Adrenergic alpha-2 Receptor Antagonists
Receptors, Adrenergic, alpha
One of the two major pharmacological subdivisions of adrenergic receptors that were originally defined by the relative potencies of various adrenergic compounds. The alpha receptors were initially described as excitatory receptors that post-junctionally stimulate SMOOTH MUSCLE contraction. However, further analysis has revealed a more complex picture involving several alpha receptor subtypes and their involvement in feedback regulation.
Receptors, Adrenergic, alpha-2
A subclass of alpha-adrenergic receptors found on both presynaptic and postsynaptic membranes where they signal through Gi-Go G-PROTEINS. While postsynaptic alpha-2 receptors play a traditional role in mediating the effects of ADRENERGIC AGONISTS, the subset of alpha-2 receptors found on presynaptic membranes signal the feedback inhibition of NEUROTRANSMITTER release.
Precursor of epinephrine that is secreted by the adrenal medulla and is a widespread central and autonomic neurotransmitter. Norepinephrine is the principal transmitter of most postganglionic sympathetic fibers and of the diffuse projection system in the brain arising from the locus ceruleus. It is also found in plants and is used pharmacologically as a sympathomimetic.
Cell-surface proteins that bind epinephrine and/or norepinephrine with high affinity and trigger intracellular changes. The two major classes of adrenergic receptors, alpha and beta, were originally discriminated based on their cellular actions but now are distinguished by their relative affinity for characteristic synthetic ligands. Adrenergic receptors may also be classified according to the subtypes of G-proteins with which they bind; this scheme does not respect the alpha-beta distinction.
Adrenergic alpha-2 Receptor Agonists
Adrenergic alpha-1 Receptor Antagonists
Drugs that inhibit the actions of the sympathetic nervous system by any mechanism. The most common of these are the ADRENERGIC ANTAGONISTS and drugs that deplete norepinephrine or reduce the release of transmitters from adrenergic postganglionic terminals (see ADRENERGIC AGENTS). Drugs that act in the central nervous system to reduce sympathetic activity (e.g., centrally acting alpha-2 adrenergic agonists, see ADRENERGIC ALPHA-AGONISTS) are included here.
The active sympathomimetic hormone from the ADRENAL MEDULLA. It stimulates both the alpha- and beta- adrenergic systems, causes systemic VASOCONSTRICTION and gastrointestinal relaxation, stimulates the HEART, and dilates BRONCHI and cerebral vessels. It is used in ASTHMA and CARDIAC FAILURE and to delay absorption of local ANESTHETICS.
A mixture of three different hydrogenated derivatives of ERGOTAMINE: DIHYDROERGOCORNINE; DIHYDROERGOCRISTINE; and DIHYDROERGOCRYPTINE. Dihydroergotoxine has been proposed to be a neuroprotective agent and a nootropic agent. The mechanism of its therapeutic actions is not clear, but it can act as an alpha-adrenergic antagonist and a dopamine agonist. The methanesulfonate salts of this mixture of alkaloids are called ERGOLOID MESYLATES.
Sympathetic Nervous System
The thoracolumbar division of the autonomic nervous system. Sympathetic preganglionic fibers originate in neurons of the intermediolateral column of the spinal cord and project to the paravertebral and prevertebral ganglia, which in turn project to target organs. The sympathetic nervous system mediates the body's response to stressful situations, i.e., the fight or flight reactions. It often acts reciprocally to the parasympathetic system.
Dose-Response Relationship, Drug
An ergot derivative that is a congener of LYSERGIC ACID DIETHYLAMIDE. It antagonizes the effects of serotonin in blood vessels and gastrointestinal smooth muscle, but has few of the properties of other ergot alkaloids. Methysergide is used prophylactically in migraine and other vascular headaches and to antagonize serotonin in the carcinoid syndrome.
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A vasodilator that apparently has direct actions on blood vessels and also increases cardiac output. Tolazoline can interact to some degree with histamine, adrenergic, and cholinergic receptors, but the mechanisms of its therapeutic effects are not clear. It is used in treatment of persistent pulmonary hypertension of the newborn.
Receptors, Adrenergic, alpha-1
Parasympathetic Nervous System
The craniosacral division of the autonomic nervous system. The cell bodies of the parasympathetic preganglionic fibers are in brain stem nuclei and in the sacral spinal cord. They synapse in cranial autonomic ganglia or in terminal ganglia near target organs. The parasympathetic nervous system generally acts to conserve resources and restore homeostasis, often with effects reciprocal to the sympathetic nervous system.
Neural modulation of cephalexin intestinal absorption through the di- and tripeptide brush border transporter of rat jejunum in vivo. (1/784)Intestinal absorption of beta-lactamine antibiotics (e.g., cefixime and cephalexin) has been shown to proceed through the dipeptide carrier system. In a previous study, nifedipine (NFP), an L-type calcium channel blocker, enhanced the absorption of cefixime in vivo but not in vitro, and it was suggested that neural mechanisms might be involved in the effect of NFP. The aim of the present study was to assess the involvement of the nervous system on the intestinal absorption of cephalexin (CFX). To investigate this, we used a single-pass jejunal perfusion technique in rats. NFP and diltiazem enhanced approximately 2-fold the plasma levels of CFX in treated rats versus untreated controls. NFP also increased approximately 2-fold the CFX level in portal plasma and increased urinary excretion of CFX, thus indicating that CFX did effectively increase CFX intestinal absorption. Perfusing high concentrations of dipeptides in the jejunal lumen competitively reduced CFX absorption and inhibited the enhancement of CFX absorption produced by NFP. Hexamethonium and lidocaine inhibited the effect of NFP, whereas atropine, capsaicin, clonidine, and isoproterenol enhanced CFX absorption by the same order of magnitude as NFP. Thus, complex neural networks can modulate the function of the intestinal di- and tripeptide transporter. Sympathetic noradrenergic fibers, intestinal sensory neurons, and nicotinic synapses are involved in the increase of CFX absorption produced by NFP. (+info)
Facilitatory beta2-adrenoceptors on cholinergic and adrenergic nerve endings of the guinea pig trachea. (2/784)Using electrical field stimulation of epithelium-denuded intact guinea pig tracheal tube preparations, we studied the presence and role of prejunctional beta2-adrenoceptors by measuring evoked endogenous acetylcholine (ACh) and norepinephrine (NE) release directly. Analysis of ACh and NE was through two HPLC systems with electrochemical detection. Electrical field stimulation (150 mA, 0.8 ms, 16 Hz, 5 min, biphasic pulses) released 29.1 +/- 2.5 pmol ACh/g tissue and 70.2 +/- 6.2 pmol NE/g tissue. Preincubation for 15 min with the selective beta2-adrenoceptor agonist fenoterol (1 microM) increased both ACh and NE overflow to 178 +/- 28 (P < 0.01) and 165 +/- 12% (P < 0.01), respectively, of control values, increases that were abolished completely by the selective beta2-adrenoceptor antagonist ICI-118551 (1 microM). Further experiments with increasing fenoterol concentrations (0.1-100 microM) and different preincubation periods (1, 5, and 15 min) showed a strong and concentration-dependent facilitation of NE release, with maximum response levels decreasing (from nearly 5-fold to only 2.5-fold of control value) with increasing agonist contact time. In contrast, sensitivity of facilitatory beta2-adrenoceptors on cholinergic nerves to fenoterol gradually increased when the incubation period was prolonged; in addition, a bell-shaped concentration-response relationship was found at 15 min of preincubation. Fenoterol concentration-response relationships (15-min agonist preincubation) in the presence of atropine and yohimbine (1 microM each) were similar in the case of NE release, but in the case of ACh release, the bell shape was lost. The results indicate a differential capacity and response time profile of facilitatory prejunctional beta2-adrenoceptors on adrenergic and cholinergic nerve terminals in the guinea pig trachea and suggest that the receptors on adrenergic nerves are more susceptible to desensitization. (+info)
Effects of clonidine on myocardial beta-adrenergic receptor-adenyl cyclase-cAMP system after scalds in rats. (3/784)AIM: To study the role of clonidine (Clo) on the myocardial beta-adrenergic receptor (beta-AR)-adenyl cyclase (AC)-cAMP system after the scalds in rats. METHODS: A 30% skin-full-thickness scald was produced by immersing rats in 95 degrees C water for 9 s. Clo 0.1-3.0 mg.kg-1 was injected i.p. to rats at 30 min before scalds, yohimbine (Yoh) 0.05 mg.kg-1 or prazosin (Pra) 0.03 mg.kg-1 to rats at 30 min before i.p. Clo. beta-AR density and affinity, AC activity, phosphoric diester hydrolases (PDH) activity, and cAMP content were determined with radioreceptor assay, indirect method, enzymeradiochemical assay, and radioimmunoassay, respectively. RESULTS: Clo inhibited the decrease of the myocardial beta-AR density, the attenuation of AC activity, and the reduction of cAMP content at 12 h after the scalds. Yoh partially reversed the effects of Clo on the three parameters. But Pra did not. CONCLUSION: Clo reversed the changes of the myocardial beta-AR-AC-cAMP system resulted from the scalds in rats. (+info)
Differential potentiation of arachidonic acid release by rat alpha2 adrenergic receptor subtypes. (4/784)CHO transfectants expressing the three subtypes of rat alpha2 adrenergic receptors (alpha2AR): alpha2D, alpha2B, alpha2C were studied to compare the transduction pathways leading to the receptor-mediated stimulation of phospholipase A2 (PLA2) in the corresponding cell lines CHO-2D, CHO-2B, CHO-2C. The alpha2B subtype stimulated the arachidonic acid (AA) release after incubation of the cells with 1 microM epinephrine, whereas alpha2D and alpha2C gave no stimulation. Calcium ionophore A23187 (1 microM) increased the release by a factor of 2-4 in the three strains. When cells were incubated with both epinephrine and Ca2+ ionophore, the AA release differed greatly between cell lines with strong potentiation in CHO-2B (2-3 times greater than Ca2+ ionophore alone), moderate potentiation in CHO-2D, and no potentiation in CHO-2C. The three cell lines each inhibited adenylylcyclase with similar efficiencies when 1 microM epinephrine was used as the agonist. The potentiation depended on both alpha2AR and Gi proteins since yohimbine and pertussis toxin inhibited the process. Pretreatment of CHO-2B cells with MAFP which inhibits both cytosolic and Ca2+-independent PLA2, reduced the release of AA induced by epinephrine+Ca2+ ionophore to basal value, whereas bromoenol lactone, a specific Ca2+-independent PLA2 inhibitor, had no effect. Preincubation of the cells with the intracellular calcium chelator BAPTA gave a dose-dependent inhibition of the arachidonic acid (AA) release. In CHO cells expressing the angiotensin II type 1 receptor, coupled to a Gq protein, the agonist (10-7 M) produced maximal AA release: there was no extra increase when angiotensin and Ca2+ ionophore were added together. There was no increase in the amount of inositol 1,4, 5-triphosphate following stimulation of CHO-2B, -2C, -2D cells with 1 microM epinephrine. Epinephrine led to greater phosphorylation of cPLA2, resulting in an electrophoretic mobility shift for all three cell lines, so inadequate p42/44 MAPKs stimulation was not responsible for the weaker stimulation of cPLA2 in CHO-2C cells. Therefore, the stimulation of cPLA2 by Gi proteins presumably involves another unknown mechanism. The differential stimulation of cPLA2 in these transfectants will be of value to study the actual involvement of the transduction pathways leading to maximal cPLA2 stimulation. (+info)
Canine external carotid vasoconstriction to methysergide, ergotamine and dihydroergotamine: role of 5-HT1B/1D receptors and alpha2-adrenoceptors. (5/784)The antimigraine drugs methysergide, ergotamine and dihydroergotamine (DHE) produce selective vasoconstriction in the external carotid bed of vagosympathectomized dogs anaesthetized with pentobarbital and artificially respired, but the receptors involved have not yet been completely characterized. Since the above drugs display affinity for several binding sites, including alpha-adrenoceptors and several 5-HT1 and 5-HT2 receptor subtypes, this study has analysed the mechanisms involved in the above responses. Intracarotid (i.c.) infusions during 1 min of methysergide (31-310 microg min(-1)), ergotamine (0.56-5.6 microg min(-1)) or DHE (5.6-31 microg min(-1)) dose-dependently reduced external carotid blood flow (ECBF) by up to 46+/-4, 37+/-4 and 49+/-5%, respectively. Blood pressure and heart rate remained unchanged. The reductions in ECBF by methysergide were abolished and even reversed to increases in animals pre-treated with GR127935 (10 microg kg(-1), i.v.). The reductions in ECBF by ergotamine and DHE remained unchanged in animals pre-treated (i.v.) with prazosin (300 microg kg(-1)), but were partly antagonized in animals pre-treated with either GR127935 (10 or 30 microg kg(-1)) or yohimbine (1000 microg kg(-1)). Pre-treatment with a combination of GR127935 (30 microg kg(-1)) and yohimbine (1000 microg kg(-1)) abolished the responses to both ergotamine and DHE. The above doses of antagonists were shown to produce selective antagonism at their respective receptors. These results suggest that the external carotid vasoconstrictor responses to methysergide primarily involve 5-HT1B/1D receptors, whereas those to ergotamine and DHE are mediated by 5-HT1B/1D receptors as well as alpha2-adrenoceptors. (+info)
Effects of vasopressin on the sympathetic contraction of rabbit ear artery during cooling. (6/784)In order to analyse the effects of arginine-vasopressin on the vascular contraction to sympathetic nerve stimulation during cooling, the isometric response of isolated, 2-mm segments of the rabbit central ear (cutaneous) artery to electrical field stimulation (1-8 Hz) was recorded at 37 and 30 degrees C. Electrical stimulation (37 degrees C) produced frequency-dependent arterial contraction, which was reduced at 30 degrees C and potentiated by vasopressin (10 pM, 100 pM and 1 nM). This potentiation was greater at 30 than at 37 degrees C and was abolished at both temperatures by the antagonist of vasopressin V1 receptors d(CH2)5 Tyr(Me)AVP (100 nM). Desmopressin (1 microM) did not affect the response to electrical stimulation. At 37 degrees C, the vasopressin-induced potentiation was abolished by the purinoceptor antagonist PPADS (30 microM), increased by phentolamine (1 microM) or prazosin (1 microM) and not modified by yohimbine (1 microM), whilst at 30 degrees C, the potentiation was reduced by phentolamine, yohimbine or PPADS, and was not modified by prazosin. The Ca2+-channel blockers, verapamil (10 microM) and NiCl2 (1 mM), abolished the potentiating effects of vasopressin at 37 degrees C whilst verapamil reduced and NiCl2 abolished this potentiation at 30 degrees C. The inhibitor of nitric oxide synthesis, L-NOARG (100 microM), or endothelium removal did not modify the potentiation by vasopressin at 37 and 30 degrees C. Vasopressin also increased the arterial contraction to the alpha2-adrenoceptor agonist BHT-920 (10 microM) and to ATP (2 mM) at 30 and 37 degrees C, but it did not modify the contraction to noradrenaline (1 microM) at either temperature. These results suggest that in cutaneous (ear) arteries, vasopressin potentiaties sympathetic vasoconstriction to a greater extent at 30 than at 37 degrees C by activating vasopressin V1 receptors and Ca2+ channels at both temperatures. At 37 degrees C, the potentiation appears related to activation of the purinoceptor component and, at 30 degrees C, to activation of both purinoceptor and alpha2-adrenoceptor components of the sympathetic response. (+info)
Recovery of locomotion after ventral and ventrolateral spinal lesions in the cat. II. Effects of noradrenergic and serotoninergic drugs. (7/784)The effects of serotoninergic and noradrenergic drugs (applied intrathecally) on treadmill locomotion were evaluated in two adult cats subjected to a ventral and ventrolateral spinal lesion (T13). Despite the extensive spinal lesion, severely damaging important descending pathways such as the reticulo- and vestibulospinal tracts, both cats recovered quadrupedal voluntary locomotion. As detailed in a previous paper, the locomotor recovery occurred in three stages defined as early period, when the animal could not walk with its hindlimbs, recovery period, when progressive improvement occurred, and plateau period, when a more stable locomotor performance was observed. At this latter stage, the cats suffered from postural and locomotor deficits, such as poor lateral stability, irregular stepping of the hindlimbs, and inconsistent homolateral fore- and hindlimb coupling. The present study aimed at evaluating the potential of serotoninergic and/or noradrenergic drugs to improve the locomotor abilities in the early and late stages. Both cats were implanted chronically with an intrathecal cannula and electromyographic (EMG) electrodes, which allowed determination, under similar recording conditions, of the locomotor performance pre- and postlesion and comparisons of the effects of different drugs. EMG and kinematic analyses showed that norepinephrine (NE) injected in early and plateau periods improved the regularity of the hindlimb stepping and stabilized the interlimb coupling, permitting to maintain constant locomotion for longer periods of time. Methoxamine, the alpha1-agonist (tested only at the plateau period), had similar effects. In contrast, the alpha2-agonist, clonidine, deteriorated walking. Serotoninergic drugs, such as the neurotransmitter itself, serotonin (5HT), the precursor 5-hydroxytryptophan (5HTP), and the agonist quipazine improved the locomotion by increasing regularity of the hindlimb stepping and by increasing the step cycle duration. In contrast, the 5HT1A agonist 8-hydroxy-dipropylaminotetralin (DPAT) caused foot drag in one of the cats, resulting in frequent stumbling. Injection of combination of methoxamine and quipazine resulted in maintained, regular stepping with smooth movements and good lateral stability. Our results show that the effects of drugs can be integrated to the residual voluntary locomotion and improve some of its postural aspects. However, this work shows clearly that the effects of drugs (such as clonidine) may depend on whether or not the spinal lesion is complete. In a clinical context, this may suggest that different classes of drugs could be used in patients with different types of spinal cord injuries. Possible mechanisms underlying the effect of noradrenergic and serotoninergic drugs on the locomotion after partial spinal lesions are discussed. (+info)
Effects of A1-adenosine receptor antagonists on purinergic transmission in the guinea-pig vas deferens in vitro. (8/784)1. Intracellularly recorded excitatory junction potentials (ej.ps) were used to study the effects of adenosine receptor antagonists on neurotransmitter release from postganglionic sympathetic nerve terminals in the guinea-pig vas deferens in vitro. 2. The A1 adenosine receptor antagonists, 8-phenyltheophylline (10 microM) and 8-cyclopentyl-1,3-dipropylxanthine (0.1 microM), increased the amplitude of e.j.ps evoked during trains of 20 stimuli at 1 Hz in the presence, but not in the absence, of the alpha2-adrenoceptor antagonist, yohimbine (1 microM) or the non-selective alpha-adrenoceptor antagonist, phentolamine (1 microM). 3. Adenosine (100 microM) reduced the amplitude of e.j.ps, both in the presence and in the absence of phentolamine (1 microM). This inhibitory effect of adenosine is most likely caused by a reduction in transmitter release as there was no detectable change in spontaneous ej.p. amplitudes. 4. In the presence of phentolamine, application of the adenosine uptake inhibitor, S-(p-nitrobenzyl)-6-thioinosine (0.1 microM), had no effect on ej.p. amplitudes. 5. The phosphodiesterase inhibitor, 3-isobutyl-1-methylxanthine (100 microM), significantly increased the amplitudes of all e.j.ps evoked during trains of 20 stimuli at 1 Hz, both in the presence and in the absence of phentolamine (1 microM). 6. These results suggest that endogenous adenosine modulates neurotransmitter release by an action at prejunctional A1 adenosine receptors only when alpha2-adrenoceptors are blocked. (+info)
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Yohimbine HCL Synonyms: Yohimbin, Corynine, Quebrachin, Quebrachine, Aphrosol, Yohimex, Yohimbe HCL (commonly confused with)What is Yohimbine HCL Powder?Yohimbine is an alkaloid found in Yohimbe, a tall evergreen bark native to Africa. Yohimbine has some exciting possibilities, such as promoting and enhancing erectile function. However, many users primarily take Yohimbine as a fat loss aid.Yohimbine Powder BenefitsYohimbine directly aids weight loss. There are two types of adrenergic receptors, alpha and beta, and depending on which are activated, lipolysis (breakdown of fat) can be either stimulated or inhibited. Activation of the alpha 2 receptors inhibits the release of norepinephrine. This is not good if you are trying to reduce weight. Because alpha 2 receptors activate at lower catecholamine levels than the beta receptors, thermogenesis is basically always turned off. Even during exercise, alpha 2 receptors are still acting to inhibit lipolysis. This is where Yohimbine comes into play. Yohimbine
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In the US, yohimbe preparations are sold as a dietary supplements for enhancing libido, for weight loss and as aids for bodybuilding; but There is virtually no published research on yohimbe which supports these or any other claims.:861 Often, these products explicitly claim to contain yohimbine. Cohen et al. found that samples of brands sold in American brick-and-mortar stores contained highly variable amounts of yohimbine, and sometimes none at all.:368 Labelling claims were often misleading.:368 Similar results have been reported by other laboratories for products sold in the U.S., in other countries and on the internet. One study found that many brands of yohimbe might not derive from the P. johimbe tree in the first place. According to yet another source the yohimbe sold in markets in West Africa, where the tree grows, is frequently adulterated with other species of the genus Pausinystalia; these contain little yohimbine. The amounts of alkaloid ...
Yohimbine - wikidoc
Yohimbine is the principal alkaloid of the bark of the West-African evergreen Pausinystalia yohimbe Pierre (formerly Corynanthe yohimbe), family Rubiaceae (Madder family). There are 31 other yohimbane alkaloids found in Yohimbe. In Africa, yohimbine has traditionally been used as an aphrodisiac. However it is very important to note that while the terms yohimbine, yohimbine hydrochloride, and yohimbe bark extract are related, they are not interchangeable. The active chemical present in yohimbe bark is Yohimbine HCl (indole alkaloid) found in the bark of the Pausinystalia yohimbe tree. However, the levels of yohimbine that are present in yohimbe bark extract are variable and often very low. Therefore, although yohimbe bark has been used traditionally to reduce male erectile dysfunction, there is not enough scientific evidence to form a definitive conclusion in this area. ...
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Transdermal application as a viable alternative? About five to ten years ago fat loss gels and cremes were all the rage in the fitness community. These days, however, many topicals carve out a miserable existence in the clearance section of the average supplement store. Wrongfully, if you put some faith into the results Frank L. Greenway and George A. Bray from the UCLA School of Medicine, and the University of Southern California present in a paper from the late 1980s (Greenway. 1987). The results of the corresponding experiments do yet only confirm that it is likely that yohimbine makes an excellent adjunct to a cream thats based on the combination of a beta stimulator with a phosphodiesterase inhibitor (forskolin and aminophylline + yohimbine) - a combination of which Greenway & Bray found that it reduces the thigh circumference by an additonal 2.03 ± 1.36 cm compared to diet alone. The effects of yohimine, alone (dosed at 10mmol/L), which were tested in a seperate experiment, were ...
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Yohimbine is an alkaloid found in Yohimbe, a tall evergreen bark native to Africa. Yohimbine has some exciting possibilities, such as promoting and enhancing erectile function and vasodilation for vascularity. However, many users primarily take Yohimbine as a direct aid for fat loss. There are two types of adrenergic receptors, alpha and beta, and depending on which are activated, lipolysis (breakdown of fat) can be either stimulated or inhibited. Activation of the alpha 2 receptors inhibits the release of norepinephrine. This is not good if you are trying to reduce weight. Because alpha 2 receptors activate at lower catecholamine levels than the beta receptors, thermogenesis is basically always turned off. Even during exercise, alpha 2 receptors are still acting to inhibit lipolysis. This is where Yohimbine comes into play. Yohimbine is a selective alpha 2 antagonist and can short circuit this feedback loop, maximizing norepinephrine levels, and leading to maximized fat loss.. ...
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The transdermal formula in LipoBurn is specifically designed to help you lose weight. This is because it specifically targets stores of fat in the body. The thermogenic properties of LipoBurn send lipolytic agents directly to these stores. The agents invade the cells and destroy them allowing you to lose weight in the process! The LipoBurn formula is comprised of specific ingredients that target the fat cells and keep your body healthy in the process. Yohimbine is just one part of LipoBurn. This ingredient serves as an antioxidant. Yohimbine is an adrenergic antagonist of alpha-2. It works to increase the activity of the nervous system while increasing epineprhine levels. Yohimbine is used as a fat burning supplement because it has transdermal properties. Synephrine is an adrenergic agonist of beta-1. This aids in the break down of fat deposits through the process of lipolysis. Synephrine is a known appetite suppressant and like Yohimbine contains thermogenic
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Ample experimental evidence supports the existence of two distinct types of vasoconstrictor α-adrenoceptors in vascular smooth muscle at postjunctional sites, showing similarities with α1 and α2-adrenoceptors. Especially in vivo, the characterization of an α2-adrenoceptor mediating an increase in diastolic pressure has been most successful. In this respect the model of the pithed rat has been employed most frequently (for reviews see [1, 2]).. At present, the agents cirazoline, (−) phenylephrine, (±)-erythro-methoxamine, (−)-amidephrine, SKF89748, St587 and Sgd 101/75 fulfil the criteria for selective α1-adrenoceptor agonists; their log dose-vasopressor effect curves are virtually unaffected by previous treatment with yohimbine or rauwolscine (selective dose in pithed rats: 1 mg/kg), whereas prazosin (selective dose in pithed rats: 0.1 mg/kg) causes an appreciable parallel rightward displacement. The reverse holds true for the stimulants B-HT 920, B-HT 933, B-HT 958, UK-14304, ...
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Package insert-style information on the drug; covers clinical pharmacology, indications, side effects, and drug interactions. ...
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Yohimbine is sold by prescription under the names of Aphrodyne, Yocon and Yohimex in 5.4 milligram (mg) capsules. Natural food stores carry the natural bark, which has an unspecified amount of the active ingredient yohimbine. The usual dosage is 18 mg daily, but one study used 42 mg. (Journal of Urology 141:1360, 1989). In this trial, 34 percent of men with Serious physical problems, such as advanced atherosclerosis and diabetes, were helped. There are no serious side effects reported from its use ...
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Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking this medicine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.. Using this medicine with any of the following medicines may cause an increased risk of certain side effects, but using both drugs may be the best treatment for you. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.. ...
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Possible involvement of central adrenaline neurons in vasomotor and respiratory control. Studies with clonidine and its...
Possible involvement of central adrenaline neurons in vasomotor and respiratory control. Studies with clonidine and its interactions with piperoxane and yohimbine
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"Yohimbine". DrugBank. Archived from the original on 30 January 2013. Retrieved 12 February 2013. Fattorusso, p. 53 Thomas ... including morphine and yohimbine are very slightly water-soluble (0.1-1 g/L). Alkaloids and acids form salts of various ...
"Yohimbine (PIM 567)". Inchem.org. Retrieved 2013-05-26. Winsauer PJ, Rodriguez FH, Cha AE, Moerschbaecher JM (January 1999). " ... Arthur JM, Casañas SJ, Raymond JR (June 1993). "Partial agonist properties of rauwolscine and yohimbine for the inhibition of ... Kaumann AJ (June 1983). "Yohimbine and rauwolscine inhibit 5-hydroxytryptamine-induced contraction of large coronary arteries ... Tiospirone Trazodone Trifluoromethylphenylpiperazine Trimethoxyamphetamine Umespirone Urapidil Vilazodone Xaliproden Yohimbine ...
Adrenergic blocking agent
Tam, S. W.; Worcel, M.; Wyllie, M. (2001-09-01). "Yohimbine: a clinical review". Pharmacology & Therapeutics. 91 (3): 215-243. ... Phenoxybenzamine Phentolamine Prazosin Tamsulosin Yohimbine Propranolol Timolol Atenolol Metoprolol Butaxamine Still under ...
List of dopaminergic drugs
Yohimbine Piperazines: DBL-583 • GBR-12,935 • Nefazodone • Vanoxerine Piperidines: 1-(1-(1-Benzothiophen-2-yl)cyclohexyl) ...
Eugene van Tamelen
He led a team who were the first persons to achieve the total synthesis of yohimbine. He pioneered in what is today called ... "The Total Synthesis of Yohimbine". J. Am. Chem. Soc. 80 (18): 5006-5007. doi:10.1021/ja01551a062. E. E. van Tamelen "The Role ...
Jacobsen, E. N.; Dustin, J. M.; Zuend, S. J. (November 2008). "Catalytic asymmetric total synthesis of (+)-Yohimbine". Org. ... In the Jacobsen synthesis of (+)-yohimbine, an indole alkaloid, an early enantioselective Pictet-Spengler reaction using a ...
Ajmalicine Corynanthine Spegatrine Yohimbine KOHLI JD, DE NN (June 1956). "Pharmacological action of rauwolscine". Nature. 177 ... Arthur JM, Casañas SJ, Raymond JR (June 1993). "Partial agonist properties of rauwolscine and yohimbine for the inhibition of ... Rauwolscine, also known as isoyohimbine, α-yohimbine, and corynanthidine, is an alkaloid found in various species within the ... Perry BD, U'Prichard DC (December 1981). "[3H]rauwolscine (alpha-yohimbine): a specific antagonist radioligand for brain alpha ...
... , also known as δ-yohimbine or raubasine, is an antihypertensive drug used in the treatment of high blood pressure. ... Corynanthine Rauwolscine Spegatrine Yohimbine Wink, Michael; Roberts, M. W. (1998). Alkaloids: biochemistry, ecology, and ... Ajmalicine is structurally related to yohimbine, rauwolscine, and other yohimban derivatives. Like corynanthine, it acts as a ...
Yohimbine was used for the treatment of erectile dysfunction in men until emergence of more efficient drugs. Some alkaloids ... Yohimbine is more selective to α2 adrenoceptor; by blocking presynaptic α2-adrenoceptors, it increases the release of ... Strictosidine Catharanthine Yohimbine Vinca Strychnine Ellipticine There are also purely structural classifications based on ...
Total synthesis of (±)-reserpine and (±)-α-yohimbine". Journal of the American Chemical Society. 109 (20): 6124-6134. doi: ...
Recreational drug use
... yohimbine (Procomil; a tryptamine alkaloid found in Pausinystalia johimbe) Alcohol: "Euphoria, the feeling of well-being, has ... yohimbine and corynanthine many others Fungi: psilocybin mushrooms: psilocybin and psilocin various Amanita mushrooms: muscimol ...
Yohimbine has been shown to be effective in the treatment of orgasmic dysfunction in men. Meditation has demonstrated ... Adeniyi AA, Brindley GS, Pryor JP, Ralph DJ (May 2007). "Yohimbine in the treatment of orgasmic dysfunction". Asian Journal of ...
The NIH states that yohimbine hydrochloride has been shown in human studies to be possibly effective in the treatment of male ... Retrieved 13 December 2010.[dead link] Adeniyi AA, Brindley GS, Pryor JP, Ralph DJ (May 2007). "Yohimbine in the treatment of ... Cyproheptadine, buspirone, stimulants such as amphetamines (including the antidepressant bupropion), nefazodone and yohimbine ...
Conophylline Vobtusine Rauwolscine Yohimbine Dewick, Paul M (2002). Medicinal Natural Products. A Biosynthetic Approach. Second ...
Like yohimbine and rauwolscine, corynanthine has also been shown to possess some activity at serotonin receptors. Ajmalicine ... Dual effects of yohimbine, rauwolscine and corynanthine as alpha-adrenoceptor antagonists and 5-HT-receptor agonists". Naunyn- ... This is in contrast to yohimbine and rauwolscine which have around 30-fold higher affinity for the α2-adrenergic receptor over ... It is one of the two diastereoisomers of yohimbine, the other being rauwolscine. It is also related to ajmalicine. Corynanthine ...
Yohimbine, an α2 blocker derived from the bark of the Pausinystalia johimbe tree, has been tested to increase libido and treat ... Yohimbine can interact with stimulants, hypertension drugs, naloxone, and clonidine. Interactions with such drugs can cause ... Conversely, α2 blockers, such as Yohimbine, appear to provide significant improvement of the sclerotic symptoms in Raynaud's ... Alpha blockers that may have these side effects include yohimbine, phenoxybenzamine, and phentolamine. When alpha blockers are ...
"Erowid Yohimbe Vaults : Notes on Yohimbine by William White, 1994". Erowid.org. Archived from the original on 2013-01-26. ...
Alpha-2C adrenergic receptor
Bavadekar SA, Ma G, Mustafa SM, Moore BM, Miller DD, Feller DR (November 2006). "Tethered yohimbine analogs as selective human ... 2-phenoxy-nicotinamide Quetiapine Risperidone Spiroxatrine Yohimbine derivatives 9 and 10: >43 fold selectivity over α2A, α2B ...
Yohimbine specifically has so been declared by the European Union, but not by the US National Institutes of Health.[additional ... The main phytochemical in the extract is the indoloquinolizidine alkaloid yohimbine. It also contains other alkaloids, such as ... and yohimbine levels may vary substantially among supplement products. Although proposed as a potential treatment for erectile ... citation(s) needed] Coffea Mitragyna speciosa List of herbs with known adverse effects Yohimbine "Corynanthe johimbe K.Schum ...
Lipokinetix also contained norephedrine (PPA), caffeine, yohimbine and 3,5-diiodothyronine. Usnic acid has been found to have ... The product contains norephedrine (also known as phenylpropanolamine or PPA), caffeine, yohimbine, diiodothyronine, and sodium ...
Ajmalicine Corynanthine Deserpidine Mitragynine Rauwolscine Spegatrine Reserpine Rescinnamine Yohimbine Elisabetsky, E; Costa- ...
Yohimbine, historically used as an aphrodisiac, is sometimes used in veterinary medicine (although now largely replaced by ... yohimbine, and rauwolscine, phentolamine. Lemke, KA (June 2004). "Perioperative use of selective alpha-2 agonists and ...
Cohen PA, Wang YH, Maller G, DeSouza R, Khan IA (March 2016). "Pharmaceutical quantities of yohimbine found in dietary ... Some botanical supplements include high dosages of compounds found in plants with stimulant effects including yohimbine and ...
Yohimbine, an α2 adrenergic receptor antagonist, has been used to decrease glucose levels to a healthy level. In clinical ... Combining yohimbine and 4-aminopyridine in an effort to antagonize xylazine is superior as compared to the administration of ... Ndeereh DR, Mbithi PM, Kihurani DO (June 2001). "The reversal of xylazine hydrochloride by yohimbine and 4-aminopyridine in ... yohimbine, atropine, orciprenaline, metoclopramide, ranitidine, metoprolol, enoxaparin, flucloxacillin, insulin, and irrigation ...
Yohimbine, harmine, haramaline and ajmalicine occurs in descending order, yohimbine being highest. The tobacco plant readily ...
Yohimbine can be used as an antidote to rapidly reverse the effects. Spadavecchia C, Arendt-Nielsen L, Andersen OK, ...
For example, one of the common reported side effects of the intake of yohimbine is piloerection. Piloerection is one of the ... Goldberg, M R (1983). "Influence of yohimbine on blood pressure, autonomic reflexes, and plasma catecholamines in Humans". ...
Alpha-2B adrenergic receptor
Petrash AC, Bylund DB (Jun 1986). "Alpha-2 adrenergic receptor subtypes indicated by [3H]yohimbine binding in human brain". ... Agonists (−)-Dibromophakellin Antagonists Imiloxan Yohimbine Adrenergic receptor GRCh38: Ensembl release 89: ENSG00000274286 - ...
Yohimbine may also be used in an emergency situation, but is not licensed. Medetomidine can be used as an antifouling substance ...
Other indole alkaloids found in Rauvolfia include reserpine, ajmalicine, serpentine, corynanthine, and yohimbine. While 86 ...
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Yohimbine Hydrochloride) may treat, side effects, dosage, drug interactions, warnings, patient labeling, reviews, and related ... Yohimbine is a 3alpha -15alpha -20beta -17alpha -hydroxy Yohimbine-16alpha - carboxylic acid methyl ester. The alkaloid is ... Yohimbine exerts a stimulating action on the mood and may increase anxiety. Such actions have not been adequately studied or ... Yohimbine readily penetrates the CNS and produces a complex pattern of responses in lower doses than required to produce ...
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- So it is more information which is currently available for you to choose from, clenbuterol yohimbine stack. (xdstudios.net)
- In a stack with beta-2 agonist Clenbuterol, alpha-2 antagonist Yohimbine leave pretty much zero chances to your fat tissue. (roids101.com)
- Do not exceed the recommended dosage for Yohimbine as an overdose could, in extreme cases, result in death. (supplementxpress.com)
- Start with the minimum dosage - 20 mcg for clenbuterol, for yohimbine - just 5 mg will be enough for starters. (roids101.com)
- Yohimbine HCl is an a2 antagonist. (nutrithority.com)
- Yohimbine is an alpha receptor antagonist. (damagedstudios.com)
- Moreover, as a natural antagonist to A2-receptors, yohimbine may also enhance one's ability to burn fat. (morningsteel.com)
- Does Yohimbine Boost Testosterone Levels? (morningsteel.com)
- Yocon (yohimbine hydrochloride) blocks presynaptic alpha-2 adrenergic receptors. (rxlist.com)
- Yohimbine works on the alpha receptors. (tigerfitness.com)
- Since alpha receptors inhibit fat breakdown, and Yohimbine HCl inhibits alpha receptors, the net result is that you get an INCREASE in fat breakdown. (tigerfitness.com)
- Yohimbine HCl helps to turn those alpha receptors off, so that fat can be burned from those areas just as easily as the rest of your body. (nutrithority.com)
- This can be particularly compelling when combined with studies showing that Yohimbine may modulate the adrenergic receptors of the subject's fat cells. (morningsteel.com)
- Yohimbine can block the alpha-2 adrenergic receptors, which play a role inr storing fat. (betterme.world)
- The reason for this is unclear, but it may be due to the fact that yohimbine can block the alpha-2 adrenergic receptors. (betterme.world)
- Yohimbine is an indolalkylamine alkaloid with chemical similarity to reserpine. (rxlist.com)
- Yohimbine alkaloid, which acts as an aphrodisiac. (buyyohimbine.com)
- When you actually break it down, yohimbine is a powerful alkaloid, which means that some pharmacologic effect is almost guaranteed. (morningsteel.com)
- We want the Yohimbine HCl-the ACTIVE EXTRACT-- not yohimbe bark which tends to not be accurately dosed. (tigerfitness.com)
- Yohimbine is a substance found in the bark of the Pausinystalia yohimbe tree, which is native to central Africa. (betterme.world)
- The supplement yohimbine is derived from the bark of the yohimbe tree which is native to Africa, where its bark has been used for centuries in traditional medicine there. (betterme.world)
- Yohimbine is an herbal supplement extracted from the bark of the Pausinystalia johimbe tree. (moreforce.com)
- Yohimbine comes from the bark of a West African evergreen tree and it has been used as ED treatment for 70 years already. (viagrafor.com)
- For example, one study had 20 top-level male soccer players take yohimbine extract at doses of 20 mg a day for three weeks (while another group ingested a placebo). (morningsteel.com)
- Take enough yohimbe extract to provide 5-20 milligrams of yohimbine per dose, 2-3 times per day, with one of those doses 30-60 minutes before workouts on training days. (bodybuildingfocus.com)
- Yohimbine is a substance from the alkaloids class. (roids101.com)
- A common substance in Extenze - yohimbine - is associated with a rare type of heart failure. (moreforce.com)
- Yohimbine readily penetrates the CNS and produces a complex pattern of responses in lower doses than required to produce peripheral alpha-adrenergic blockade. (rxlist.com)
- Yohimbine is considered safe when taken in small doses. (betterme.world)
- Known to be extremely quick-acting (within 30 minutes), yohimbine primarily works by increasing the size and flow of blood vessels (vasodilation) through increased nitric oxide production and by stimulating the pituitary gland in the brain to produce adrenaline and noradrenaline. (supplementxpress.com)
- It contains just the right amount of L-Citrulline, Nitrosigine, Yohimbine, and Vitamin C to boost nitric oxide production, increase drive, and enhance blood flow. (uncrate.com)
- As I was discussing with Joe Daniels of Swing This Kettlebells, Yohimbine HCl's effects work the best in the absence of insulin, and its effects start to diminish the more insulin is present. (tigerfitness.com)
- The combination of both increased blood flow and energy contribute to yohimbine HCL's effectiveness to help maintain a healthy heart, but yohimbe also has been shown to decrease fat synthesis in the body by increasing fatty acid mobilization. (hitechpharma.com)
- Each compressed tablet contains (1/12 gr.) 5.4 mg of Yohimbine Hydrochloride. (rxlist.com)
- Yocon (yohimbine hydrochloride) is indicated as a sympathicolytic and mydriatic. (rxlist.com)
- So that means a 220lb bodybuilder (divide by 2.2 to get Kg) is 100Kg and would work up to a dose of 20mg of Yohimbine HCl, or eight capsules of MTS Nutrition Yohimbine HCl. (tigerfitness.com)
- Luckily, MOST side effects are dose-dependent, so you're relatively safe if you won't abuse Clenbuterol or Yohimbine. (roids101.com)
- When it comes to taking yohimbine for weight loss, there is no standard dose. (betterme.world)
- Research also suggests that the effects of Yohimbine supplementation for both men and women can be continually sustained with little, if any, drop in effectiveness for periods up to 14 days and maybe even longer. (supplementxpress.com)
- Health Canada had extended a warning on dietary supplement products being sold in Canada with Natural Products Numbers and containing illegal ingredients such as yohimbine and sildenafil analogues. (nutraingredients-usa.com)
- yohimbine HCl appetite suppressant In this, the same way, and most active ingredients provide other benefits for a few days. (cnrs.fr)
- Some products may not contain pure yohimbine, and may also contain other ingredients that can cause side effects. (betterme.world)
- Warning: Because it has stimulating effects, don't combine yohimbine with other stimulants like caffeine or weight loss pills. (vmnutrition.com)
- No coffee or other drinks containing caffeine while you're on Clenbuterol and Yohimbine. (roids101.com)
- Just because supplements like caffeine and yohimbine can help to free up more fat from your fat cells doesn't necessarily mean that that fat will be burned off for good. (bodybuildingfocus.com)
- Used for centuries as an aphrodisiac, western medicine has recently recognized Yohimbine as a powerful all-natural alternative for decreasing erectile dysfunction and increasing sexual performance - especially for older men. (supplementxpress.com)
- Not only is to spower the ability to ensure you feel hungry, yohimbine HCl appetite suppressant but there are some substances that you're only aware of those substances. (cnrs.fr)
- Bonjour en parcourant le net, j'ai trouvé une formule utilisant : clenbuterol, t3 et yohimbine si pour les deux premières substances c'est. (damagedstudios.com)
- Selective agonists and antagonists for 5-hydroxytriptamine receptor subtypes, and interactions with yohimbine and FG 7142 using the elevated plus-maze test in rats. (bvsalud.org)
- Our Yohimbine HCL is a 2 in 1 formula (sex stimulant + natural fat burner) which provides enhanced blood flow, increased endurance, and improvements in mood and well-being. (vmnutrition.com)
- There is a slight stimulant effect from Yohimbine HCl but it is very mild for most people. (nutrithority.com)
- Yohimbine works by widening blood vessels and increasing blood flow in the body. (hitechpharma.com)
- By increasing blood flow and increasing genital sensitivity, Yohimbine has been shown in studies to promote sexual desire, satisfaction, and quality of erection while aroused. (supplementxpress.com)
- weight loss pills in Houston Products Appetite is a natural fiber that helps yohimbine HCl appetite suppressant to reduce body fat fuel. (cnrs.fr)
- Chrissy Teigen diet pills that yohimbine HCl appetite suppressant sold with the formula may be instead of swallowing the best weight loss pills for women. (cnrs.fr)
- Yohimbine promotes weight loss by affecting the alpha 2-adrenoceptors, which block the release of fat. (roids101.com)
- It's no surprise that people are curious about the weight loss benefits of yohimbine. (betterme.world)
- More recently, yohimbine has been gaining popularity as a weight loss aid. (betterme.world)
- The theory behind the weight loss effect of yohimbine is that it is thought to help to release stored fat from your fat cells . (betterme.world)
- A few studies have looked at the effects of yohimbine on weight loss. (betterme.world)
- However, not all research has shown that yohimbine is effective for weight loss. (betterme.world)
- It's also important to note that most of the research on yohimbine for weight loss has been done with short-term studies. (betterme.world)
- 1 pack of yohimbine 50 tablets (5mg) yohimbine hcl. (damagedstudios.com)
- Yohimbine has been used as a mydriatic and in the treatment of impotence. (charmhtml.com)
- The reason Yohimbine is banned in some countries is due to less scrupulous brands inaccurate product labeling and dosing which can potentially cause side effects. (priceplow.com)
- Yohimbine, which is a chemical derived from the Yohimbe root barks, has been approved by the Food and Drug Administration (FDA) as an oral treatment for erectile dysfunction. (buyyohimbine.com)
- Efficacy and Safety of Oral Combination of Yohimbine and L-arginine (SX) for the Treatment of Erectile Dysfunction: a multicenter, randomized, double blind, placebo-controlled clinical trial. (priceplow.com)
- Yohimbine HCl vyrábaný spoločnosťou USA Supplements LLC* patrí do kategórie výživových a predtréningových doplnkov s primárnou funkciou spaľovača tukov . (americansupplements.eu)
- https://musclebody.sk/usa-produkty/117-usa-supplements-llc-yohimbine-hcl-10-mg-200-kapsul.html">USA Supplements LLC. (musclebody.sk)
- NutraKey's Yohimbine is a premium-grade supplement designed for maximum bioavailability and absorption. (supplementxpress.com)
- Yohimbine is available in powder form or as a supplement . (betterme.world)
- One study from 1991 looked at the effects of yohimbine on 20 obese women who were all placed on a very low calorie diet. (betterme.world)
- Relationship of cytochrome P450 pharmacogenetics to the effects of yohimbine on gastrointestinal transit and catecholamines in healthy subjects. (cdc.gov)
- The formula is an energy boosting effect, and helps to make you lose weight easier yohimbine HCl appetite suppressant and lose weight easily. (cnrs.fr)
- yohimbine HCl appetite suppressant keto diet fat burning pills to provide you with enough energy boosting thermogenic storage and burn fat. (cnrs.fr)
- how to yohimbine HCl appetite suppressant lose weight in 2 days naturally, I've used to read the first one pill and a few weeks, I mentioned it a period of time. (cnrs.fr)
- On the flip side, yohimbine might actually worsen anxiety in people who suffer frequent bouts of panic. (morningsteel.com)
- Yohimbine may also cause anxiety or jitters in some people. (betterme.world)
- Yohimbine HCl acts as an alpha receptor blocker. (tigerfitness.com)
- What you can do is take the Yohimbine HCl DURING your weight training workout 15-20 minutes before you are done. (tigerfitness.com)
- According to one study , the yohimbine interferes with what's known as the "noradrenaline system feedback loop. (morningsteel.com)
- Interestingly, they didn't see any effect of yohimbine on lipolysis in this study. (betterme.world)
- This occurs from a 2017 study diagnosed in a man who had overdosed on yohimbine  . (moreforce.com)