|
Ajmalicine
Ajmalicine, also known as δ-yohimbine or raubasine, is an antihypertensive drug used in the treatment of high blood pressure. It has been marketed under numerous brand names including Card-Lamuran, Circolene, Cristanyl, Duxil, Duxor, Hydroxysarpon, Iskedyl, Isosarpan, Isquebral, Lamuran, Melanex, Raunatin, Saltucin Co, Salvalion, and Sarpan. It is an alkaloid found naturally in various plants such as ''Rauvolfia'' spp., '' Catharanthus roseus'', and ''Mitragyna speciosa''. Ajmalicine is structurally related to yohimbine, rauwolscine, and other yohimban derivatives. Like corynanthine, it acts as a α1-adrenergic receptor antagonist with preferential actions over α2-adrenergic receptors, underlying its hypotensive rather than hypertensive effects. Additionally, it is a very strong inhibitor of the CYP2D6 Cytochrome P450 2D6 (CYP2D6) is an enzyme that in humans is encoded by the ''CYP2D6'' gene. ''CYP2D6'' is primarily expressed in the liver. It is also highly expressed ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Mitragyna Speciosa
''Mitragyna speciosa'' (commonly known as kratom, an herbal leaf from a tree of the Rubiaceae family, ) is a tropical evergreen tree in the coffee family native to Southeast Asia. It is indigenous to Thailand, Indonesia, Malaysia, Myanmar, and Papua New Guinea, where it has been used in herbal medicine since at least the nineteenth century. It has also historically been used for chewing, smoking, and tea. Kratom has opioid properties and some stimulant-like effects. , the efficacy and safety of kratom are unclear, and the drug was not approved as a therapeutic agent in the United States due to the poor quality of the research. In 2019, the United States Food and Drug Administration (FDA) stated that there is no evidence that kratom is safe or effective for treating any condition. Some people take it for managing chronic pain, for treating opioid withdrawal symptoms, or for recreational purposes. The onset of effects typically begins within five to ten minutes and l ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Yohimbine
Yohimbine (), also known as quebrachine, is an indole alkaloid derived from the bark of the African tree '' Pausinystalia johimbe''; also from the bark of the unrelated South American tree ''Aspidosperma quebracho-blanco''. Yohimbine is an α2-adrenergic receptor antagonist, and has been used in a variety of research projects. It is a veterinary drug used to reverse sedation in dogs and deer. While yohimbine behaves as an aphrodisiac in some mammals, it does not do so in humans. It has been prescribed as a treatment for erectile dysfunction, although its reported clinical benefits were modest and it has largely been superseded by the PDE5 inhibitor class of drugs. Substances that have purported to be extracts from the yohimbe tree have been marketed as dietary supplements for various purposes, but they contain highly variable amounts of yohimbine, if any; no published scientific evidence supports their efficacy. Uses Yohimbine is a drug used in veterinary medicine to reverse ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Corynanthine
Corynanthine, also known as rauhimbine, is an alkaloid found in the ''Rauvolfia'' and ''Corynanthe'' (including ''Pausinystalia'') genera of plants. It is one of the two diastereoisomers of yohimbine, the other being rauwolscine. It is also related to ajmalicine. Corynanthine acts as an alpha-1 adrenergic receptor, α1-adrenergic and alpha-2 adrenergic receptor, α2-adrenergic receptor receptor antagonist, antagonist with approximately 10-fold binding selectivity, selectivity for the former site over the latter. This is in contrast to yohimbine and rauwolscine which have around 30-fold higher affinity for the α2-adrenergic receptor over the α1-adrenergic receptor. As a result, corynanthine is not a stimulant (or an aphrodisiac for that matter), but a depressant, and likely plays a role in the antihypertensive properties of ''Rauvolfia'' extracts. Like yohimbine and rauwolscine, corynanthine has also been shown to possess some activity at serotonin receptors. See also * Ajmalici ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Yohimban
Yohimban is a chemical compound. It is the base chemical structure of various alkaloids in the ''Rauvolfia'' and ''Corynanthe'' plant genera, including yohimbine, rauwolscine, corynanthine, ajmalicine, reserpine, deserpidine, and rescinnamine Rescinnamine, known by the brand names moderil, cinnasil, and anaprel, is an angiotensin-converting enzyme inhibitor used as an antihypertensive drug. It is a vinca alkaloid obtained from ''Rauvolfia serpentina'' and other species of ''Rauvolf ..., among others. References {{alkaloid-stub Tryptamine alkaloids Quinolizidine alkaloids Heterocyclic compounds with 5 rings ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Yohimbine
Yohimbine (), also known as quebrachine, is an indole alkaloid derived from the bark of the African tree '' Pausinystalia johimbe''; also from the bark of the unrelated South American tree ''Aspidosperma quebracho-blanco''. Yohimbine is an α2-adrenergic receptor antagonist, and has been used in a variety of research projects. It is a veterinary drug used to reverse sedation in dogs and deer. While yohimbine behaves as an aphrodisiac in some mammals, it does not do so in humans. It has been prescribed as a treatment for erectile dysfunction, although its reported clinical benefits were modest and it has largely been superseded by the PDE5 inhibitor class of drugs. Substances that have purported to be extracts from the yohimbe tree have been marketed as dietary supplements for various purposes, but they contain highly variable amounts of yohimbine, if any; no published scientific evidence supports their efficacy. Uses Yohimbine is a drug used in veterinary medicine to reverse ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Corynanthine
Corynanthine, also known as rauhimbine, is an alkaloid found in the ''Rauvolfia'' and ''Corynanthe'' (including ''Pausinystalia'') genera of plants. It is one of the two diastereoisomers of yohimbine, the other being rauwolscine. It is also related to ajmalicine. Corynanthine acts as an alpha-1 adrenergic receptor, α1-adrenergic and alpha-2 adrenergic receptor, α2-adrenergic receptor receptor antagonist, antagonist with approximately 10-fold binding selectivity, selectivity for the former site over the latter. This is in contrast to yohimbine and rauwolscine which have around 30-fold higher affinity for the α2-adrenergic receptor over the α1-adrenergic receptor. As a result, corynanthine is not a stimulant (or an aphrodisiac for that matter), but a depressant, and likely plays a role in the antihypertensive properties of ''Rauvolfia'' extracts. Like yohimbine and rauwolscine, corynanthine has also been shown to possess some activity at serotonin receptors. See also * Ajmalici ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Rauvolfia
''Rauvolfia'' (sometimes spelled ''Rauwolfia'') is a genus of evergreen trees and shrubs, commonly known as devil peppers, in the family Apocynaceae. The genus is named to honor Leonhard Rauwolf. The genus can mainly be found in tropical regions of Africa, Asia, Latin America, and various oceanic islands. Spelling The International Code of Nomenclature for algae, fungi, and plants stipulates that the genus name was established by Carl Linnaeus in his 1753 book ''Species Plantarum'', which cites his earlier description which states in Botanical Latin that the name is dedicated "to Leonhard Rauwolf": "''Leon. Rauvolfio''". Although some subsequent authors hypercorrected the Classical Latin letter "v" to a modern "w", this is not accepted by the code of nomenclature. Chemical constituents ''Rauvolfia serpentina'', commonly known as Indian snakeroot or ''sarpagandha'', contains many indole alkaloids. Medicinal uses Reserpine is an alkaloid first isolated from '' R. serpentina' ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
CYP2D6
Cytochrome P450 2D6 (CYP2D6) is an enzyme that in humans is encoded by the ''CYP2D6'' gene. ''CYP2D6'' is primarily expressed in the liver. It is also highly expressed in areas of the central nervous system, including the substantia nigra. CYP2D6, a member of the cytochrome P450 mixed-function oxidase system, is one of the most important enzymes involved in the metabolism of xenobiotics in the body. In particular, CYP2D6 is responsible for the metabolism and elimination of approximately 25% of clinically used drugs, via the addition or removal of certain functional groups – specifically, hydroxylation, demethylation, and dealkylation. CYP2D6 also activates some prodrugs. This enzyme also metabolizes several endogenous substances, such as hydroxytryptamines, neurosteroids, and both ''m''-tyramine and ''p''-tyramine which CYP2D6 metabolizes into dopamine in the brain and liver. Considerable variation exists in the efficiency and amount of CYP2D6 enzyme produced be ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tryptamine Alkaloids
Tryptamine is an indolamine metabolite of the essential amino acid, tryptophan. The chemical structure is defined by an indole ─ a fused benzene and pyrrole ring, and a 2-aminoethyl group at the second carbon (third aromatic atom, with the first one being the heterocyclic nitrogen). The structure of tryptamine is a shared feature of certain aminergic neuromodulators including melatonin, serotonin, bufotenin and psychedelic derivatives such as dimethyltryptamine (DMT), psilocybin, psilocin and others. Tryptamine has been shown to activate trace amine-associated receptors expressed in the mammalian brain, and regulates the activity of dopaminergic, serotonergic and glutamatergic systems. In the human gut, symbiotic bacteria convert dietary tryptophan to tryptamine, which activates 5-HT4 receptors and regulates gastrointestinal motility. Multiple tryptamine-derived drugs have been developed to treat migraines, while trace amine-associated receptors are being explore ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Quinolizidine Alkaloids
Quinolizidine alkaloids are natural products that have a quinolizidine structure; this includes the lupine alkaloids. Occurrence Quinolizidine alkaloids can be found in the plant family of legumes, especially in papilionaceous plants. While the lupine alkaloids (following their name) can be found in lupines, tinctorin, for example, was isolated from the dyer's broom. Examples More than 200 quinolizidine alkaloids are known which can be classified into 6 structural types: * the lupinine type with 34 known structures, including lupinine and its derivatives * the camoensine type with 6 known structures, including camoensin * the spartein type with 66 structures, including sparteine, lupanine, angustifoline * the α-pyridone type with 25 structures, including anagyrine and cytisine * the matrine type with 31 structures, including matrine * and the ormosanin type with 19 structures, including ormosanine. (–)-Lupinine Structural Formula V2.svg, (–)-lupinine (6R,7S,9S,1 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antihypertensive Agents
Antihypertensives are a class of drugs that are used to treat hypertension (high blood pressure). Antihypertensive therapy seeks to prevent the complications of high blood pressure, such as stroke and myocardial infarction. Evidence suggests that reduction of the blood pressure by 5 mmHg can decrease the risk of stroke by 34% and of ischaemic heart disease by 21%, and can reduce the likelihood of dementia, heart failure, and mortality from cardiovascular disease. There are many classes of antihypertensives, which lower blood pressure by different means. Among the most important and most widely used medications are thiazide diuretics, calcium channel blockers, ACE inhibitors, angiotensin II receptor antagonists (ARBs), and beta blockers. Which type of medication to use initially for hypertension has been the subject of several large studies and resulting national guidelines. The fundamental goal of treatment should be the prevention of the important endpoints of hyperte ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
