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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 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 a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Iboga Alkaloid
Iboga-type alkaloids are a set of monoterpene indole alkaloids comprising naturally occurring compounds found in ''Tabernanthe'' and ''Tabernaemontana'', as well as synthetic structural analogs. Naturally occurring iboga-type alkaloids include ibogamine, ibogaine, tabernanthine, and other substituted ibogamines . Many iboga-type alkaloids display Biological activity, biological activities such as Cardiotoxicity, cardiac toxicity and Psychoactive drug, psychoactive effects, and some have been studied as potential treatments for drug addiction. Naturally-occurring (16R,20S)-Ibogaine Structural Formula V2.svg, Ibogaine (16R,20S)-Ibogamine Structural Formula V2.svg, Ibogamine (16R,20S)-Tabernanthine Structural Formula V2.svg, Tabernanthine (16S,20S)-Coronaridine Structural Formula V2.svg, Coronaridine Substituted ibogamines Catharanthine is an Saturated and unsaturated compounds, unsaturated analog of coronaridine. Oxidation products Similarly to other ring-constrained Su ... [...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] |
Alpha-3 Beta-4 Nicotinic Receptor
The alpha-3 beta-4 nicotinic receptor, also known as the α3β4 receptor and the ganglion-type nicotinic receptor,Pharmacology, (Rang, Dale, Ritter & Moore, , 5th ed., Churchill Livingstone 2003) p. 138. is a type of nicotinic acetylcholine receptor, consisting of α3 and β4 subunits. It is located in the autonomic ganglia and adrenal medulla, where activation yields post- and/or presynaptic excitation, mainly by increased Na+ and K+ permeability. As with other nicotinic acetylcholine receptors, the α3β4 receptor is pentameric α3)m(β4)n where m + n = 5 The exact subunit stoichiometry is not known and it is possible that more than one functional α3β4 receptor assembles in vivo with varying subunit stoichiometries. Ligands which inhibit the α3β4 receptor have been shown to modulate drug-seeking behavior, making α3β4 a promising target for the development of novel antiaddictive agents. Ligands Source: Agonists * Acetylcholine (endogenous neurotransmitter that b ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tabernaemontana Divaricata
''Tabernaemontana divaricata'', commonly called pinwheel flower, crape jasmine, East India rosebay, and Nero's crown, is an evergreen shrub or small tree native to South Asia, Southeast Asia and China. In zones where it is not hardy it is grown as a house/glasshouse plant for its attractive flowers and foliage. The stem exudes a milky latex when broken, whence comes the name milk flower Description The plant generally grows to a height of and is dichotomously branched. The large shiny leaves are deep green and about in length and in width. The waxy blossoms are found in small clusters on the stem tips. The (single) flowers have the characteristic 'pinwheel' shape also seen in other genera in the family Apocynaceae such as '' Vinca'' and '' Nerium''. Both single and double-flowered forms are cultivated, the flowers of both forms being white. The plant blooms in spring but flowers appear sporadically all year. The flowers have a pleasing fragrance. More than 66 alkaloids are ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tabernaemontana Litoralis
''Tabernaemontana'' is a genus of flowering plants in the family Apocynaceae. It has a pan-tropical distribution, found in Asia, Africa, Australia, North America, South America, and islands of the Indian and Pacific Oceans. These plants are evergreen shrubs and small trees growing to 1–15 m tall. The leaves are arranged in opposite pairs, 3–25 cm long, with milky sap; hence it is one of the diverse plant genera commonly called "milkwood". The flowers are fragrant, white, 1–5 cm in diameter. The cultivar '' T. divaricata'' cv. 'Plena', with doubled-petaled flowers, is a popular houseplant. Some members of the genus ''Tabernaemontana'' are used as additives to some versions of the psychedelic drink ayahuasca; the genus is known to contain ibogaine (e.g. in bëcchëte, ''T. undulata''), conolidine (present in minor concentration in ''T. divaricata'') and voacangine ('' T. alba'', '' T. arborea'', '' T. africana''). Because of presence of coronaridine and voacangi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nicotinic Acetylcholine Receptor
Nicotinic acetylcholine receptors, or nAChRs, are Receptor (biochemistry), receptor polypeptides that respond to the neurotransmitter acetylcholine. Nicotinic receptors also respond to drugs such as the agonist nicotine. They are found in the central and peripheral nervous system, muscle, and many other tissues of many organisms. At the neuromuscular junction they are the primary receptor in muscle for motor nerve-muscle communication that controls muscle contraction. In the peripheral nervous system: (1) they transmit outgoing signals from the presynaptic to the postsynaptic cells within the Sympathetic nervous system, sympathetic and parasympathetic nervous system, and (2) they are the receptors found on skeletal muscle that receive acetylcholine released to signal for muscular contraction. In the immune system, nAChRs regulate inflammatory processes and signal through distinct intracellular pathways. In insects, the cholinergic system is limited to the central nervous system. ... [...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), 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, bipolar disorder, and cancer. Much is known about the binding affinity of hundreds of synthetic compounds to the σ1 receptor. An endogenous ligand (biochemistry), 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, N,N-dimethy ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Voltage-gated Sodium Channel
Voltage-gated sodium channels (VGSCs), also known as voltage-dependent sodium channels (VDSCs), are a group of voltage-gated ion channels found in the membrane of excitable cells (''e.g.'', muscle, glial cells, neurons, etc.) with a permeability to the sodium ion Na+. They are the main channels involved in action potential of excitable cells. Structure Sodium channels consist of large alpha subunits that associate with accessory proteins, such as beta subunits. An alpha subunit forms the core of the channel and is functional on its own. When the alpha subunit protein is expressed by a cell, it is able to form a pore in the cell membrane that conducts Na+ in a voltage-dependent way, even if beta subunits or other known modulating proteins are not expressed. When accessory proteins assemble with α subunits, the resulting complex can display altered voltage dependence and cellular localization. The alpha subunit consists of four repeat domains, labelled I through IV, each cont ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sodium Channel Blocker
Sodium channel blockers are drugs which impair the conduction of sodium ions (Na+) through sodium channels. Extracellular The following naturally-produced substances block sodium channels by binding to and occluding the extracellular pore opening of the channel: * Alkaloids: ** Saxitoxin (STX) ** Neosaxitoxin (NSTX) ** Tetrodotoxin (TTX) Intracellular Drugs which block sodium channels by blocking from the intracellular side of the channel include: * Local anesthetics: ''lidocaine'' * Class I antiarrhythmic agents * Various anticonvulsants: ''phenytoin, oxcarbazepine (derivative of carbamazepine)'' Unknown mechanism * Calcium has been shown to block sodium channels which explains the effects of hypercalcemia and hypocalcemia. * Lamotrigine is known to block sodium channels but it is not known whether it is extracellular or intracellular. * Cannabidiol (CBD) has been shown to cause inhibitory effects on sodium currents. This voltage-dependent inhibition is non-selective in natu ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Estrogen
Estrogen (also spelled oestrogen in British English; see spelling differences) is a category of sex hormone responsible for the development and regulation of the female reproductive system and secondary sex characteristics. There are three major endogenous estrogens that have estrogenic hormonal activity: estrone (E1), estradiol (E2), and estriol (E3). Estradiol, an estrane, is the most potent and prevalent. Another estrogen called estetrol (E4) is produced only during pregnancy. Estrogens are synthesized in all vertebrates and some insects. Quantitatively, estrogens circulate at lower levels than androgens in both men and women. While estrogen levels are significantly lower in males than in females, estrogens nevertheless have important physiological roles in males. Like all steroid hormones, estrogens readily diffuse across the cell membrane. Once inside the cell, they bind to and activate estrogen receptors (ERs) which in turn modulate the expression of many ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Alkaloid
Alkaloids are a broad class of natural product, naturally occurring organic compounds that contain at least one nitrogen atom. Some synthetic compounds of similar structure may also be termed alkaloids. Alkaloids are produced by a large variety of organisms including bacteria, fungus, fungi, Medicinal plant, plants, and animals. They can be purified from crude extracts of these organisms by acid-base extraction, or solvent extractions followed by silica-gel column chromatography. Alkaloids have a wide range of pharmacology, pharmacological activities including antimalarial medication, antimalarial (e.g. quinine), asthma, antiasthma (e.g. ephedrine), chemotherapy, anticancer (e.g. omacetaxine mepesuccinate, homoharringtonine), cholinomimetic (e.g. galantamine), vasodilation, vasodilatory (e.g. vincamine), Antiarrhythmic agent, antiarrhythmic (e.g. quinidine), analgesic (e.g. morphine), antibacterial (e.g. chelerythrine), and anti-diabetic, antihyperglycemic activities (e.g. berb ... [...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 neurological diseases, neurodegenerative, neuro-ophthalmic and cancer. 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, inc ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
