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Ibogaminalog
Ibogaminalog (developmental code name DM-506) is a drug of the ibogalog group first invented in the 1960s, which acts as both a partial agonist at the 5-HT2A receptor, 5-HT2A Receptor (biochemistry), receptor, and a negative allosteric modulator at the α7 and α9α10 nicotinic acetylcholine receptors. It can be regarded as a structurally simplified derivative of ibogaine and has been researched both for anti-addictive effects and for the treatment of neuropathic pain. See also * Ibogalog * Lorcaserin * PHA-57378 * PNU-22394 * PNU-181731 * Ibogainalog * Tabernanthalog References N,N-Dialkyltryptamines Ibogalogs Serotonin receptor agonists {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tabernanthalog
Tabernanthalog (TBG, DLX-007) is a novel water-soluble, non-toxic ibogalog or simplified analogue of the psychoactive drug tabernanthine first synthesized by David E. Olson at UC Davis. Tabernanthalog is a non-hallucinogenic serotonin 5-HT2A receptor agonist. It is also a serotonin 5-HT2B receptor antagonist. The drug is described as having high selectivity for the serotonin 5-HT2 receptors. Other targets of the drug include monoamine oxidase A (MAO-A), the α2A-adrenergic receptor, the serotonin 5-HT1B and 5-HT2C receptors, and the serotonin transporter (SERT). In rodents, it was found to promote structural neural plasticity, reduce drug seeking behavior, and produce antidepressant like effects. It has also been shown that it effectively reduces motivation for heroin and alcohol in rats. This indicates its efficacy in animals with a history of heroin and alcohol polydrug use. Due to the rapidly-induced and enduring neuroplasticity, tabernanthalog is a member of the clas ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ibogainalog
Ibogainalog (IBG), also known as 9-methoxyibogaminalog, is a serotonergic psychedelic and psychoplastogen of the ibogalog group related to ibogaine but with a simplified chemical structure. Pharmacology It acts as a serotonin 5-HT2A receptor agonist, serotonin 5-HT2B receptor antagonist, and also interacts with other serotonin receptors, such as the serotonin 5-HT1F receptor (agonist), 5-HT2C receptor (very weak partial agonist or antagonist), and 5-HT6 receptor (agonist). Unlike noribogaine, IBG shows no activation of the opioid receptors or κ-opioid receptor agonism. In addition to its actions at serotonin receptors, IBG inhibits certain nicotinic acetylcholine receptors. The drug produces the head-twitch response in animals and hence shows psychedelic-like effects. However, it has reduced hallucinogen-like effects compared to 5-MeO-DMT. Conversely, tabernanthalog (TBG), a simplified analogue of tabernanthine and positional isomer of IBG, appears to be completely non-h ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
PNU-22394
PNU-22394 is a drug of the ibogalog group which acts as an agonist at serotonin 5-HT2 Receptor (biochemistry), receptors, with strongest binding affinity for 5-HT2A receptor, 5-HT2A and 5-HT2C receptor, 5-HT2C and slightly weaker at 5-HT2B receptor, 5-HT2B, although it is only a full agonist at 5-HT2C, but partial agonist at 5-HT2A and 5-HT2B. It has anorectic effects in both animal studies and human trials, along with "Pro-Cognitive Properties", although it has never been developed for medical use. See also * Ibogalog * Ibogaminalog * Lorcaserin * Tryptoline * PNU-181731 * PHA-57378 * Tabernanthalog References 1-Alkyltryptamines Ibogalogs N-Monoalkyltryptamines Serotonin receptor agonists {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ibogalog
Noribogaminalog, or ''N''-desmethylibogaminalog, also known as 1,2,3,4,5,6-hexahydroazepino[4,5-b]indole, is a chemical compound and parent structure of the ibogalog group of compounds. The ibogalogs that have been described include ibogaminalog, ibogainalog, noribogainalog, tabernanthalog, fluorogainalog, LS-22925, PNU-22394, and PHA-57378, among others. The ibogalogs, specifically ibogainalog and analogues, were first described in the scientific literature by 1968. See also * Azepinoindole * Iboga-type alkaloid * Desethylibogamine References External links Noribogaminalog - Isomer DesignIbogalogs, Drug Discovery, and the New Psychedelic Era - NeuWrite West Ibogalogs {{Organic-compound-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lorcaserin
Lorcaserin, marketed under the brand name Belviq, was a weight-loss drug developed by Arena Pharmaceuticals. It reduces appetite by activating serotonin receptor the 5-HT2C receptor in the hypothalamus, a region of the brain which is known to control appetite. It was approved in 2012, and in 2020, it was removed from the market in the United States due to an increased risk of cancer detected in users of Belviq. Medical uses Lorcaserin was used long term for weight loss in those who are obese. The safety and efficacy of Belviq were evaluated in three randomized, placebo-controlled trials that included nearly 8,000 obese and overweight patients, with and without type 2 diabetes, treated for 52 to 104 weeks. All participants received lifestyle modification that consisted of a reduced calorie diet and exercise counseling. Compared with placebo, treatment with Belviq for up to one year was associated with average weight loss ranging from 3 percent to 3.7 percent. About 47 percen ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
PNU-181731
PNU-181731 is a drug which acts as an agonist at serotonin 5-HT2 receptors, with strongest binding affinity for the 5-HT2C subtype at 4.8nM, and weaker 5-HT2A affinity of 18nM. It has anxiolytic effects in animal studies with around one tenth the potency of alprazolam and no significant ataxia or other side effects noted. See also * Lorcaserin * PNU-22394 * PHA-57378 PHA-57378 is a drug related to the ibogalogs which acts as an agonist at serotonin 5-HT2 receptors, having a binding affinity of 4.1 nM at the 5-HT2A subtype and 4.3 nM at 5-HT2C. It has anxiolytic effects in animal studies. See also * Ibog ... References Serotonin receptor agonists Pyrrolodiazepines Isotryptamines {{anxiolytic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
PHA-57378
PHA-57378 is a drug related to the ibogalogs which acts as an agonist at serotonin 5-HT2 receptors, having a binding affinity of 4.1 nM at the 5-HT2A subtype and 4.3 nM at 5-HT2C. It has anxiolytic effects in animal studies. See also * Ibogalog * PNU-22394 PNU-22394 is a drug of the ibogalog group which acts as an agonist at serotonin 5-HT2 Receptor (biochemistry), receptors, with strongest binding affinity for 5-HT2A receptor, 5-HT2A and 5-HT2C receptor, 5-HT2C and slightly weaker at 5-HT2B recept ... * PNU-181731 * WAY-470 References 1-Alkyltryptamines Ibogalogs N-Monoalkyltryptamines Serotonin receptor agonists {{anxiolytic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ibogalog
Noribogaminalog, or ''N''-desmethylibogaminalog, also known as 1,2,3,4,5,6-hexahydroazepino[4,5-b]indole, is a chemical compound and parent structure of the ibogalog group of compounds. The ibogalogs that have been described include ibogaminalog, ibogainalog, noribogainalog, tabernanthalog, fluorogainalog, LS-22925, PNU-22394, and PHA-57378, among others. The ibogalogs, specifically ibogainalog and analogues, were first described in the scientific literature by 1968. See also * Azepinoindole * Iboga-type alkaloid * Desethylibogamine References External links Noribogaminalog - Isomer DesignIbogalogs, Drug Discovery, and the New Psychedelic Era - NeuWrite West Ibogalogs {{Organic-compound-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Partial Agonist
In pharmacology, partial agonists are drugs that bind to and activate a given Receptor (biochemistry), receptor, but have only partial Intrinsic activity, efficacy at the receptor relative to a full agonist. They may also be considered Ligand (biochemistry), ligands which display both agonistic and Receptor antagonist, antagonistic effects—when both a full agonist and partial agonist are present, the partial agonist actually acts as a competitive antagonist, competing with the full agonist for receptor occupancy and producing a net decrease in the receptor activation observed with the full agonist alone. Clinically, partial agonists can be used to activate receptors to give a desired submaximal response when inadequate amounts of the endogenous ligand are present, or they can reduce the overstimulation of receptors when excess amounts of the endogenous ligand are present. Some currently common drugs that have been classed as partial agonists at particular receptors include buspi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Neuropathic Pain
Neuropathic pain is pain caused by a lesion or disease of the somatosensory nervous system. Neuropathic pain may be associated with abnormal sensations called dysesthesia or pain from normally non-painful stimuli (allodynia). It may have continuous and/or episodic (paroxysmal) components. The latter resemble stabbings or electric shocks. Common qualities include burning or coldness, "pins and needles" sensations, numbness and itching. Up to 7–8% of the European population is affected by neuropathic pain, and in 5% of persons it may be severe. The pain may result from disorders of the peripheral nervous system or the central nervous system (brain and spinal cord). Neuropathic pain may occur in isolation or in combination with other forms of pain. Medical treatments focus on identifying the underlying cause and relieving pain. In cases of peripheral neuropathy, the pain may progress to insensitivity. Diagnosis Diagnosis of pain conditions relies on the character of the pain w ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ibogaine
Ibogaine is a psychoactive indole alkaloid derived from plants such as '' Tabernanthe iboga'', characterized by hallucinogenic and oneirogenic effects. Traditionally used by Central African foragers, it has undergone controversial research for the treatment of substance use disorders. Ibogaine exhibits complex pharmacology by interacting with multiple neurotransmitter systems, notably affecting opioid, serotonin, sigma, and NMDA receptors, while its metabolite noribogaine primarily acts as a serotonin reuptake inhibitor and κ-opioid receptor agonist. The psychoactivity of the root bark of the iboga tree, ''T. iboga'', one of the plants from which ibogaine is extracted, was first discovered by forager tribes in Central Africa, who passed the knowledge to the Bwiti tribe of Gabon. It was first documented in the 19th century for its spiritual use, later isolated and synthesized for its psychoactive properties, briefly marketed in Europe as a stimulant, and ultimately rese ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
