Results 21 to 30 of about 5,591 (212)

Allosteric modulation of adenosine A1 and cannabinoid 1 receptor signaling by G‐peptides

Pharmacology Research & Perspectives, 2020
While allosteric modulation of GPCR signaling has gained prominence to address the need for receptor specificity, efforts have mainly focused on allosteric sites adjacent to the orthosteric ligand‐binding pocket and lipophilic molecules that target ...
Anja M. Touma, Rabia U. Malik, Tejas Gupte, Sivaraj Sivaramakrishnan   +3 more
doaj   +1 more source

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.
Saoirse Elizabeth O’Sullivan, Andrew S. Yates, Richard K. Porter   +2 more
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Modulation of Nicotinic Receptors by Cannabinoids

The FASEB Journal, 2018
The legalization of medicinal and recreational use of marijuana by many states in the USA, has resulted in an increase in its use. The two most abundant phytocannabinoids in marijuana Δ 9 ‐Tetrahydrocannabinol (THC) and cannabidiol (CBD) have been shown to have tremendous therapeutic ...
Carla Sofia Rodriguez‐Tirado, Jose Orlando Colon‐Saez, Jose Lasalde‐Dominicci   +2 more
openaire   +1 more source

Cannabinoid Receptor–Interacting Protein 1a Modulates CB1 Receptor Signaling and Regulation [PDF]

Molecular Pharmacology, 2015
Cannabinoid CB1 receptors (CB1Rs) mediate the presynaptic effects of endocannabinoids in the central nervous system (CNS) and most behavioral effects of exogenous cannabinoids. Cannabinoid receptor-interacting protein 1a (CRIP1a) binds to the CB1R C-terminus and can attenuate constitutive CB1R-mediated inhibition of Ca(2+) channel activity.
Smith, TH, Blume, LC, Straiker, A, Cox, JO, David, BG, Mcvoy, JRS, Sayers, KW, Poklis, JL, Abdullah, RA, Egertova, M, Chen, C-K, Mackie, K, Elphick, MR, Howlett, AC, Selley, DE   +14 more
openaire   +3 more sources

Targeting cannabinoid CB2 receptors in the Central Nervous System. Medicinal chemistry approaches with focus on neurodegenerative disorders

Frontiers in Neuroscience, 2016
Endocannabinoids activate two types of specific receptors, namely cannabinoid CB1 and CB2. Contrary to the psychotropic actions of agonists of CB1 receptors, and serious side effects of the selective antagonists of this receptor, drugs acting on CB2 ...
Gema Navarro, Paula Morales, Carmen Rodríguez-Cueto, Javier Fernández-Ruiz, Nadine Jagerovic, Rafael Franco   +5 more
doaj   +1 more source

Experimental Cannabinoid 2 Receptor-Mediated Immune Modulation in Sepsis [PDF]

Mediators of Inflammation, 2014
Sepsis is a complex condition that results from a dysregulated immune system in response to a systemic infection. Current treatments lack effectiveness in reducing the incidence and mortality associated with this disease. The endocannabinoid system offers great promise in managing sepsis pathogenesis due to its unique characteristics. The present study
J. Sardinha, M. E. M. Kelly, J. Zhou, C. Lehmann   +3 more
openaire   +3 more sources

Design, synthesis and biological evaluation of novel orthosteric-allosteric ligands of the cannabinoid receptor type 2 (CB2R)

Frontiers in Chemistry, 2022
It is well known that G protein–coupled receptors (GPCRs) assume multiple active states. Orthosteric ligands and/or allosteric modulators can preferentially stabilize specific conformations, giving rise to pathway-biased signaling.
Rebecca Ferrisi, Francesca Gado, Francesca Gado, Beatrice Polini, Caterina Ricardi, Kawthar A. Mohamed, Lesley A. Stevenson, Gabriella Ortore, Simona Rapposelli, Giuseppe Saccomanni, Roger G. Pertwee, Robert B. Laprairie, Robert B. Laprairie, Clementina Manera, Clementina Manera, Grazia Chiellini, Grazia Chiellini   +16 more
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The Endocannabinoid System and Oligodendrocytes in Health and Disease

Frontiers in Neuroscience, 2018
Cannabinoid-based interventions are being explored for central nervous system (CNS) pathologies such as neurodegeneration, demyelination, epilepsy, stroke, and trauma. As these disease states involve dysregulation of myelin integrity and/or remyelination,
Alexander A. Ilyasov, Alexander A. Ilyasov, Carolanne E. Milligan, Carolanne E. Milligan, Emily P. Pharr, Emily P. Pharr, Allyn C. Howlett, Allyn C. Howlett   +7 more
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The type 1 cannabinoid receptor positive allosteric modulators GAT591 and GAT593 reduce spike-and-wave discharges in Genetic Absence Epilepsy Rats from Strasbourg

IBRO Neuroscience Reports, 2022
Childhood absence epilepsy (CAE) is a non-convulsive seizure disorder primarily in children characterized by absence seizures. Absence seizures consist of 2.5–5 Hz spike-and-wave discharges (SWDs) detectable using electroencephalography (EEG).
Dan L. McElroy, Andrew J. Roebuck, Quentin Greba, Sumanta Garai, Asher L. Brandt, Orhan Yilmaz, Stuart M. Cain, Terrance P. Snutch, Ganesh A. Thakur, Robert B. Laprairie, John G. Howland   +10 more
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An Autonomous Cannabinoid System in Islets of Langerhans

Frontiers in Endocrinology, 2021
While endocannabinoids (ECs) and cannabis were primarily studied for their nervous system effects, it is now clear that ECs are also produced in the periphery where they regulate several physiological processes, including energy storage, glucose and ...
Kanikkai Raja Aseer, Josephine M. Egan
doaj   +1 more source