CRB-4001 was specifically designed to eliminate blood-brain barrier penetration and brain CB1 receptor
occupancy that mediate the neuropsychiatric issues associated with first-generation CB1 inverse agonists such as rimonabant.
The CB1 receptor
was subsequently identified in other mammalian brains, including those of humans.
Lab techniques that block access to the CB1 receptor
by THC eliminated the effects of THC exposure on endothelial cells.
Anandamide (and also2-arachydonoylglycerol) reduced excitatory postsynaptic currents in hippocampal slices from mice with temporal lobe epilepsy via CB1 receptor
In 1988, the first canabinnoid receptor was identified and isolated and named endocannabinoid receptor type 1 (CB1 receptor
); a second canabinnoid receptor was discovered in 1993 and named endocannabinoid receptor type 2 (CB2 receptor) (MUNRO et al., 1993).
For the CB1 receptor
, the optimal combination with the wild-type [beta]arr2 was established to be CB1-LgBiT SmBiT-[beta]arr2.
For instance, research using the chronic unpredictable stress model of depression found that the density of endocannabinoids and CB1 receptor
binding sites is decreased in a number of brain areas that are often related to affective disorders. Further, the antidepressant-like effects induced by antidepressant drugs in animal models, the administration of inhibitors of anandamide uptake or metabolism, and CB1 receptor
agonists all up-regulated the expression of endocannabinoids and the CB1 receptor
For example, activation of CB1 receptor
(CB1R) leads to activation of dopaminergic neurons .
In mice, peripheral administration of low doses of JZL184 was found to prevent the development of cisplatin-induced mechanical hyperalgesia in a CB1 receptor
, but not CB2 receptor, dependent manner .
stimulation regulates the intensity and duration of synaptic transmission (22).
Feasibility of Central Cannabmoid CB1 Receptor
Imaging with [124IJAM281 PET Demonstrated in a Schizophrenic Patient.
(2.) Mackie K, Mechanisms of CB1 receptor
signaling: endocannabinoid modulation of synaptic strength, International Journal of Obesity (2006) 30, S19-S23.