Results 31 to 40 of about 205,233 (331)

Cannabigerol Action at Cannabinoid CB1 and CB2 Receptors and at CB1–CB2 Heteroreceptor Complexes

Frontiers in Pharmacology, 2018
Cannabigerol (CBG) is one of the major phytocannabinoids present in Cannabis sativa L. that is attracting pharmacological interest because it is non-psychotropic and is abundant in some industrial hemp varieties.
Gemma Navarro, Gemma Navarro, Katia Varani, Irene Reyes-Resina, Irene Reyes-Resina, Verónica Sánchez de Medina, Rafael Rivas-Santisteban, Rafael Rivas-Santisteban, Carolina Sánchez-Carnerero Callado, Fabrizio Vincenzi, Salvatore Casano, Carlos Ferreiro-Vera, Enric I. Canela, Enric I. Canela, Pier Andrea Borea, Xavier Nadal, Rafael Franco, Rafael Franco   +17 more
doaj   +1 more source

Synthesis, biological evaluation, and SAR studies of 14β-phenylacetyl substituted 17-cyclopropylmethyl-7, 8-dihydronoroxymorphinones derivatives : Ligands with mixed NOP and opioid receptor profile [PDF]

, 2018
© 2018 Kumar, Polgar, Cami-Kobeci, Thomas, Khroyan, Toll and Husbands.A series of 14β-acyl substituted 17-cyclopropylmethyl-7,8-dihydronoroxymorphinone compounds has been synthesized and evaluated for affinity and efficacy for mu (MOP), kappa (KOP), and ...
Cami-Kobeci, Champion, Cheng, Christoph, Ding, Dooley, Greedy, Greiner, Gumusel, Günther, Hu, Huang, Jenck, Khroyan, Khroyan, Kiguchi, Ko, Lewis, Lewis, Lia, Manabe, Meunier, Meunier, Mogil, Mollereau, Moynihan, Pomonis, Raffa, Reinsceid, Rizzi, Rossi, Saccone, Sandin, Schmidhammer, Schmidhammer, Schmidhammer, Spagnolo, Sukhtankar, Thompson, Toll, Toll, Traynor, Ueda, Vanderah, Váradi, Woodcock, Yu, Zeilhofer   +47 more
core   +4 more sources

Partial agonists in schizophrenia [PDF]

British Journal of Psychiatry, 2005
The editorial by Bolonna & Kerwin ([2005][1]) is both timely and important. The authors succinctly present the case for the use of partial agonists of dopamine receptors, concluding that ‘the reviewed evidence suggests a promising future for dopamine receptor partial agonists’.
D. A. Cousins, A. H. Young
openaire   +1 more source

The “C3aR Antagonist” SB290157 is a Partial C5aR2 Agonist

Frontiers in Pharmacology, 2021
Innate immune complement activation generates the C3 and C5 protein cleavage products C3a and C5a, defined classically as anaphylatoxins. C3a activates C3aR, while C5a activates two receptors (C5aR1 and C5aR2) to exert their immunomodulatory activities ...
Xaria X. Li, Vinod Kumar, Richard J. Clark, John D. Lee, Trent M. Woodruff   +4 more
doaj   +1 more source

Transdiagnostic Efficacy of Cariprazine: A Systematic Review and Meta-Analysis of Efficacy Across Ten Symptom Domains

Pharmaceuticals
Introduction: The introduction of the transdiagnostic approach in psychiatry shifts the focus from discrete diagnoses to shared symptoms across various disorders.
Agota Barabassy, Réka Csehi, Zsófia Borbála Dombi, Balázs Szatmári, Thomas Brevig, György Németh   +5 more
doaj   +1 more source

Bitopic binding mode of an M1 muscarinic acetylcholine receptor agonist associated with adverse clinical trial outcomes [PDF]

, 2018
The realisation of the therapeutic potential of targeting the M1 muscarinic acetylcholine receptor (M1 mAChR) for the treatment of cognitive decline in Alzheimer's disease has prompted the discovery of M1 mAChR ligands showing efficacy in alleviating ...
Bradley, Sophie J., Broad, Lisa M., Brooke, Simon M., Bundgaard, Christoffer, Christopoulos, Arthur, Crabtree, Michael D., Dwomoh, Louis, Felder, Christian C., Langmead, Christopher J., Mogg, Adrian J., Molloy, Colin, Sanger, Helen E., Sexton, Patrick M., Thompson, Karen J., Tobin, Andrew B.   +14 more
core   +1 more source

Terguride stimulates locomotor activity at 2 months but not 10 months after 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine treatment of common marmosets [PDF]

, 1992
The mixed dopamine (DA) agonist/antagonist terguride acts as a DA antagonist on normosensitive receptors but shows DA agonistic properties at supersensitive DA receptors.
Horowski, R., Jenner, P., Jähnig, P., Lange, Klaus W., Löschmann, P. A., Marsden, C. D., Wachtel, H.   +6 more
core   +1 more source

The efficiency of CD4 recruitment to ligand-engaged TCR controls the agonist/partial agonist properties of peptide-MHC molecule ligands. [PDF]

, 1997
One hypothesis seeking to explain the signaling and biological properties of T cell receptor for antigen (TCR) partial agonists and antagonists is the coreceptor density/kinetic model, which proposes that the pharmacologic behavior of a TCR ligand is ...
Bluestone, JA, Chau, LA, Germain, RN, Madrenas, J, Smith, J   +4 more
core  

The novel mu-opioid antagonist, GSK1521498, reduces ethanol consumption in C57BL/6J mice. [PDF]

, 2015
RATIONALE Using the drinking-in-the-dark (DID) model, we compared the effects of a novel mu-opioid receptor antagonist, GSK1521498, with naltrexone, a licensed treatment of alcohol dependence, on ethanol consumption in mice.
C Giuliano, C Giuliano, David N. Stephens, David R. Wille, DM Ignar, DN Stephens, DW Oslin, EA Rabiner, Edward T. Bullmore, EE Codd, F Kiefer, GH Jones, H Wit de, H Ziauddeen, HM Pettinati, JR Volpicelli, JS Rhodes, Kay Maltby, LA Berner, LA Parker, LD Middaugh, LS Hwa, Manolo Mugnaini, NK Kamdar, P Monti, PJ Nathan, PJ Nathan, Pradeep Nathan, S Loeber, Sam R. Miller, Sandra Sanchez-Roige, Tamzin L. Ripley, TJ Phillips, TL Ripley   +33 more
core   +1 more source

Predicting Chronicity in Children and Adolescents With Newly Diagnosed Immune Thrombocytopenia at the Timepoint of Diagnosis Using Machine Learning‐Based Approaches

Pediatric Blood &Cancer, EarlyView.
ABSTRACT Objectives To identify predictors of chronic ITP (cITP) and to develop a model based on several machine learning (ML) methods to estimate the individual risk of chronicity at the timepoint of diagnosis. Methods We analyzed a longitudinal cohort of 944 children enrolled in the Intercontinental Cooperative immune thrombocytopenia (ITP) Study ...
Severin Kasser, Alice Bizeul, Meera Chitlur, Hugo Donato, Jelena Roganovic, Julia E. Vogt, Thomas Kühne   +6 more
wiley   +1 more source