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Herbs with Antidepressant Effects
Published in Scott Mendelson, Herbal Treatment of Major Depression, 2019
Sub-chronic administration of the cannabinoid type 1 receptor agonist, HU-210, reduces immobility of rats in the forced swim test,17 as does the CB1 agonist, WIN55,212-2.18 Other cannabinoidergic substances with such antidepressant-like effects in rats are oleamide, a natural cannabinoid agonist, and the synthetic endocannabinoid uptake inhibitor, AM404.19
The Role of Cannabis and Cannabinoids in Pain Management
Published in Mark V. Boswell, B. Eliot Cole, Weiner's Pain Management, 2005
Dexanabinol is a synthetic cannabinoid agent developed at Hebrew University from Δ8-THC. It is a nonpsychoactive enantiomer of the extremely potent cannabis agonist, HU-210 (Pop, 2000). It has several interesting properties including antioxidant and anti-inflammatory effects, as well as suppression of TNF-α production. Additionally, it reduced damage in experimental focal ischemia, as may be associated with closed head injury (Lavie, Teichner, Shohami, Ovadia, & Leker, 2001). In one human Phase II clinical trial of 67 patients with closed-head injury, dexanabinol reduced intracranial pressure and perfusion significantly with few adverse events (Knoller et al., 2002). Improvements in clinical outcome scales were seen after 3 and 6 months, but were relatively subtle.
Historical overview
Published in G. Hussein Rassool, Alcohol and Drug Misuse, 2017
Synthetic drugs are created using man-made chemical compounds that mimic the effects of illicit drugs and are commonly divided into two categories: Cannabinoids such as “Spice” and “K2 (synthetic marijuana products); and stimulants such as bath salts. Most synthetic stimulants contain chemical compounds that mimic the effects of cocaine, LSD and methamphetamine. Similar drugs include MDMA (Ecstasy). Historically, Spice was first introduced for sale in London in 2004. Competitive brands of Spice entered the US market and became prevalent throughout the country by 2008 (www.drugfreeworld.org). However, the chemical compounds were created for experimental purposes decades ago. These chemical compounds include: CP 47,497, named after Charles Pfizer of Pfizer Pharmaceuticals, developed in the 1980’s for scientific research; HU-210 (100 to 800 times more potent than natural THC) from Hebrew University of Jerusalem (1988); and JWH-018 and others in the JWH series, created by Professor John W. Huffman of Clemson University (South Carolina) in 1995 (www.drugfreeworld.org). When the chemical compounds found in synthetic marijuana were banned in the US (2012), it is reported that “underground chemists then developed new experimental drugs, UR-144 and XLR11, that mimic the effects of marijuana, to replace those that had been banned. In 2013, UR-144 and XLR11 were made illegal, but by that time a new generation of synthetic marijuana had surfaced” (www.drugfreeworld.org). Bath salts (synthetic cathinones) as psychoactive substance refer to a white powder or crystalline substance that has no bathing or other cosmetic use. The substances were first synthesised in France in 1928 and 1929, researched for potential medical use and later used as antidepressants in the former Soviet Union in the 1930’s and 40’s (www.drugfreeworld.org). The khat-like cathinones substance which contains the active ingredients Cathinone, Methcathinone and Cathine, entered the Israeli drug scene as hagigat. The bath salts gained broader popularity among drug misusers and appeared on Internet drug forums. The bath salts were introduced in the US in the 1990’s. N-BOMe, also known as “N-Bomb” or “Smiles”, is a powerful synthetic hallucinogen, similar to LSD. N-bomb was discovered in 2003 by chemist Ralf Heim at the Free University of Berlin, Germany. It was derived from a group of drugs called the 2C family of phenethylamines (PEA) (www.drugfreeworld.org). It was in 2010 that the drug emerged as a common recreational drug.
Cannabinoid Receptor Type 1 and Its Role as an Analgesic: An Opioid Alternative?
Published in Journal of Dual Diagnosis, 2020
Amber L. Milligan, Thomas A. Szabo-Pardi, Michael D. Burton
Intrathecal (i.t.) injection of anandamide, an endogenous cannabinoid ligand, was found to inhibit A-delta and C-fiber neuronal responses to inflammatory pain (Harris, Drew, & Chapman, 2000). This was also demonstrated with (i.t.) HU-210, an exogenous cannabinoid ligand, with the most robust findings showing inhibition of hyper-excitability of C-fibers after repeated firing to inflammatory pain. Co-administration of selective CB1R antagonist S141716 (i.t.) blocked the analgesic effects of anandamide and HU-210, indicating a critical role of CB1R activation. Follow-up studies demonstrated that i.t. injection of HU-210 blocked neuronal nociceptive responses, as well as peak action potentials in the DRG (Millns, Chapman, & Kendall, 2001). The inhibitory action of HU-210 was again blocked by intrathecal co-administration of S141716. These results were also seen with WIN 55-212-2, another CB1R agonist (Fox et al., 2001). Systemically administered WIN 55-212-2 inhibited hyper-responsivity of neurons in the DRG to noxious pressure but did not alter non-nociceptive neurons (Hohmann, Martin, Tsou, & Walker, 1995). These findings provide strong support to suggest a specific role of CB1R in anti-nociception and acute analgesia in the peripheral nervous system.
Old and new synthetic cannabinoids: lessons from animal models
Published in Drug Metabolism Reviews, 2018
Mary Tresa Zanda, Liana Fattore
Discrimination stimulus effect induced by cannabinoid agonists is likely mediated by CB1 cannabinoid receptors since it is blocked by cannabinoid antagonists such as SR141716A (Maldonado 2002). Several compounds (e.g. opioids, hallucinogens, psychostimulants, antidepressants) have been studied in substitution to THC in drug discriminative studies but with little (if any) success, confirming the pharmacological specificity of the discriminative stimulus effects of cannabinoids (Järbe and Mathis 1991). In light of the pharmacological specificity of THC discriminative stimulus effect, it is expected that synthetic cannabinoids are able to generalize to THC. Among the first generation of synthetic cannabinoids, CP 55,940 fully substitutes for THC in both rats and monkeys trained to discriminate THC from vehicle (Gold et al. 1992; Hruba and McMahon 2014). Notably, when CP 55,940 is used as training drug, it is fully substituted by other cannabinoids with different chemical structures, like THC and WIN 55,212-2, suggesting that CP 55,940 possesses effective discriminative stimulus effects (Wiley et al. 1995). Similarly, CP 47,497, a bicyclic synthetic cannabinoid similar in structure to CP 55,940 but 6.3-fold more potent than THC (Grim et al. 2016), fully substitutes and generalizes with THC. The synthetic cannabinoid HU-210 also substitutes for THC in trained rhesus monkeys (Hruba and McMahon 2014), while WIN 55,212-2 generalizes to discriminative stimulus effect of THC in both rhesus monkeys (Hruba and McMahon 2014) and rats (Järbe et al. 2010).
Towards a better understanding of the cannabinoid-related orphan receptors GPR3, GPR6, and GPR12
Published in Drug Metabolism Reviews, 2018
Paula Morales, Israa Isawi, Patricia H. Reggio
It is also important to underscore that related phytocannabinoids, Δ9-tetrahydrocannabinol, cannabinol, and cannabigerol among them, were also evaluated at these receptors, but they did not exhibit activity at the concentrations tested in cAMP accumulation or β-arrestin2 recruitment assays (Brown et al. 2017; Laun and Song 2017). Additionally, synthetic cannabinoid ligands such as HU-210, CP55,940 and WIN55,212–2 were assessed at GPR12 (Brown et al. 2017). These compounds were able to inhibit cAMP accumulation, but only at high micromolar concentrations.