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Mystical States achieved through Psychedelics: The Origins, Classical, and Contemporary Use of Psychedelics
Published in Andrew C. Papanicolaou, A Scientific Assessment of the Validity of Mystical Experiences, 2021
Psychedelics come in many varieties. Those that are most frequently used—the so-called “classical” psychedelics—are primarily, though not exclusively, serotonin agonists, that is they bind to serotonin receptors, mainly the receptor 5-HT 2A. This is known because serotonin antagonists, that is, chemicals that block the effects of serotonin also block the effects of these psychotropic drugs.
Neurological problems
Published in Catherine Nelson-Piercy, Handbook of Obstetric Medicine, 2020
There are few data regarding pizotifen (Sanomigran®), a serotonin antagonist used for the prevention of migraine outside pregnancy, but its use is justified after the first trimester if first- and second-line prophylactic agents are not effective.
Regulation Of Cell Kinetics And Colon Cancer
Published in Herman Autrup, Gary M. Williams, Experimental Colon Carcinogenesis, 2019
Serotonin receptors have recently been classified into two groups, alpha and beta; the responses to alpha serotonin receptors being mediated by calcium ions and then possibly by cGMP, whereas the responses to beta serotonin receptors are mediated by cAMP.86 However, it should be noted that recent evidence regarding cGMP as an intracellular regulator is difficult to interpret since many agents that were previously shown to regulate guanylate cyclase in intact tissues have been shown not to activate the enzyme in disrupted cells.84 It is not currently possible to clearly distinguish between these two types of serotonin receptors, but preliminary evidence shows that those serotonin antagonists that most specifically inhibit the effects of serotonin on cAMP are not effective inhibitors of tumor cell proliferation. Hence, it is likely that the serotonin receptors stimulating tumor growth are of the alpha (that is, calcium ion-cGMP coupled) variety.
Emerging 5-HT receptor antagonists for the treatment of Schizophrenia
Published in Expert Opinion on Emerging Drugs, 2020
Mackenzie T. Jones, Martin T. Strassnig, Philip D. Harvey
In addition to the implications of serotonin antagonists for the treatment of negative symptoms, it is also possible that they could play a role in the modulation of antipsychotic-induced dopamine super-sensitivity. Since antipsychotic medications block dopamine receptors, the CNS responds to this blockade by increasing the sensitivity of dopamine receptors to try and overcome the blockade. This can interfere with ongoing treatment and increase the risk of relapse to psychosis in non-adherent patients. It is hypothesized that this sensitivity may be modulated by 5-HT2 receptors, since it has been found that activation of 5-HT2, or 5-HT2A receptors selectively, is required for full expression of antipsychotic-induced dopamine super-sensitivity in rats [85]. These findings raise the possibility that blockade of the 5-HT2A receptors could stave off relapse. Therefore, even if serotonin antagonists produce limited direct effects on psychosis, they may play a role in preventing relapse.
Anti-nociceptive effects of low dose ketamine in mice may be mediated by the serotonergic systems
Published in Psychiatry and Clinical Psychopharmacology, 2019
Meral Erdinc, Emre Uyar, Ilker Kelle, Hasan Akkoc
Drugs obtained from Sigma (St. Louis, MO, USA) were dissolved in saline and administered intraperitoneally (i.p.) in a volume of 0.1 ml/10 g body weight. Mice were separated into 14 groups (n = 8) and were treated with fluoxetine (20 mg/kg, 7 days) and a serotonin depleting agent; p-chlorophenylalanine (pCPA, 150 mg/kg, 4 days) or %0.9 saline. Drugs were administered once daily until the experiment day. A serotonin antagonist; methiothepin (0.1 mg/kg), an α-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) receptor antagonist; GYKI-52466 (20 mg/kg), an analgesic; metamizole (500 mg/kg); and ketamine (20 mg/kg) were administered 60 mins before the test procedure. Doses of the drugs were selected according to previous studies. An HP test was performed for a single time for these groups. Three groups (vehicle, metamizole, and ketamine) were separated in order to test the sustained analgesic effect of ketamine. The HP test was performed for 6 consecutive times with a 1-hour break between each test [12].
Cannabinoid hyperemesis syndrome: potential mechanisms for the benefit of capsaicin and hot water hydrotherapy in treatment
Published in Clinical Toxicology, 2018
John R. Richards, Jeff M. Lapoint, Guillermo Burillo-Putze
As legalization and availability of high-potency cannabis and synthetic cannabinoids continues to increase in the United States and worldwide, cannabinoid hyperemesis syndrome-related emergency department visits and hospital admissions will undoubtedly rise in step. There is limited research detailing the pathophysiology and best pharmacologic treatment of cannabinoid hyperemesis syndrome. Serotonin antagonists are often ineffective. Dopamine antagonists, such as phenothiazines and butyrophenones, appear to be somewhat more effective than 5-HT3 antagonists. Hot showers and baths often provide transient relief of cannabinoid hyperemesis syndrome-associated nausea, vomiting, and abdominal pain. Topical capsaicin can be administered rapidly and has been utilized to successfully treat acute attacks of cannabinoid hyperemesis syndrome. Future studies are needed to further define the role of topical capsaicin for cannabinoid hyperemesis syndrome. Recognition of cannabinoid hyperemesis syndrome and its resistance to routine antiemetics is important to help reduce emergency department visits, hospital admissions, unnecessary diagnostic testing, ineffective treatment, morbidity, and health care costs.