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  • endocannabinoid
  • Here we show that muscarinic acetylcholine receptor (mAChR) activation also enhances transient endocannabinoid release (DSI) and induces persistent release. (jneurosci.org)
  • Although they were independent at the receptor level, muscarinic and glutamatergic mechanisms of endocannabinoid release shared intracellular machinery. (jneurosci.org)
  • Effects of genetic disruption of cannabinoid receptors or enzymes controlling endocannabinoid degradation on neuropathic nociception are described. (springer.com)
  • Potential mechanisms involved in the neuroprotective and corrective activity of ω3 PUFAs in the brain are discussed, in particular the sensing activity of free fatty acid receptors and the activity of the PUFAs-derived endocannabinoid system and the hypothalamic-pituitary-adrenal axis. (frontiersin.org)
  • 2-Arachidonoylglycerol (2-AG) is an endocannabinoid, an endogenous agonist of the CB1 receptor. (wikipedia.org)
  • The Endocannabinoid-CB Receptor System: Importance for development and in pediatric disease Neuroendocrinology Letters Nos.1/2, Feb-Apr Vol.25, 2004. (wikipedia.org)
  • It is closely related to the cannabinoid receptor type 1, which is largely responsible for the efficacy of endocannabinoid-mediated presynaptic-inhibition, the psychoactive properties of tetrahydrocannabinol, the active agent in cannabis, and other phytocannabinoids (plant cannabinoids). (wikipedia.org)
  • excitatory amin
  • Endo)cannabinoids have also been tested in models of excitotoxicity, which is a concept of neuronal cell death caused by overactivation of excitatory amino acid receptors. (jneurosci.org)
  • antagonists
  • 9-Aminoacridine, 9-tetrahydroaminoacridine, N1-dansyl-spermine, N1-dansyl-spermidine, and pentamidine have been shown to act as antagonists of δ2-containing receptors. (wikipedia.org)
  • Antagonists of the 5-HT2A receptor like cyproheptadine and chlorpromazine are able to reverse and mediate recovery from serotonin syndrome. (wikipedia.org)
  • residues
  • The binding of ligand to the α-chains of the IR ectodomain induces structural changes within the receptor leading to autophosphorylation of various tyrosine residues within the intracellular TK domain of the β-chain. (wikipedia.org)
  • Based on computer modeling, ligand interactions with CB2 receptor residues S3.31 and F5.46 appears to determine differences between CB1 and CB2 receptor selectivity. (wikipedia.org)
  • epithelial cells
  • Specific binding of anti-CB(1) immunoglobulin-G in tissue sections localized cannabinoid CB(1) receptor protein to the non-pigmented epithelial cells of the ciliary process and cells of the trabecular meshwork. (duke.edu)
  • mechanism
  • Although the precise binding mechanism of IR and its ligand has not yet been elucidated structurally, as identified using a systems biology approach, biologically relevant prediction of the IR-ligand kinetics (insulin/IGF-I) has been identified in the context of the currently available IR ectodomain structure. (wikipedia.org)
  • At a concentration of 0.3nM, 2-AG induces a rapid, transient increase in intracellular free calcium in NG108-15 neuroblastoma X glioma cells through a CB1 receptor-dependent mechanism. (wikipedia.org)
  • In 1985, not long after becoming section chief of NIDDK's neurobiology lab, Skolnick and colleagues published work helping to characterize the mechanism of action of barbiturates, which function as positive allosteric modulators at the GABAA receptor-a mechanism of action they share with benzodiazepines. (wikipedia.org)
  • Expression
  • Cannabinoid CB(1) receptor expression, activation and detection of endogenous ligand in trabecular meshwork and ciliary process tissues. (duke.edu)
  • Structure of a cannabinoid receptor and functional expression of the cloned cDNA. (springer.com)
  • The ability of RACs before or after treatment with TLR ligands to interact with T cells was assessed by measuring major histocompatibility complex class II and costimulatory molecule expression and cytokine production. (arvojournals.org)
  • At a global level, D1 receptors have widespread expression throughout the brain. (wikipedia.org)
  • Maximum expression of dopamine D3 receptors is noted in the islands of Calleja and nucleus accumbens. (wikipedia.org)
  • The sites of receptor expression are clearly linked to the different functions played by apelin in the organism. (wikipedia.org)
  • Vascular expression of the receptor participates in the control of blood pressure and its activation promotes the formation of new blood vessels (angiogenesis). (wikipedia.org)
  • Recently, receptor expression was also detected in skeletic muscle cells. (wikipedia.org)
  • This has created a long history of debate as to the Central Nervous System expression of the CB2 receptor. (wikipedia.org)
  • This has the potential to resolve questions about the expression of CB2 receptors in various tissues. (wikipedia.org)
  • In response, these receptors work with other proteins to regulate the expression of specific genes, thereby controlling the development, homeostasis, and metabolism of the organism. (wikipedia.org)
  • inhibits
  • said differently, that the initial binding of ligand to the IR inhibits further binding to its second active site - exhibition of allosteric inhibition. (wikipedia.org)
  • The D2-like family receptors are coupled to the G protein Giα, which directly inhibits the formation of cAMP by inhibiting the enzyme adenylyl cyclase. (wikipedia.org)
  • peptides
  • Synthetic peptides derived from the C-terminal amino acid sequence of bovine preproapelin were capable of specifically promoting the acidification rate in the cells expressing the APJ receptor in a range from 10(-7) to 10(-10) M, indicating that apelin is an endogenous ligand for the APJ receptor. (sigmaaldrich.com)
  • Endomorphins are endogenous opioid peptides that cause potent antinociception in rodent models of acute and neuropathic pain with less undesirable side effects than opioid alkaloids. (frontiersin.org)
  • Activation
  • Activation of a G protein-coupled receptor by its endogenous ligand triggers the innate immune response of Caenorhabditis elegans. (nih.gov)
  • The neural mechanisms underlying these prosocial effects are unclear but are likely to involve activation of CB 1 cannabinoid receptors, the main molecular target of marijuana in the human brain ( 5 ). (pnas.org)
  • To determine whether Toll-like receptor (TLR) ligands regulate the activation of retinal astrocytes (RACs) and the possible role of RACs in the polarization of interphotoreceptor retinoid-binding protein (IRBP)-specific T cells. (arvojournals.org)
  • Dopamine receptor activation of Ca2+/calmodulin-dependent protein kinase II can be cAMP dependent or independent. (wikipedia.org)
  • In addition, I1 receptor activation is used in ophthalmology to reduce intraocular pressure. (wikipedia.org)
  • I2 receptor activation has also been shown to decrease body temperature, potentially mediating neuroprotective effects seen in rats. (wikipedia.org)
  • The hypotensive effect of apelin results from the activation of receptors expressed at the surface of endothelial cells. (wikipedia.org)
  • In stomach, activation of receptors on enterochromaffine-like cells by apelin secreted by parietal cells can inhibit histamine release by enterochromaffine-like cells, which in turn decreases acid secretion by parietal cells. (wikipedia.org)
  • Their hallucinogenic effects are specifically mediated by activation of the 5-HT2A receptor. (wikipedia.org)