• efficacy
  • It is selective for CB2, with Ki values of 0.64 nM at CB2 vs 270 nM at the psychoactive CB1 receptor, but while it exhibits selective analgesic, anti-inflammatory and anti-hyperalgesic effects at low doses, its high efficacy at both targets results in typical cannabis-like effects appearing at higher doses, despite its low binding affinity for CB1. (wikipedia.org)
  • Obtaining a comprehensive understanding of the diverse mechanisms of cannabinoid action may lead to the design and development of therapeutic agents with greater efficacy and specificity for their cellular targets. (frontiersin.org)
  • compounds
  • The structure-activity relationships of these compounds have subsequently been investigated further leading to the development of a number of more potent analogues, derived by cyclisation around the indole or piperazine rings. (wikipedia.org)
  • Structurally it closely resembles cannabinoid compounds from patent WO 2003/035005 but with an indole core instead of indazole, and a simple pentyl chain on the indole 1-position. (wikipedia.org)
  • novel
  • We recently demonstrated that SA13353 (1-[2-(1-adamantyl)ethyl]-1-pentyl-3-[3-(4-pyridyl)propyl]urea), a novel TRPV1 agonist, inhibits tumor necrosis factor-a production by the activation of capsaicin-sensitive afferent neurons and reduces the severity of symptoms in kidney injury, lung inflammation, arthritis, and encephalomyelitis. (mdpi.com)
  • Pharmacological
  • Pharmacological testing determined APICA to have an IC50 of 175 nM at CB1, only slightly less potent than JWH-018 which had an IC50 of 169 nM, but over four times more tightly binding than APINACA, which had an IC50 of 824 nM. (wikipedia.org)
  • The future of medical marijuana lies in classical pharmacological drug development, and indeed there has been a resurgence of scientific, as well as public, interest in the therapeutic applications of cannabinoids. (nap.edu)
  • Currently available pharmacological treatments include serotonin reuptake inhibitors, serotonin-norepinephrine reuptake inhibitors, benzodiazepines, monoamine oxidase inhibitors, tricyclic antidepressant drugs, and partial 5-hydroxytryptamine (5-HT) 1A receptor agonists. (springer.com)
  • anandamide
  • The term cannabinoids is used in this chapter to refer to a group of substances that are structurally related to THC by virtue of a tricyclic chemical structure or that bind to cannabinoid receptors, such as the natural ligand anandamide. (nap.edu)
  • This important family of endogenous fatty acid molecules includes anandamide, the endocannabinoid that binds directly to the CB1 receptor (which is concentrated in the mammalian brain and central nervous system). (projectcbd.org)
  • PPAR
  • Recent studies indicate that CBD influences the expression of some genes by directly activating PPAR -gamma, a non-cannabinoid receptor situated on the cell's nucleus. (projectcbd.org)
  • Several studies have documented CBD 's role as a PPAR -gamma agonist. (projectcbd.org)
  • According to a 2008 report by Italian scientists at the University of Rome, both PPAR -alpha and PPAR -gamma agonists regulate angiogenesis, which entails the creation of new blood vessels, particularly capillaries. (projectcbd.org)
  • PPAR agonists have wide-ranging effects including inhibition of chemokine expression and pain behavior reduction in animal models. (frontiersin.org)
  • Experimental evidence suggests a connection between the pain ameliorating effects of PPAR agonists and suppression of inflammatory gene expression, including chemokines. (frontiersin.org)
  • In early clinical research, one PPARα agonist, palmitoylethanolamide (PEA), shows promise in relieving chronic pain. (frontiersin.org)
  • While much remains to be understood about how PPAR agonists achieve this effect, it seems probable that inhibiting the expression of pain-causing inflammatory mediators like chemokines represents at least one mechanism for pain reduction. (frontiersin.org)
  • therapeutic
  • The cannabinoid molecules are derived from Cannabis sativa plant which acts on the cannabinoid receptors types 1 and 2 (CB 1 and CB 2 ) which have been explored as potential therapeutic targets for drug discovery and development. (hindawi.com)
  • Therefore, the plant based cannabinoid molecules proved to be promising and emerging therapeutic alternative. (hindawi.com)
  • These scientific accomplishments have propelled interest in developing new drugs that can treat more effectively or more safely the constellation of symptoms for which cannabinoids might have therapeutic benefit (see chapter 4). (nap.edu)
  • Through the process of what is referred to as ''rational drug design,'' scientists manipulate the chemical structures of known cannabinoids to design better therapeutic agents. (nap.edu)
  • These sections serve as a road map to determine whether the therapeutic potential of cannabinoids is likely to be exploited commercially to meet patient needs. (nap.edu)
  • Cannabinoids are well known for their psychotropic properties, as well as for their therapeutic potential. (arvojournals.org)
  • selectivity
  • Unfortunately, many of these drugs have numerous side effects, due to a lack of receptor subtype selectivity ( 4 ) and/or an interference with physiological signaling ( 5 ). (pubmedcentralcanada.ca)
  • closely related
  • It is closely related to natural cannabinoids of the tetrahydrocannabinol (THC) group, differing mainly by its longer and branched side chain, and the replacement of the 9-position carbon with a nitrogen. (wikipedia.org)
  • A family of closely related cation channels, known as transient receptor potential (TRP) channels, has been discovered since the 1990s. (mdpi.com)
  • molecules
  • Also, these naturally derived molecules possess the least adverse effects opposed to the synthetically derived cannabinoids. (hindawi.com)
  • Cannabinoids include the active constituents of Cannabis or are molecules that mimic the structure and/or function of these Cannabis -derived molecules. (frontiersin.org)
  • Cannabis
  • Furthermore, APICA possesses cannabis-like effects in rats, and appears to be less potent than JWH-018 but more potent than THC. (wikipedia.org)
  • Results of this study show that Δ 9 -THC and other cannabinoids exert antidepressant-like actions, and thus may contribute to the overall mood-elevating properties of cannabis. (pubmedcentralcanada.ca)
  • dopamine
  • The endocannabinoids virodhamine and N -arachidonoyl dopamine are potent inhibitors of N -formyl- l -methionyl- l -leucyl- l -phenylalanine-induced migration of human neutrophils, with IC 50 values of 0.2 and 8.80 nM, respectively. (aspetjournals.org)
  • Patent
  • AM-679 AM-1235 AM-2201 AM-2232 AM-2233 FUBIMINA JWH-018 List of AM cannabinoids List of JWH cannabinoids THJ-2201 WO patent 200128557, Makriyannis A, Deng H, "Cannabimimetic indole derivatives", granted 2001-06-07 Willis PG, Katoch-Rouse R, Horti AG. (wikipedia.org)
  • Controlled Substances
  • Like controlled substances, cannabinoids developed for medical use encounter a gauntlet of public health regulatory controls administered by two federal agencies: the Food and Drug Administration (FDA) of the U.S. Department of Health and Human Services (DHHS) and the Drug Enforcement Administration (DEA) of the U.S. Department of Justice. (nap.edu)
  • clinical
  • It was developed with the aim of finding a water-soluble cannabinoid agonist suitable for intravenous use as an analgesic, and while it achieved this aim and has progressed as far as Phase II clinical trials in humans as both a sedative and an analgesic, results against the comparison drugs (midazolam and morphine respectively) were not particularly favourable in initial testing. (wikipedia.org)