Yohimbine
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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as a treatment for erectile dysfunction, although its reported clinical benefits were modest and it has largely been superseded by the PDE5 inhibitor class of drugs.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 th ...
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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as a treatment for erectile dysfunction, although its reported clinical benefits were modest and it has largely been superseded by the PDE5 inhibitor class of drugs.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 th ...
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Aphrodisiac
An aphrodisiac is a substance that increases sexual desire, sexual attraction, sexual pleasure, or sexual behavior. Substances range from a variety of plants, spices, foods, and synthetic chemicals. Natural aphrodisiacs like cannabis or cocaine are classified into plant-based and non-plant-based substances. There are non-naturally-occurring aphrodisiacs like MDMA and methamphetamine. Aphrodisiacs can be classified by their type of effects (i.e., psychological or physiological). Aphrodisiacs that contain hallucinogenic properties like Bufotenin have psychological effects on a person that can increase sexual desire and sexual pleasure. Aphrodisiacs that contain smooth muscle relaxing properties like yohimbine have physiological effects on a person that can affect hormone levels and increase blood flow. It is possible that the aphrodisiac effect of a substance is due to the placebo effect. Other substances that impede on areas that aphrodisiacs aim to enhance are classified as an ...
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Pausinystalia Johimbe
''Corynanthe johimbe'', synonym ''Pausinystalia johimbe'', common name yohimbe, is a plant species in the family Rubiaceae native to western and central Africa (Nigeria, Cabinda, Cameroon, Congo-Brazzaville, Gabon, Equatorial Guinea). Extracts from yohimbe have been used in traditional medicine in West Africa as an aphrodisiac, called in some languages burantashi, and have been marketed in developed countries as dietary supplements. Synonyms Botanical According to Royal Botanical Gardens Kew, Plants of the World Online, the accepted name is ''Corynanthe johimbe'' K.Schum (first published in Notizbl. Bot. Gart. Berlin-Dahlem 3: 94, 1901) and it has the following recognised synonyms: Homotypic: *''Pausinystalia johimbe'' (K.Schum.) Pierre in Actes Soc. Linn. Bordeaux 61: 130 (1906) *''Pseudocinchona johimbe'' (K.Schum.) A.Chev. in : 266 (1926) Heterotypic: *''Pausinystalia trillesii'' Beille in Actes Soc. Linn. Bordeaux 61: 130 (1906) *''Pausinystalia zenkeri'' W.Brandt in Arch ...
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5-HT1A
The serotonin 1A receptor (or 5-HT1A receptor) is a subtype of serotonin receptor, or 5-HT receptor, that binds serotonin, also known as 5-HT, a neurotransmitter. 5-HT1A is expressed in the brain, spleen, and neonatal kidney. It is a G protein-coupled receptor (GPCR), coupled to the Gi protein, and its activation in the brain mediates hyperpolarisation and reduction of firing rate of the postsynaptic neuron. In humans, the serotonin 1A receptor is encoded by the HTR1A gene. Distribution The 5-HT1A receptor is the most widespread of all the 5-HT receptors. In the central nervous system, 5-HT1A receptors exist in the cerebral cortex, hippocampus, septum, amygdala, and raphe nucleus in high densities, while low amounts also exist in the basal ganglia and thalamus. The 5-HT1A receptors in the raphe nucleus are largely somatodendritic autoreceptors, whereas those in other areas such as the hippocampus are postsynaptic receptors. Function Neuromodulation 5-HT1A receptor ag ...
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Delayed Ejaculation
Delayed ejaculation (DE) describes a man's inability or persistent difficulty in achieving orgasm, despite typical sexual desire and sexual stimulation. Generally, a man can reach orgasm within a few minutes of active thrusting during sexual intercourse, whereas a man with delayed ejaculation either does not have orgasms at all or cannot have an orgasm until after prolonged intercourse which might last for 30–45 minutes or more. Delayed ejaculation is closely related to anorgasmia. In the Diagnostic and Statistical Manual of Mental Disorders (DSM), fifth edition, the definition of DE requires 1 of 2 symptoms: either a marked delay in or a marked infrequency or absence of ejaculation on ''75% to 100%'' of occasions for ''at least 6 months'' of partnered sexual activity without the individual desiring delay, and causing significant distress to the individual. DE is meant to describe any and all of the ejaculatory disorders that result in a delay or absence of ejaculation. The Thir ...
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Alpha-2 Adrenergic Receptor
The alpha-2 (α2) adrenergic receptor (or adrenoceptor) is a G protein-coupled receptor (GPCR) associated with the Gi heterotrimeric G-protein. It consists of three highly homologous subtypes, including α2A-, α2B-, and 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 and peripheral nervous systems. Cellular localization The α2A adrenergic receptor is localised in the following central nervous system (CNS) structures: * Brainstem (especially the locus coeruleus) * Midbrain * Hypothalamus * Hippocampus * Spinal cord * Cerebral cortex * Cerebellum * Septum Whereas the α2B adrenergic receptor is localised in the following CNS structures: * Olfactory system * Thalamus * Pyramidal layer of the hippocampus * Cerebellar Purkinje layer and the α2C adrenergic receptor is localised in the CN ...
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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 * Spegatrine * 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 ... References {{Serotonergics Indoloquinolizines Tryptamine alkaloids Quinolizidine alkaloids Alkaloids found in Rauvolfia Alpha-2 blockers 5-HT1A ag ...
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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
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Alkaloids are produced by a large variety of organisms including , , Medicinal plant, plants, an ...
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5-HT1B
5-hydroxytryptamine receptor 1B also known as the 5-HT1B receptor is a protein that in humans is encoded by the ''HTR1B'' gene. The 5-HT1B receptor is a 5-HT receptor subtype. Tissue distribution and function 5-HT1B receptors are widely distributed throughout the central nervous system with the highest concentrations found in the frontal cortex, basal ganglia, striatum, and the hippocampus. The function of the 5-HT1B receptor differs depending upon its location. In the frontal cortex, it is believed to act as a postsynaptic receptor inhibiting the release of dopamine. In the basal ganglia and the striatum, evidence suggests 5-HT signaling acts on an autoreceptor, inhibiting the release of serotonin and decreasing glutamatergic transmission by reducing miniature excitatory postsynaptic potential (mEPSP) frequency, respectively. In the hippocampus, a recent study has demonstrated that activation of postsynaptic 5-HT1B heteroreceptors produces a facilitation in excitatory synap ...
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Xylazine
Xylazine is a pharmaceutical drug used for sedation, anesthesia, muscle relaxation, and analgesia in animals such as horses, cattle, and other non-human mammals. Veterinarians also use xylazine as an emetic, especially in cats. It is an analog of clonidine and an agonist at the of adrenergic receptor. In veterinary anesthesia, xylazine is often used in combination with ketamine. It is sold under many brand names worldwide, most notably the Bayer brand name Rompun. It is also marketed as Anased, Sedazine, and Chanazine. The drug interactions vary with different animals. It has become a drug of abuse, particularly in Puerto Rico, where it is diverted from stocks used by equine veterinarians and used as a cutting agent for heroin. Medical uses Xylazine is often used as a sedative, muscle relaxant, and analgesic. It is frequently used in the treatment of tetanus. Xylazine is very similar to drugs such as phenothiazine, tricyclic antidepressants, and clonidine. As an anesthetic, i ...
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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 α1-adrenergic and α2-adrenergic receptor antagonist with approximately 10-fold 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 * Ajmalicine * Rauwolscine * Spegatrine * Yohimbine Yohimbine (), also known as quebrachine, is an in ...
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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. See also * Corynanthine * Rauwolscine * Spegatrine * Yo ...
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