of PK 11195, 1-(2-chlorophenyl)-N-methyl-N-(1-methylpropyl)-3-isoquinolinecarboxamide. I. In vitro studies

Autor: G, Le Fur, M L, Perrier, N, Vaucher, F, Imbault, A, Flamier, J, Benavides, A, Uzan, C, Renault, M C, Dubroeucq, C, Guérémy

Publikováno v: Life sciences. 32(16)

[3H] RO5-4864 binding sites have been characterized in kidney, heart, brain, adrenals and platelets in the rat. In all these organs the following order of potency in the RO5-4864 displacement was found: RO5-4864 greater than diazepam greater than clo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::e06f057459e39f55a13b6697c9c423de
https://pubmed.ncbi.nlm.nih.gov/6300588

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The 5-hydroxytryptamine-releasing properties of two epimer quinoline derivatives

Autor: G, Le Fur, F, Imbault, N, Mitrani, F, Marquis, C, Renault, M C, Dubroeucq, C, Gueremy, A, Uzan

Publikováno v: Neuropharmacology. 23(2A)

Two epimer quinoline derivatives, PK 5078 and PK 7059, have been shown to be potent at releasing 5-HT from blood platelets. Moreover PK 5078 was also a potent and selective inhibitor of the uptake of 5-HT, being about 20 times as active as clomiprami

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::ee6b0a4d1ec2e3d03f0ca62e456afd0c
https://pubmed.ncbi.nlm.nih.gov/6717757

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'Peripheral type' benzodiazepine binding sites in rat adrenals: binding studies with [3H]PK 11195 and autoradiographic localization

Autor: J, Benavides, C, Malgouris, F, Imbault, F, Begassat, A, Uzan, C, Renault, M C, Dubroeucq, C, Gueremy, G, Le Fur

Publikováno v: Archives internationales de pharmacodynamie et de therapie. 266(1)

PK 11195 [1-(2-chlorophenyl)-N-methyl-N-(1-methylpropyl)-3-isoquinolinec arboxamide] is a compound chemically unrelated to benzodiazepines with a high affinity for the "peripheral type" binding sites for benzodiazepines (Le Fur et al., 1983a). [3H]PK

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::54d38e9e181f064cd2cd3a115b05794a
https://pubmed.ncbi.nlm.nih.gov/6667063

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Peripheral benzodiazepine binding sites: effect of PK 11195, 1-(2-chlorophenyl)-N-methyl-(1-methylpropyl)-3 isoquinolinecarboxamide. II. In vivo studies

Autor: G, Le Fur, F, Guilloux, P, Rufat, J, Benavides, A, Uzan, C, Renault, M C, Dubroeucq, C, Guérémy

Publikováno v: Life sciences. 32(16)

Peripheral type of benzodiazepine binding sites were labelled in the kidney, the heart and the brain with [3H] RO5-4864 following intravenous injection in mice. The regional distribution of this in vivo binding parallels the in vitro binding: heart a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::d35c9a86d80c65a875c611079379920c
https://pubmed.ncbi.nlm.nih.gov/6300589

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Histidine modification with diethylpyrocarbonate induces a decrease in the binding of an antagonist, PK 11195, but not of an agonist, RO5-4864, of the peripheral benzodiazepine receptors

Autor: J, Bénavidès, F, Begassat, T, Phan, C, Tur, A, Uzan, C, Renault, M C, Dubroeucq, C, Guérémy, G, Le Fur

Publikováno v: Life sciences. 35(12)

[3H]PK 11195 binding to peripheral type benzodiazepine binding sites in kidney membranes is inhibited by the histidine blocking agent diethylpyrocarbonate. This reagent irreversibly decreases the Bmax for [3H]PK 11195 without affecting the affinity.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::bdeb0dca22491efe40004bf63d6af597
https://pubmed.ncbi.nlm.nih.gov/6090832

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Pharmacology of peripheral type benzodiazepine receptors in the heart

Autor: G, Le Fur, M, Mestre, T, Carriot, C, Belin, C, Renault, M C, Dubroeucq, C, Guérémy, A, Uzan

Publikováno v: Progress in clinical and biological research. 192

RO5-4864 decreased in a dose-dependent manner the duration of intra cellular action potential and the contractility in the guinea pig papillary muscle. Diazepam was less active and clonazepam inactive. The effects of RO5-4864 were blocked by PK 11195

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::4bf08d24aa00e8d5e97d1636103dd14b
https://pubmed.ncbi.nlm.nih.gov/3001750

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