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Spegatrine
Spegatrine is an alpha-1 adrenergic receptor, α1- and alpha-2 adrenergic receptor, α2-adrenergic receptor receptor antagonist, antagonist isolated from ''Rauvolfia verticillata''. Its Dimer (chemistry), dimer dispegatrine has greater antagonist affinity (pharmacology), affinity for alpha-adrenergic receptor, α-adrenergic receptors. See also * Ajmalicine * Corynanthine * Rauwolscine * Yohimbine References Alkaloids found in Rauvolfia Alpha-1 blockers Alpha-2 blockers Tryptamine alkaloids Indoloquinolizines Heterocyclic compounds with 5 rings Hydroxyarenes {{Organic-chem-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dispegatrine
Spegatrine is an α1- and α2-adrenergic receptor antagonist isolated from '' Rauvolfia verticillata''. Its dimer dispegatrine has greater antagonist affinity for α-adrenergic receptors. See also * Ajmalicine * Corynanthine * Rauwolscine * Yohimbine Yohimbine, also known as quebrachine, is an indole alkaloid derived from the bark of the African tree '' Pausinystalia johimbe'' (yohimbe); also from the bark of the unrelated South American tree '' Aspidosperma quebracho-blanco''. Yohimbine is ... References Alkaloids found in Rauvolfia Alpha-1 blockers Alpha-2 blockers Tryptamine alkaloids Indoloquinolizines Heterocyclic compounds with 5 rings Hydroxyarenes {{Organic-chem-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Spegatrine 3D
Spegatrine is an α1- and α2-adrenergic receptor antagonist isolated from '' Rauvolfia verticillata''. Its dimer dispegatrine has greater antagonist affinity for α-adrenergic receptors. See also * Ajmalicine * Corynanthine * Rauwolscine * Yohimbine Yohimbine, also known as quebrachine, is an indole alkaloid derived from the bark of the African tree '' Pausinystalia johimbe'' (yohimbe); also from the bark of the unrelated South American tree '' Aspidosperma quebracho-blanco''. Yohimbine is ... References Alkaloids found in Rauvolfia Alpha-1 blockers Alpha-2 blockers Tryptamine alkaloids Indoloquinolizines Heterocyclic compounds with 5 rings Hydroxyarenes {{Organic-chem-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Rauwolscine
Rauwolscine, also known as isoyohimbine, α-yohimbine, and corynanthidine, is an alkaloid found in various species within the genera ''Rauvolfia'' and '' Corynanthe'' (including ''Pausinystalia''). It is a stereoisomer of yohimbine. Rauwolscine is a central nervous system stimulant, a local anesthetic and a vague aphrodisiac. Rauwolscine acts predominantly as a α2-adrenergic receptor antagonist. It has also been shown to function as a 5-HT1A receptor partial agonist and 5-HT2A and 5-HT2B receptor antagonist. See also * Ajmalicine * 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 relat ... * Spegatrine References {{Tryptamines Indoloquinolizines Tryptamine alkaloids Quinolizidine alkaloids Alkaloids found in Rauvolfia Alpha-2 blockers 5-HT1A agonists ... [...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] |
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 liver enzyme, which is responsible for the breakdown of many drugs. Its binding affinity at this receptor is 3.30 nM. Biosynthesis Two moieties are involved in the ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dimer (chemistry)
In chemistry, dimerization is the process of joining two identical or similar Molecular entity, molecular entities by Chemical bond, bonds. The resulting bonds can be either strong or weak. Many symmetrical chemical species are described as dimers, even when the monomer is unknown or highly unstable. The term ''homodimer'' is used when the two subunits are identical (e.g. A–A) and ''heterodimer'' when they are not (e.g. A–B). The reverse of dimerization is often called Dissociation (chemistry), dissociation. When two oppositely-charged ions associate into dimers, they are referred to as ''Bjerrum pairs'', after Danish chemist Niels Bjerrum. Noncovalent dimers Anhydrous carboxylic acids form dimers by hydrogen bonding of the acidic hydrogen and the carbonyl oxygen. For example, acetic acid forms a dimer in the gas phase, where the monomer units are held together by hydrogen bonds. Many OH-containing molecules form dimers, e.g. the water dimer. Dimers that form based on w ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Rauvolfia Verticillata
''Rauvolfia verticillata'', the common devil pepper, is a plant in the family Apocynaceae. The specific epithet ''verticillata'' means 'whorled' and refers to the plant's leaves. Description ''Rauvolfia verticillata'' grows as a shrub or small tree, up to tall. The bark is yellowish black or brown. Inflorescences bear up to 35 or more flowers. The flowers feature a white or pinkish corolla. The fruits are whitish purple when ripe, in shape, measuring up to long. Distribution and habitat ''Rauvolfia verticillata'' is native to China, Taiwan and tropical Asia from India east to the Philippines. It grows in a variety of habitats, including forests and savannas, from sea level to altitude. Uses ''Rauvolfia verticillata'' is used in traditional Chinese medicine, including as a treatment for snakebite, malaria, typhus and hypertension. The root may be locally used as a sedative and the leaves are used in the treatment of wounds. Conservation ''Rauvolfia verticillata'' has been a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Affinity (pharmacology)
In biochemistry and pharmacology, a ligand is a substance that forms a complex with a biomolecule to serve a biological purpose. The etymology stems from Latin ''ligare'', which means 'to bind'. In protein-ligand binding, the ligand is usually a molecule which produces a signal by binding to a site on a target protein. The binding typically results in a change of conformational isomerism (conformation) of the target protein. In DNA-ligand binding studies, the ligand can be a small molecule, ion, or protein which binds to the DNA double helix. The relationship between ligand and binding partner is a function of charge, hydrophobicity, and molecular structure. Binding occurs by intermolecular forces, such as ionic bonds, hydrogen bonds and Van der Waals forces. The association or docking is actually reversible through dissociation. Measurably irreversible covalent bonding between a ligand and target molecule is atypical in biological systems. In contrast to the definition o ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Alpha-adrenergic Receptor
The adrenergic receptors or adrenoceptors are a class of G protein-coupled receptors that are targets of many catecholamines like norepinephrine (noradrenaline) and epinephrine (adrenaline) produced by the body, but also many medications like beta blockers, beta-2 (β2) agonists and alpha-2 (α2) agonists, which are used to treat high blood pressure and asthma, for example. Many cells have these receptors, and the binding of a catecholamine to the receptor will generally stimulate the sympathetic nervous system (SNS). The SNS is responsible for the fight-or-flight response, which is triggered by experiences such as exercise or fear-causing situations. This response dilates pupils, increases heart rate, mobilizes energy, and diverts blood flow from non-essential organs to skeletal muscle. These effects together tend to increase physical performance momentarily. History By the turn of the 19th century, it was agreed that the stimulation of sympathetic nerves could cause diff ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Receptor Antagonist
A receptor antagonist is a type of receptor ligand or drug that blocks or dampens a biological response by binding to and blocking a receptor rather than activating it like an agonist. Antagonist drugs interfere in the natural operation of receptor proteins.Pharmacology Guide: In vitro pharmacology: concentration-response curves ." '' GlaxoWellcome.'' Retrieved on December 6, 2007. They are sometimes called blockers; examples include alpha blockers, beta b ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Alpha-2 Adrenergic Receptor
The alpha-2 (α2) adrenergic receptor (or adrenoceptor) is a G protein-coupled receptor (GPCR) associated with the Gi alpha subunit, Gi heterotrimeric G-protein. It consists of three highly homologous subtypes, including α2A-adrenergic, α2A-, α2B-adrenergic, α2B-, and α2C-adrenergic, α2C-adrenergic. Some species other than humans express a fourth α2D-adrenergic receptor as well. Catecholamines like norepinephrine (noradrenaline) and epinephrine (adrenaline) signal through the α2-adrenergic receptor in the central nervous system, central and peripheral nervous systems. Cellular localization The Alpha-2A adrenergic receptor, α2A adrenergic receptor is localised in the following central nervous system (CNS) structures: * Brainstem (especially the locus coeruleus as presynaptic & somatodendritic autoreceptor ) * Midbrain * Hypothalamus * Olfactory system * Hippocampus * Spinal cord * Cerebral cortex * Cerebellum * Septum Whereas the Alpha-2B adrenergic receptor, α2B adren ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
