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Molecular mechanism of allosteric modulation for the cannabinoid receptor CB1

Nature Chemical Biology, 2022
Given the promising clinical value of allosteric modulators of G protein-coupled-receptors (GPCRs), mechanistic understanding of how these modulators alter GPCR function is of significance. Here, we report the crystallographic and cryo-electron microscopy structures of the cannabinoid receptor CB1 bound to the positive allosteric modulator (PAM) ZCZ011.
Xin Yang   +15 more
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   +2 more
openaire   +2 more sources

D2 Dopamine Receptors Modulate Gα-Subunit Coupling of the CB1 Cannabinoid Receptor

The Journal of Pharmacology and Experimental Therapeutics, 2004
CB(1) cannabinoid (CB(1)) and D(2) dopamine (D(2)) receptors are known to couple to the G protein Galpha(i/o). It has been reported that concurrent activation of D(2) receptors and CB(1) receptors, in primary striatal neuronal culture, promotes functional CB(1) receptor coupling to Galpha(s) resulting in elevations in intracellular cyclic AMP levels ...
A, Jarrahian, V J, Watts, E L, Barker
openaire   +2 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

Modulation of rat brain cannabinoid receptors after chronic morphine treatment

NeuroReport, 1997
Intraperitoneal injection of delta9-THC (7.5 mg/kg) in rats made tolerant to morphine by s.c. implantation of morphine pellets had a much greater analgesic effect than in placebo pellet plus delta9-THC treatment. To investigate whether this was due to some change in cannabinoid receptor levels and/or expression induced by chronic morphine, we designed ...
RUBINO, TIZIANA   +4 more
openaire   +3 more sources

Cannabinoid Receptor Modulation of Synapses Received by Cerebellar Purkinje Cells

Journal of Neurophysiology, 2000
The high density of cannabinoid receptors in the cerebellum and the degradation of motor coordination produced by cannabinoid intoxication suggest that synaptic transmission in the cerebellum may be strongly regulated by cannabinoid receptors. Therefore the effects of exogenous cannabinoids on synapses received by Purkinje cells were investigated in ...
K A, Takahashi, D J, Linden
openaire   +2 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   +8 more
openaire   +2 more sources

Cholesterol‐dependent modulation of type 1 cannabinoid receptors in nerve cells

Journal of Neuroscience Research, 2005
AbstractType 1 cannabinoid receptors (CB1R) are G‐protein‐coupled receptors that mediate several actions of the endocannabinoid anandamide (N‐arachidonoylethanolamine; AEA) in the central nervous system. Here we show that cholesterol enrichment of rat C6 glioma cell membranes reduces by approximately twofold the binding efficiency (i.e., the ratio ...
Bari M   +3 more
openaire   +4 more sources

Cannabinoid receptor 2 (CB2) modulators: A patent review (2016–2024)

Bioorganic Chemistry
Cannabinoid receptors CB1 and CB2 play critical roles in regulating numerous central and peripheral physiological activities. While efforts have been made to develop ligands for both CB1 and CB2 receptors, CB1 receptor ligands often have restricted use due to undesirable psychotropic side effects. Consequently, recent cannabis research has increasingly
Rayees Ahmad, Naikoo   +3 more
openaire   +2 more sources

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