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Tabernanthine
Tabernanthine is an alkaloid found in ''Tabernanthe iboga''. It has been used in laboratory experiments to study how addiction affects the brain. Tabernanthine persistently reduced the self-administration of cocaine and morphine in rats. Pharmacology It is kappa opioid agonist (Ki = 0.15 μM) and NMDA receptor (Ki = 10.5 μM) antagonist. Compared to ibogaine, it binds weakly to σ1 and σ2 receptor. See also * Coronaridine * Ibogamine * Voacangine Voacangine (12-methoxyibogamine-18-carboxylic acid methyl ester) is an alkaloid found predominantly in the root bark of the ''Voacanga africana'' tree, as well as in other plants such as ''Tabernanthe iboga'', ''Tabernaemontana africana'', ''Trach ... * Tabernaemontanine * Tabernanthalog References Alkaloids found in Iboga NMDA receptor antagonists Azepines Quinuclidine alkaloids Tryptamine alkaloids {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ibogamine
Ibogamine is an anti-convulsant, anti-addictive, CNS stimulant alkaloid found in ''Tabernanthe iboga'' and Crepe Jasmine (''Tabernaemontana divaricata''). Basic research related to how addiction affects the brain has used this chemical. Ibogamine persistently reduced the self-administration of cocaine and morphine in rats. The same study found that ibogamine (40 mg/kg) and coronaridine (40 mg/kg) did not produce "any tremor effects in rats that differ significantly from saline control". While the related alkaloids ibogaine (20–40 mg/kg), harmaline (10–40 mg/kg) and desethylcoronaridine (10–40 mg/kg) were "obviously tremorgenic". Chemistry Synthesis Ibogamine can be prepared from one-step demethoxycarbonylation process through coronaridine. Pharmacology Like ibogaine, it has seems to have similar pharmacology. It has effects on KOR, NMDAR, nAChR and serotonin sites. It also inhibits acetylcholinesterase and butyrylcholinesterase See also ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Coronaridine
Coronaridine, also known as 18-carbomethoxyibogamine, is an alkaloid found in ''Tabernanthe iboga'' and related species, including ''Tabernaemontana divaricata'' for which (under the now obsolete synonym ''Ervatamia coronaria'') it was named. Like ibogaine, (''R'')-coronaridine and (''S'')-coronaridine can decrease intake of cocaine and morphine intake in animals and it may have muscle relaxant and hypotensive activity. Chemistry Congeners Coronaridine congers are important in drug discovery and development due to multiple actions on different targets. They have ability to inhibit Cav2.2 channel, modulate and inhibit subunits of nAChr selectively such as α9α10, α3β4 and potentiate GABAA activity. Pharmacology Coronaridine has been reported to bind to an assortment of molecular sites, including: μ-opioid (Ki = 2.0 μM), δ-opioid (Ki = 8.1 μM), and κ-opioid receptors (Ki = 4.3 μM), NMDA receptor (Ki = 6.24 μM) (as an antagonist), and nAChRs (as an antagonist). It h ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tabernaemontanine
Tabernaemontanine is a naturally occurring monoterpene indole alkaloid found in several species in the genus ''Tabernaemontana'' including ''Tabernaemontana divaricata''. History Tabernaemontanine was first reported in 1939 but its structure was only fully confirmed in the 1970s as there was confusion in the original literature regarding the configuration of the ethyl group in the piperidine ring of this alkaloid and its isomer dregamine, so that their identities had been reversed. Both compounds were isolated from plants of the dogbane (Apocynaceae) family including '' Tabernaemontana coronaria''. They have structures that are reduced versions of vobasine. Biosynthesis As with other Indole alkaloids, the biosynthesis of tabernaemontanine starts from the amino acid tryptophan. This is converted into strictosidine before further elaboration. Natural occurrence Tabernaemontanine is found commonly in the genera ''Tabernaemontana'' and ''Kopsia'', including the species '' Ervatamia h ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Azepines
Azepines are unsaturated heterocycles of seven atoms, with a nitrogen replacing a carbon at one position. See also * Azepane * Benzazepines * Diazepine * Oxepin * Borepin Borepins are a class of boron-containing heterocycles used in main group chemistry. They consist of a seven-membered unsaturated ring with a tricoordinate boron in it. Simple borepins are analogues of cycloheptatriene, which is a seven-membered ... Azepines {{Heterocyclic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
NMDA Receptor Antagonists
NMDA receptor antagonists are a class of drugs that work to antagonize, or inhibit the action of, the ''N''-Methyl-D-aspartate receptor (NMDAR). They are commonly used as anesthetics for animals and humans; the state of anesthesia they induce is referred to as dissociative anesthesia. Several synthetic opioids function additionally as NMDAR-antagonists, such as pethidine, levorphanol, methadone, dextropropoxyphene, tramadol and ketobemidone. Some NMDA receptor antagonists, such as ketamine, dextromethorphan (DXM), phencyclidine (PCP), methoxetamine (MXE), and nitrous oxide (N2O), are sometimes used as recreational drugs, for their dissociative, hallucinogenic, and euphoriant properties. When used recreationally, they are classified as dissociative drugs. Uses and effects NMDA receptor antagonists induce a state called dissociative anesthesia, marked by catalepsy, amnesia, and analgesia. Ketamine is a favored anesthetic for emergency patients with unknown medical history and i ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Alkaloids Found In Iboga
Alkaloids are a class of basic, naturally occurring organic compounds that contain at least one nitrogen atom. This group also includes some related compounds with neutral and even weakly acidic properties. Some synthetic compounds of similar structure may also be termed alkaloids. In addition to carbon, hydrogen and nitrogen, alkaloids may also contain oxygen, sulfur and, more rarely, other elements such as chlorine, bromine, and phosphorus.Chemical Encyclopedia: alkaloids xumuk.ru Alkaloids are produced by a large variety of organisms including , , |
Tabernanthalog
Tabernanthalog is a novel water-soluble, non-toxic azepinoindole analog of the psychoactive drug ibogaine first synthesized by Professor David E. Olson at UC Davis. * In rodents, it was found to promote structural neural plasticity, reduce drug seeking behavior, and produce antidepressant like effects. Due to the rapidly-induced and enduring neuroplasticity, Tabernanthalog is a member of the class of compounds known as non-hallucinogenic psychoplastogens. * This compound, as well as related compounds, are licensed by Delix Therapeutics and are being developed as potential medicines for neuropsychiatric disorders. See also * PNU-22394 * Psychoplastogen Psychoplastogens are a group of small molecule drugs that produce rapid and sustained effects on neuronal structure and function, intended to manifest therapeutic benefit after a single administration. Several existing psychoplastogens have been ... * Delix Therapeutics * David E. Olson References Tryptamines H ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Voacangine
Voacangine (12-methoxyibogamine-18-carboxylic acid methyl ester) is an alkaloid found predominantly in the root bark of the ''Voacanga africana'' tree, as well as in other plants such as ''Tabernanthe iboga'', ''Tabernaemontana africana'', ''Trachelospermum jasminoides'', ''Tabernaemontana divaricata'' and ''Ervatamia yunnanensis''. It is an iboga alkaloid which commonly serves as a precursor for the semi-synthesis of ibogaine. It has been demonstrated in animals to have similar anti-addictive properties to ibogaine itself. It also potentiates the effects of barbiturates. Under UV-A and UV-B light its crystals fluoresce blue-green, and it is soluble in ethanol. Pharmacology Pharmacodynamics Voacangine exhibits AChE inhibitory activity. Docking simulation reveals that it has inhibitory effect on VEGF2 kinase and reduces angiogenesis. Like ibogaine, its a potent HERG blocker in vitro. It also acts as antagonist to TRPM8 and TRPV1 receptor but agonist of TRPA1. Pharmacokinetics The a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Alkaloid
Alkaloids are a class of basic, naturally occurring organic compounds that contain at least one nitrogen atom. This group also includes some related compounds with neutral and even weakly acidic properties. Some synthetic compounds of similar structure may also be termed alkaloids. In addition to carbon, hydrogen and nitrogen, alkaloids may also contain oxygen, sulfur and, more rarely, other elements such as chlorine, bromine, and phosphorus.Chemical Encyclopedia: alkaloids xumuk.ru Alkaloids are produced by a large variety of organisms including , , Medicinal plant, plants, an ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tabernanthe Iboga
''Tabernanthe iboga'' (iboga) is an evergreen rainforest shrub native to Central Africa. A member of the Apocynaceae family indigenous to Gabon, the Democratic Republic of Congo, and the Republic of Congo, it is cultivated across Central Africa for its medicinal and other effects. In African traditional medicine and rituals, the yellowish root or bark is used to produce hallucinations and near-death outcomes, with some fatalities occurring. In high doses, ibogaine is considered to be toxic, and has caused serious comorbidities when used with opioids or prescription drugs. The United States Drug Enforcement Administration (DEA) lists ibogaine as a controlled substance of the Controlled Substances Act. Description Iboga is native to tropical forests, preferring moist soil in partial shade. It bears dark green, narrow leaves and clusters of white tubular flowers on an erect and branching stem, with yellow-orange fruits resembling Chili pepper , Normally growing to a height of ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sigma-2 Receptor
The sigma-2 receptor (σ2R) is a sigma receptor subtype that has attracted attention due to its involvement in diseases such as cancer and neurological diseases. It is currently under investigation for its potential diagnostic and therapeutic uses. Although the sigma-2 receptor was identified as a separate pharmacological entity from the sigma-1 receptor in 1990, the gene that codes for the receptor was identified as TMEM97 only in 2017. TMEM97 was shown to regulate the cholesterol transporter NPC1 and to be involved in cholesterol homeostasis. The sigma-2 receptor is a four-pass transmembrane protein located in the endoplasmic reticulum. It has been found to play a role in both hormone signaling and calcium signaling, in neuronal signaling, in cell proliferation and death, and in binding of antipsychotics. Classification The sigma-2 receptor is located in the lipid raft. The sigma-2 receptor is found in several areas of the brain, including high densities in the cerebellum, m ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sigma-1 Receptor
The sigma-1 receptor (σ1R), one of two sigma receptor subtypes, is a chaperone protein at the endoplasmic reticulum (ER) that modulates calcium signaling through the IP3 receptor. In humans, the σ1 receptor is encoded by the ''SIGMAR1'' gene. The σ1 receptor is a transmembrane protein expressed in many different tissue types. It is particularly concentrated in certain regions of the central nervous system. It has been implicated in several phenomena, including cardiovascular function, schizophrenia, clinical depression, the effects of cocaine abuse, and cancer. Much is known about the binding affinity of hundreds of synthetic compounds to the σ1 receptor. An endogenous ligand for the σ1 receptor has yet to be conclusively identified, but tryptaminergic trace amines and neuroactive steroids have been found to activate the receptor. Especially progesterone, but also testosterone, pregnenolone sulfate, and dehydroepiandrosterone sulfate (DHEA-S) bind to the σ1 receptor. C ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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