• 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)
  • noladin ether
  • The data also show that noladin ether-induced enhancement of outflow facility is mediated through the trabecular meshwork CB1 receptor, with an involvement of p42/44 MAP kinase signaling pathway and changes in actin cytoskeletons. (arvojournals.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)
  • 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)
  • 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)
  • 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)
  • compound
  • It was developed with the aim of finding a water-soluble cannabinoid agonist suitable for intravenous use as an analgesic, but did not proceed to human trials, with the related compound Org 28611 chosen instead due to its better penetration into the brain. (wikipedia.org)
  • Inhibitors
  • 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)
  • Human subjects injected with ghrelin remember pictures of food more clearly a day later and inhibitors of the ghrelin receptor could impair those memories [ 5 ]. (hindawi.com)
  • 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)
  • therapeutic
  • 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)
  • subtype
  • 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)
  • 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)
  • whereas
  • 1 2 CB1 receptors are located in the central nervous system (CNS) as well as in the periphery, whereas CB2 receptors are mainly located in the peripheral tissues, such as immune cells. (arvojournals.org)
  • analgesic
  • A-40174 (SP-1) is an analgesic drug which acts as a potent cannabinoid receptor agonist, and was developed by Abbott Laboratories in the 1970s. (wikipedia.org)
  • 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)
  • human
  • Several new cannabinoids are being developed for human use, but none has reached the stage of human testing in the United States. (nap.edu)