Wednesday, August 20, 2014

Syntethic and Natural Serotonergic Agent for Headache Relief

Evidence is accumulating that serotonin (5-hydroxytryptamine or 5-HT) 5HT1B and 5HT1D receptor agonistic compounds work in both nerve endings and blood vessels. Prescription drugs designed based on 5-HT1B and 5-HT1D receptor agonistic actions are effective in the treatment of cluster headache. Triptans are a group of serotonergic agent prescription drugs (Imitrex, Imigran, Cinie, Illument, Migriptan, Maxalt, Amerge, Naramig, Zomig, Relpax, Axert, Almogran, Frova, Migard, Frovamig and BMS-180,048) used as abortive medication in the treatment of migraines and cluster headaches. They act as agonist on serotonin 5-HT1B and 5-HT1D receptors in cranial blood vessels and subsequent inhibition of pro-inflammatory neuropeptide release. Tianma (Gastrodia elata) and Ergot (Claviceps purpurea) have been used for headaches and other body pains in Traditional Chinese Medicine and other folk remedies. Recent pharmacological studies have shown that the compounds isolated from Tianma and Ergot also act on 5-HT receptors and should have potential use for easing cluster headache. Tianma (天麻, Gastrodia elata) is a saprophytic perennial herb, found in China, Nepal, Bhutan, India, Japan, North Korean and Siberia, and grow at elevations of 400–3200 meters at the edge of forest. Its tuber is used in Traditional Chinese medicine and Sichuan cuisine for treating headaches, dizziness, tetanus, convulsions, hypertension, neurodegenerative diseases (PD and AD) and epilepsy. People can get Tianma tubers online or from Traditional Chinese Medicine stores and make oral powder for cluster headache and other headaches relief. Ergot fungi refer to a group of fungi of the genus Claviceps, such as Claviceps purpurea (rye ergot fungus). This fungus grows on rye and related plants. Ergot alkaloids have a wide range of biological activities including effects on circulation, neurotransmission, vasoconstriction and hallucination. Ergot contains no lysergic acid diethylamide (LSD) but instead contains ergotamine, which is used to synthesize lysergic acid, an analog of and precursor for synthesis of LSD. Ergot alkaloids, serotonergic agents, have traditionally been used for the acute and preventive treatment of cluster headache and other primary headaches. Intravenous methylergonovine (a synthetic derivative of ergonovine) are effective and safe drug in the management of severe migraine attacks. Psilocybin, a 5-HT2A, 5-HT1A, 5-HT1D and 5-HT2C receptor agonist, also eases pain attack: Psilocybin, a natural psychedelic compound, is produced by many mushrooms, known as psilocybin mushrooms, such as Psilocybe Mexicana, P. azurescens, P. semilanceata, and P. cyanescens. Psilocybin is quickly converted to psilocin in human body. Psilocin has mind-altering effects similar to those of LSD, mescaline, and DMT. The effects generally include euphoria, visual and mental hallucinations, changes in perception, a distorted sense of time, and spiritual experiences. Psilocin has a high affinity for the 5-HT2A serotonin receptor in the brain, where it mimics the effects of serotonin. Psilocin binds less tightly to other serotonergic receptors 5-HT1A, 5-HT1D, and 5-HT2C. Serotonin receptors are located in numerous parts of the brain, including the cerebral cortex, and are involved in a wide range of functions, including regulation of mood and motivation.

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