Results 21 to 30 of about 562,936 (248)

Discovery of Potent Dual PPARα Agonists/CB1 Ligands [PDF]

ACS Medicinal Chemistry Letters, 2011
This letter describes the synthesis and in vitro and in vivo evaluation of dual ligands targeting the cannabinoid and peroxisome proliferator-activated receptors (PPAR). These compounds were obtained from fusing the pharmacophores of fibrates and the diarylpyrazole rimonabant, a cannabinoid receptor antagonist.
Pérez-Fernández, Ruth, Fresno, Nieves, Macías-González, Manuel, Elguero, José, Decara, Juan, Girón, Rocío, Rodríguez-Álvarez, Ana, Martín, María Isabel, Rodríguez de Fonseca, Fernando, Goya, Pilar   +9 more
openaire   +3 more sources

Design, synthesis, and structure–activity relationship study of bicyclic piperazine analogs of indole-3-carboxamides as novel cannabinoid CB1 receptor agonists

Bioorganic and Medicinal Chemistry Letters, 2010
Mark York, Glenn Walker, Takao Kiyoi
exaly   +2 more sources

The Peripheral Cannabinoid Receptor Type 1 (CB1) as a Molecular Target for Modulating Body Weight in Man

Molecules, 2021
The cannabinoid 1 (CB1) receptor regulates appetite and body weight; however, unwanted central side effects of both agonists (in wasting disorders) or antagonists (in obesity and diabetes) have limited their therapeutic utility.
S. O'Sullivan, A. Yates, R. K. Porter
semanticscholar   +1 more source

Distinct activation mechanisms regulate subtype selectivity of Cannabinoid receptors

Communications Biology, 2023
Design of cannabinergic subtype selective ligands is challenging because of high sequence and structural similarities of cannabinoid receptors (CB1 and CB2).
Soumajit Dutta, Diwakar Shukla
doaj   +1 more source

Drug-Resistant Temporal Lobe Epilepsy Alters the Expression and Functional Coupling to Gαi/o Proteins of CB1 and CB2 Receptors in the Microvasculature of the Human Brain

Frontiers in Behavioral Neuroscience, 2021
Cannabinoid receptors 1 and 2 (CB1 and CB2, respectively) play an important role in maintaining the integrity of the blood–brain barrier (BBB). On the other hand, BBB dysfunction is a common feature in drug-resistant epilepsy.
María de los Ángeles Nuñez-Lumbreras, José Luis Castañeda-Cabral, María Guadalupe Valle-Dorado, Vicente Sánchez-Valle, Sandra Orozco-Suárez, Rosalinda Guevara-Guzmán, Iris Martínez-Juárez, Mario Alonso-Vanegas, Mario Alonso-Vanegas, Fruzsina Walter, Maria A. Deli, Francia Carmona-Cruz, Luisa Rocha   +12 more
doaj   +1 more source

Peripheral, but not central, CB1 antagonism provides food intake-independent metabolic benefits in diet-induced obese rats. [PDF]

, 2008
OBJECTIVE Blockade of the CB1 receptor is one of the promising strategies for the treatment of obesity. Although antagonists suppress food intake and reduce body weight, the role of central versus peripheral CB1 activation on weight loss and related ...
Nogueiras, Ruben, Klein, Marcella, Liposits, Zsolt, Tschöp, Matthias H., Watanabe, Masahiko, Rohner-Jeanrenaud, Francoise, Wittmann, Gábor, Veyrat-Durebex, Christelle, Tschöp, Johannes, Fekete, Csaba, Reizes, Ofer, Woods, Stephen C., Suchanek, Paula M., Caldwell, Charles   +13 more
core   +3 more sources

Characterization of Structurally Novel G Protein Biased CB1 Agonists: Implications for Drug Development

Pharmacological Research, 2017
&NA; The human cannabinoid subtype 1 receptor (hCB1R) is highly expressed in the CNS and serves as a therapeutic target for endogenous ligands as well as plant‐derived and synthetic cannabinoids.
Benjamin M. Ford, L. Franks, S. Tai, W. Fantegrossi, Edward L. Stahl, Michael D. Berquist, Christian V. Cabanlong, Catheryn D. Wilson, Narsimha R Penthala, P. Crooks, P. Prather   +10 more
semanticscholar   +1 more source

CB1 agonists, locally applied to the cortico-thalamic circuit of rats with genetic absence epilepsy, reduce epileptic manifestations.

Epilepsy Research, 2013
Drugs that modulate the endocannabinoid system and endocannabinoids typically play an anticonvulsant role although some proconvulsant effects have been reported both in humans and animal models.
R. Citraro, E. Russo, R. Ngomba, F. Nicoletti, F. Scicchitano, Benjamin J. Whalley, A. Calignano, G. Sarro   +7 more
semanticscholar   +1 more source

Unique agonist-bound cannabinoid CB1 receptor conformations indicate agonist specificity in signaling [PDF]

European Journal of Pharmacology, 2008
Cannabinoid drugs differ in their rank order of potency to produce analgesia versus other central nervous system effects. We propose that these differences are due to unique agonist-bound cannabinoid CB1 receptor conformations that exhibit different affinities for individual subsets of intracellular signal transduction pathways.
Teodora, Georgieva, Savitha, Devanathan, Dagmar, Stropova, Chad K, Park, Zdzislaw, Salamon, Gordon, Tollin, Victor J, Hruby, William R, Roeske, Henry I, Yamamura, Eva, Varga   +9 more
openaire   +2 more sources

Improved cyclobutyl nabilone analogs as potent CB1 receptor agonists

European Journal of Medicinal Chemistry, 2022
In earlier work, we explored the SAR for the C3 side chain pharmacophore in the hexahydrocannabinol template represented by the drug nabilone, which resulted in the development of AM2389. In an effort for further optimization, we have merged features of nabilone and AM2389 and explored the C3 side chain with varying chain lengths and terminal ...
Ioannis P. Papanastasiou, Markos-Orestis Georgiadis, Christos Iliopoulos-Tsoutsouvas, Carol A. Paronis, Christina A. Brust, Ngan K. Tran, Lipin Ji, Xiaoyu Ma, JodiAnne T. Wood, Nikolai Zvonok, Fei Tong, Laura M. Bohn, Spyros P. Nikas, Alexandros Makriyannis   +13 more
openaire   +3 more sources