Výsledky vyhledávání - "Vliet, Bernard J."

Probing the cannabinoid CB1/CB2 receptor subtype selectivity limits of 1,2-diarylimidazole-4-carboxamides by fine-tuning their 5-substitution pattern

Autor: Vliet Bernard J Van, Josephus H. M. Lange, Herman H. van Stuivenberg, Chris G. Kruse, Alice J.M. Borst, Mahmut Selman Yildirim, Martina A.W. van der Neut

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 20:2770-2775

The cannabinoid CB(1)/CB(2) receptor subtype selectivity in the 1,2-diarylimidazole-4-carboxamide series was boosted by fine-tuning its 5-substitution pattern. The presence of the 5-methylsulfonyl group in 11 led to a greater than approximately 840-f

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1132e90c911a5e665c358a7347df54f7
https://doi.org/10.1016/j.bmcl.2010.03.068

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Synthesis, SAR and intramolecular hydrogen bonding pattern of 1,3,5-trisubstituted 4,5-dihydropyrazoles as potent cannabinoid CB1 receptor antagonists

Autor: Henri C. Wals, Arnold P. den Hartog, Herman H. van Stuivenberg, Vliet Bernard J Van, Martina A.W. van der Neut, Chris G. Kruse, Josephus H. M. Lange, Jan Hoogendoorn

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 20:1752-1757

The synthesis, structure–activity relationship (SAR) studies and intramolecular hydrogen bonding pattern of 1,3,5-trisubstituted 4,5-dihydropyrazoles are described. The target compounds 6–18 represent a novel class of potent and selective CB1 rec

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e2c90d51563f82391edda9612ecec016
https://doi.org/10.1016/j.bmcl.2010.01.049

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Adaptive changes in the number of Gs- and Gi-proteins underlie adenylyl cyclase sensitization in morphine-treated rat striatal neurons

Autor: Angélique L.C.T. Van Rijswijk, Arie H. Mulder, George Wardeh, Anton N. M. Schoffelmeer, Vliet Bernard J Van

Publikováno v: European Journal of Pharmacology: Molecular Pharmacology. 245:23-29

In the present study we investigated the possible role of changes in the number of membrane-bound G-proteins in the sensitization of dopamine D 1 receptor-stimulated adenylyl cyclase, observed in primary cultures of rat striatal neurons chronically e

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ab8ce50313991dfc3e66d2467380c7f6
https://doi.org/10.1016/0922-4106(93)90165-6

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ChemInform Abstract: Synthesis, SAR and Intramolecular Hydrogen Bonding Pattern of 1,3,5-Trisubstituted 4,5-Dihydropyrazoles as Potent Cannabinoid CB1 Receptor Antagonists

Autor: Vliet Bernard J Van, Josephus H. M. Lange, Arnold P. den Hartog, Henri C. Wals, Martina A.W. van der Neut, Jan Hoogendoorn, Herman H. van Stuivenberg, Chris G. Kruse

Publikováno v: ChemInform. 41

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::8449671cf6ec8952e4dd6753e60a5351
https://doi.org/10.1002/chin.201030125

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Two distinct classes of novel pyrazolinecarboxamides as potent cannabinoid CB1 receptor agonists

Autor: Hicham Zilaout, Hans van Aken, Henri C. Wals, Amos Attali, Arie H. Mulder, Martina A.W. van der Neut, Vliet Bernard J Van, Josephus H. M. Lange, Ate Duursma

Publikováno v: Bioorganicmedicinal chemistry letters. 20(17)

The synthesis and SAR of 3-alkyl-4-aryl-4,5-dihydropyrazole-1-carboxamides 1-23 and 1-alkyl-5-aryl-4,5-dihydropyrazole-3-carboxamides 24-27 as two novel cannabinoid CB(1) receptor agonist classes were described. The target compounds elicited high aff

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2a6d7054709649e3b5815449cde19c3f
https://pubmed.ncbi.nlm.nih.gov/20688519

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Cerebral blood volume alterations in the perilesional areas in the rat brain after traumatic brain injury--comparison with behavioral outcome

Autor: Amie L Phinney, Vliet Bernard J Van, Olli Gröhn, Taina-Kaisa Stenius, Juha Yrjänheikki, Taneli Heikkinen, Tinka Tuinstra, Antti Nurmi, Riikka Immonen, Leena Tähtivaara, Jukka Puoliväli

Publikováno v: Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism. 30(7)

In the traumatic brain injury (TBI) the initial impact causes both primary injury, and launches secondary injury cascades. One consequence, and a factor that may contribute to these secondary changes and functional outcome, is altered hemodynamics. T

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::225f74852b85b0e21c0ae6743628df84
https://pubmed.ncbi.nlm.nih.gov/20145657

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Synthesis and SAR of novel imidazoles as potent and selective cannabinoid CB2 receptor antagonists with high binding efficiencies

Autor: Henri C. Wals, Vliet Bernard J Van, Josephus H. M. Lange, Alice J.M. Borst, Hicham Zilaout, Gijs D. Kuil, Martina A.W. van der Neut, Herman H. van Stuivenberg, Arnold P. den Hartog, Arie T. Mulder, Wouter Goutier

Publikováno v: Bioorganicmedicinal chemistry letters. 20(3)

The synthesis and structure–activity relationship studies of imidazoles are described. The target compounds 6 – 20 represent a novel chemotype of potent and CB 2 /CB 1 selective cannabinoid CB 2 receptor antagonists/inverse agonists with very hig

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d05bca00ba102b73cff12dc1d1f7d3f9
https://pubmed.ncbi.nlm.nih.gov/20031412

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Effect of chronic prenatal morphine treatment on μ-opioid receptor-regulated adenylate cyclase activity and neurotransmitter release in rat brain slices

Autor: Vliet Bernard J Van, François Hogenboom, Anton N. M. Schoffelmeer, Taco J. De Vries, George Wardeh, Arie H. Mulder, Jan Willem Van der Laan

Publikováno v: De Vries, T J, Van Vliet, B J, Hogenboom, F, Wardeh, G, Van der Laan, J W, Mulder, A H & Schoffelmeer, A N M 1991, ' Effect of chronic prenatal morphine treatment on μ-opioid receptor-regulated adenylate cyclase activity and neurotransmitter release in rat brain slices ', European Journal of Pharmacology: Molecular Pharmacology, vol. 208, no. 2, pp. 97-104 . https://doi.org/10.1016/0922-4106(91)90059-Q
European Journal of Pharmacology: Molecular Pharmacology, 208(2), 97-104. Elsevier BV

Timed-pregnant ratsreceived a semisynthetic diet with or without morphine (0.5-1 mg/g) for 2 weeks. After 21 days of gestation the morphine-dependent dams were decapitated and the foetal brains were dissected. Chronic morphine administration caused a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a95b31be079fd2a8249158653368fb4f
http://www.scopus.com/inward/record.url?scp=0025949825&partnerID=8YFLogxK

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μ-Opioid receptor-regulated adenylate cyclase activity in primary cultures of rat striatal neurons upon chronic morphine exposure

Autor: Vliet Bernard J Van, Anton N. M. Schoffelmeer, Taco J. De Vries, George Wardeh, Arie H. Mulder

Publikováno v: Van Vliet, B J, De Vries, T J, Wardeh, G, Mulder, A H & Schoffelmeer, A N M 1991, ' μ-Opioid receptor-regulated adenylate cyclase activity in primary cultures of rat striatal neurons upon chronic morphine exposure ', European Journal of Pharmacology: Molecular Pharmacology, vol. 208, no. 2, pp. 105-111 . https://doi.org/10.1016/0922-4106(91)90060-U
European Journal of Pharmacology: Molecular Pharmacology, 208(2), 105-111. Elsevier BV

Rat striatal neurons cultured in serum-free, hormone-supplemented medium, were exposed to 10 μM morphine for several hours or days before intracellular cyclic AMP production was measured. Dopamine D1 receptor- and β-adrenoceptor-stimulated cyclic A

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::17b1e67c1e5668db6f544e09552e068a
https://doi.org/10.1016/0922-4106(91)90060-u

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