Spiro-1-benzofuranpiperidinylalkanoic acids as a novel and selective sphingosine S1P5 receptor agonist chemotype

Autor: Axel Stoit, Sjoerd van Schaik, Josephus H. M. Lange, Annemieke Rensink, Adri van den Hoogenband, Chris G. Kruse, Hein K. A. C. Coolen, Arnold P. den Hartog

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 28:459-465

The synthesis and SAR of a novel class of spirobenzofuranpiperidinyl-derived alkanoic acids 6-34 as sphingosine S1P5 receptor agonists are described. The target compounds generally elicit high S1P5 receptor agonistic potencies and in general are sele

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::bd3ebf6ed30fa1e94992ef7801db2807
https://doi.org/10.1016/j.bmcl.2017.12.018

Optimization of N ′-(arylsulfonyl)pyrazoline-1-carboxamidines by exploiting a novel interaction site in the 5-HT 6 antagonistic binding pocket

Autor: Josephus H. M. Lange, Remco Henzen, Natasja de Bruin, Jelle de Vries, Wouter I. Iwema Bakker, Wouter de Looff, Arnold P. den Hartog, Stefan Verhoog, Rob P. van de Woestijne, Chris G. Kruse, Arnold van Loevezijn, Jennifer Venhorst, Martina A.W. van der Neut

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 26:1605-1611

The discovery of non-basic N'-(arylsulfonyl)pyrazoline-1-carboxamidines as 5-HT6 antagonists with unique structural features was recently disclosed. Here we describe how this structural class was further developed by addressing an unexplored interact

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9cf6abbf2099e90ec1e67445cecda377
https://doi.org/10.1016/j.bmcl.2016.02.001

SLV330, a cannabinoid CB1 receptor antagonist, attenuates ethanol and nicotine seeking and improves inhibitory response control in rats

Autor: Kruse Cornelis G, T.J. De Vries, Anton N. M. Schoffelmeer, Josephus H. M. Lange, Arnoldus H.J. Herremans, N.M.W.J. de Bruin, M. van Drimmelen

Publikováno v: de Bruin, N M W J, Lange, J H M, Kruse, C G, Herremans, A H, Schoffelmeer, A N M, van Drimmelen, M & de Vries, T J 2011, ' SLV330, a cannabinoid CB(1) receptor antagonist, attenuates ethanol and nicotine seeking and improves inhibitory response control in rats ', Behavioural Brain Research, vol. 217, no. 2, pp. 408-415 . https://doi.org/10.1016/j.bbr.2010.11.013
Behavioural Brain Research, 217(2), 408-415. Elsevier

Cannabinoid CB 1 receptor (CB 1 R) signaling has been shown to play a role in the regulation of addictive behavior. In the present study, our aim was to investigate whether the CB 1 R antagonist SLV330 could reduce ethanol and nicotine self-administr

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f5e67f975c3fd0653b0a29c8efea5e31
https://doi.org/10.1016/j.bbr.2010.11.013

SLV330, a cannabinoid CB1 receptor antagonist, ameliorates deficits in the T-maze, object recognition and Social Recognition Tasks in rodents

Autor: E. Hissink, Jos Prickaerts, Josephus H. M. Lange, L. Heijink, Kruse Cornelis G, J. Wijnen, M. van Drimmelen, E. Andriambeloson, M. de Haan, Sven Akkerman, N.M.W.J. de Bruin

Publikováno v: Neurobiology of Learning and Memory, 93(4), 522-531. Elsevier Science

Cannabinoid CB1 receptor (CB1R) signaling has been suggested to play an important role in the regulation of memory and cognition. In the present study, our aim was to investigate whether the CB1R antagonist SLV330 (doses ranging from 0.3 to 10 mg/kg,

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3e6ea0165c12f163d37fa7f5eb0bdac9
https://doi.org/10.1016/j.nlm.2010.01.010

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