Results 211 to 220 of about 6,065 (241)

Modulation of transmitter release via presynaptic cannabinoid receptors

Trends in Pharmacological Sciences, 2001
Cannabis (marijuana) is not only a frequently abused drug but also has the potential for the development of useful agents for the treatment of emesis, anorexia and multiple sclerosis. In this article, the effects of modulation of transmitter release by cannabinoids in both the CNS and the PNS of various species, including humans, will be discussed ...
E, Schlicker, M, Kathmann
openaire   +2 more sources

Translational potential of allosteric modulators targeting the cannabinoid CB1 receptor [PDF]

Acta Pharmacologica Sinica, 2018
The cannabinoid type-1 (CB1) receptor, a G-protein-coupled receptor, is an attractive target for drug discovery due to its involvement in many physiological processes. Historically, drug discovery efforts targeting the CB1 receptor have focused on the development of orthosteric ligands that interact with the active site to which endogenous cannabinoids
Dai Lu, Sri Sujana Immadi, Zhixing Wu
exaly   +3 more sources

Modulation of Glycine Receptor Function by the Synthetic Cannabinoid HU210

Pharmacology, 2009
Loss of inhibitory synaptic transmission within the dorsal horn of the spinal cord plays a key role in the development of chronic pain following inflammation or nerve injury. Inhibitory postsynaptic transmission in the adult spinal cord involves mainly glycine. HU210 is a non-psychotropic, synthetic cannabinoid.
Reyhan, Demir, Martin, Leuwer, Jeanne, de la Roche, Klaus, Krampfl, Nilufar, Foadi, Matthias, Karst, Reinhard, Dengler, Gertrud, Haeseler, Jörg, Ahrens   +8 more
openaire   +2 more sources

C-3 Amido-Indole cannabinoid receptor modulators

Bioorganic & Medicinal Chemistry Letters, 2002
C-3 Amido-indoles were found to selectively bind to the CB2 receptor. SAR studies led to optimized compounds with excellent in vivo potency against LPS induced TNF-alpha release in murine models of cytokine production.
John, Hynes, Katerina, Leftheris, Hong, Wu, Chennagiri, Pandit, Ping, Chen, Derek J, Norris, Bang-Chi, Chen, Rulin, Zhao, Peter A, Kiener, Xiaorong, Chen, Lori A, Turk, Vina, Patil-Koota, Kathleen M, Gillooly, David J, Shuster, Kim W, McIntyre   +14 more
openaire   +2 more sources

Development of indole sulfonamides as cannabinoid receptor negative allosteric modulators [PDF]

Bioorganic and Medicinal Chemistry Letters, 2016
Les modulateurs allostériques négatifs (MNA) CB1 existants appartiennent à une gamme limitée de classes structurelles. Malgré le potentiel théorique des NAM CB1, les études in vivo publiées n'ont généralement pas été en mesure de démontrer les effets thérapeutiques attendus médiés par CB1.
Iain R Greig, Laurent Trembleau
exaly   +4 more sources

Modulation of rat brain opioid receptors by cannabinoids.

The Journal of Pharmacology and Experimental Therapeutics, 1987
The interaction of delta 9-tetrahydrocannabinol (delta 9-THC) and related cannabinoids with opioid receptors of neuronal membranes has been investigated. Treatment of membranes with delta 9-THC consistently decreased specific in vitro binding of [3H]dihydromorphine (mu opioid) in a dose-dependent fashion. Similar dose-dependent changes were elicited by
P J, Vaysse, E L, Gardner, R S, Zukin
openaire   +2 more sources

Cannabinoid Receptors and Modulation of Cyclic AMP Accumulation in the Rat Brain

Journal of Neurochemistry, 1990
Abstract: The mechanism by which cannabinoid compounds produce their effects in the rat brain was evaluated in this investigation. Cannabinoid receptors, quantitated by [3H]CP‐55,940 binding, were found in greatest abundance in the rat cortex, cerebellum, hippocampus, and striatum, with smaller but significant binding also found in the hypothalamus ...
M, Bidaut-Russell, W A, Devane, A C, Howlett   +2 more
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Modulation of Excitatory Synaptic Transmission During Cannabinoid Receptor Activation

Cellular and Molecular Neurobiology, 2021
The present research has reported that cannabinoid receptor 1 (CB1) agonist, delta-(9)-tetrahydrocannabinol (THC) modulates synaptogenesis during overexcitation. Microtubule and synaptic distribution, poly(ADP)-ribose (PAR) accumulation were estimated during overexcitation and in the presence of THC.
openaire   +2 more sources

Cannabinoid CB1 receptor antagonism modulates plasma corticosterone in rodents

European Journal of Pharmacology, 2006
Although the involvement of cannabinoids and the endogenous cannabinoid system in the regulation of the hypothalamo-pituitary-adrenal axis in rodents is well documented, the precise role played by the cannabinoid type one (CB(1)) receptor in this effect has not been fully elucidated.
Mark R, Wade, Aldemar, Degroot, George G, Nomikos   +2 more
openaire   +2 more sources

Biased Agonism and Biased Allosteric Modulation at the CB1 Cannabinoid Receptor

Molecular Pharmacology, 2015
CB1 cannabinoid receptors (CB1Rs) are attractive therapeutic targets for numerous central nervous system disorders. However, clinical application of cannabinoid ligands has been hampered owing to their adverse on-target effects. Ligand-biased signaling from, and allosteric modulation of, CB1Rs offer pharmacological approaches that may enable the ...
Elham, Khajehali, Daniel T, Malone, Michelle, Glass, Patrick M, Sexton, Arthur, Christopoulos, Katie, Leach   +5 more
openaire   +2 more sources