The number of times the HEART VENTRICLES contract per unit of time, usually per minute.
The process by which PAIN is recognized and interpreted by the brain.
The farthest or outermost projections of the body, such as the HAND and FOOT.
Voluntary authorization, by a patient or research subject, with full comprehension of the risks involved, for diagnostic or investigative procedures, and for medical and surgical treatment.
The 10th cranial nerve. The vagus is a mixed nerve which contains somatic afferents (from skin in back of the ear and the external auditory meatus), visceral afferents (from the pharynx, larynx, thorax, and abdomen), parasympathetic efferents (to the thorax and abdomen), and efferents to striated muscle (of the larynx and pharynx).
Primarily a technique of group psychotherapy which involves a structured, directed, and dramatized acting out of the patient's personal and emotional problems.
The ENTERIC NERVOUS SYSTEM; PARASYMPATHETIC NERVOUS SYSTEM; and SYMPATHETIC NERVOUS SYSTEM taken together. Generally speaking, the autonomic nervous system regulates the internal environment during both peaceful activity and physical or emotional stress. Autonomic activity is controlled and integrated by the CENTRAL NERVOUS SYSTEM, especially the HYPOTHALAMUS and the SOLITARY NUCLEUS, which receive information relayed from VISCERAL AFFERENTS.
Disorders related or resulting from use of cocaine.
An alkaloid ester extracted from the leaves of plants including coca. It is a local anesthetic and vasoconstrictor and is clinically used for that purpose, particularly in the eye, ear, nose, and throat. It also has powerful central nervous system effects similar to the amphetamines and is a drug of abuse. Cocaine, like amphetamines, acts by multiple mechanisms on brain catecholaminergic neurons; the mechanism of its reinforcing effects is thought to involve inhibition of dopamine uptake.
Timed test in which the subject must read a list of words or identify colors presented with varying instructions and different degrees of distraction. (Campbell's Psychiatric Dictionary. 8th ed.)
An act performed without delay, reflection, voluntary direction or obvious control in response to a stimulus.
Non-invasive method of demonstrating internal anatomy based on the principle that atomic nuclei in a strong magnetic field absorb pulses of radiofrequency energy and emit them as radiowaves which can be reconstructed into computerized images. The concept includes proton spin tomographic techniques.
A single nucleotide variation in a genetic sequence that occurs at appreciable frequency in the population.
Signals for an action; that specific portion of a perceptual field or pattern of stimuli to which a subject has learned to respond.
A response by the BARORECEPTORS to increased BLOOD PRESSURE. Increased pressure stretches BLOOD VESSELS which activates the baroreceptors in the vessel walls. The net response of the CENTRAL NERVOUS SYSTEM is a reduction of central sympathetic outflow. This reduces blood pressure both by decreasing peripheral VASCULAR RESISTANCE and by lowering CARDIAC OUTPUT. Because the baroreceptors are tonically active, the baroreflex can compensate rapidly for both increases and decreases in blood pressure.
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.
Receptors in the vascular system, particularly the aorta and carotid sinus, which are sensitive to stretch of the vessel walls.
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.
The dilated portion of the common carotid artery at its bifurcation into external and internal carotids. It contains baroreceptors which, when stimulated, cause slowing of the heart, vasodilatation, and a fall in blood pressure.
A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company.
Systemic inflammatory response syndrome with a proven or suspected infectious etiology. When sepsis is associated with organ dysfunction distant from the site of infection, it is called severe sepsis. When sepsis is accompanied by HYPOTENSION despite adequate fluid infusion, it is called SEPTIC SHOCK.
The portion of the descending aorta proceeding from the arch of the aorta and extending to the DIAPHRAGM, eventually connecting to the ABDOMINAL AORTA.
Drugs that act locally on cutaneous or mucosal surfaces to produce inflammation; those that cause redness due to hyperemia are rubefacients; those that raise blisters are vesicants and those that penetrate sebaceous glands and cause abscesses are pustulants; tear gases and mustard gases are also irritants.
A pathological condition manifested by failure to perfuse or oxygenate vital organs.
Sepsis associated with HYPOTENSION or hypoperfusion despite adequate fluid resuscitation. Perfusion abnormalities may include, but are not limited to LACTIC ACIDOSIS; OLIGURIA; or acute alteration in mental status.
A disturbance in the prooxidant-antioxidant balance in favor of the former, leading to potential damage. Indicators of oxidative stress include damaged DNA bases, protein oxidation products, and lipid peroxidation products (Sies, Oxidative Stress, 1991, pxv-xvi).
Laws and regulations, pertaining to the field of veterinary medicine, proposed for enactment or enacted by a legislative body.
A personality disorder characterized by the avoidance of accepting deserved blame and an unwarranted view of others as malevolent. The latter is expressed as suspiciousness, hypersensitivity, and mistrust.
A disease of the eye in which the eyelashes abnormally turn inwards toward the eyeball producing constant irritation caused by motion of the lids.
The moral and ethical bases of the protection of animals from cruelty and abuse. The rights are extended to domestic animals, laboratory animals, and wild animals.
An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS.
Images used to comment on such things as contemporary events, social habits, or political trends; usually executed in a broad or abbreviated manner.
A voluntary organization concerned with the prevention and treatment of heart and vascular diseases.
A subclass of alpha-adrenergic receptors that mediate contraction of SMOOTH MUSCLE in a variety of tissues such as ARTERIOLES; VEINS; and the UTERUS. They are usually found on postsynaptic membranes and signal through GQ-G11 G-PROTEINS.
Works containing information articles on subjects in every field of knowledge, usually arranged in alphabetical order, or a similar work limited to a special field or subject. (From The ALA Glossary of Library and Information Science, 1983)
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.
Drugs that bind to and block the activation of ADRENERGIC ALPHA-1 RECEPTORS.
A subclass of beta-adrenergic receptors (RECEPTORS, ADRENERGIC, BETA). The adrenergic beta-2 receptors are more sensitive to EPINEPHRINE than to NOREPINEPHRINE and have a high affinity for the agonist TERBUTALINE. They are widespread, with clinically important roles in SKELETAL MUSCLE; LIVER; and vascular, bronchial, gastrointestinal, and genitourinary SMOOTH MUSCLE.
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.
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.
Procedures, such as TISSUE CULTURE TECHNIQUES; mathematical models; etc., when used or advocated for use in place of the use of animals in research or diagnostic laboratories.
The protection of animals in laboratories or other specific environments by promoting their health through better nutrition, housing, and care.
The use of animals as investigational subjects.
Alternatives to the use of animals in research, testing, and education. The alternatives may include reduction in the number of animals used, replacement of animals with a non-animal model or with animals of a species lower phylogenetically, or refinement of methods to minimize pain and distress of animals used.
Institutional committees established to protect the welfare of animals used in research and education. The 1971 NIH Guide for the Care and Use of Laboratory Animals introduced the policy that institutions using warm-blooded animals in projects supported by NIH grants either be accredited by a recognized professional laboratory animal accrediting body or establish its own committee to evaluate animal care; the Public Health Service adopted a policy in 1979 requiring such committees; and the 1985 amendments to the Animal Welfare Act mandate review and approval of federally funded research with animals by a formally designated Institutional Animal Care and Use Committee (IACUC).
An array of tests used to determine the toxicity of a substance to living systems. These include tests on clinical drugs, foods, and environmental pollutants.
A plant genus of the family RUBIACEAE. Members produce YOHIMBINE.
The discipline concerned with using the combination of conventional ALLOPATHIC MEDICINE and ALTERNATIVE MEDICINE to address the biological, psychological, social, and spiritual aspects of health and illness.
An approach of practicing medicine with the goal to improve and evaluate patient care. It requires the judicious integration of best research evidence with the patient's values to make decisions about medical care. This method is to help physicians make proper diagnosis, devise best testing plan, choose best treatment and methods of disease prevention, as well as develop guidelines for large groups of patients with the same disease. (from JAMA 296 (9), 2006)
The outer layer of the woody parts of plants.
PLANTS, or their progeny, whose GENOME has been altered by GENETIC ENGINEERING.
Expanded structures, usually green, of vascular plants, characteristically consisting of a bladelike expansion attached to a stem, and functioning as the principal organ of photosynthesis and transpiration. (American Heritage Dictionary, 2d ed)

Canine external carotid vasoconstriction to methysergide, ergotamine and dihydroergotamine: role of 5-HT1B/1D receptors and alpha2-adrenoceptors. (1/222)

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)

G-protein activation by putative antagonists at mutant Thr373Lys alpha2A adrenergic receptors. (2/222)

1. Replacement of a threonine by a lysine at position 373 in the C-terminal portion of the third intracellular loop of the human alpha2A-adrenergic receptor (alpha2A AR) has been reported to generate a constitutively active mutant receptor in analogy with similar mutations in the alpha1B and beta2 AR (Ren et al., 1993). In the present study, the mutant Thr373Lys alpha2A AR receptor was investigated by measuring the formation of inositol phosphates in either the absence or presence of mouse G(alpha)15 protein in Cos-7 cells. 2. Increased affinity, potency and/or efficacy for the agonists [(-)-adrenaline, UK 14304, clonidine, guanabenz and oxymetazoline] was observed, consistent with a precoupled mutant alpha2A AR: G-protein state. The basal inositol phosphates response was similar at the wild-type (wt) and mutant alpha2A AR, but was enhanced at the mutant alpha2A AR upon co-expression with the mouse G(alpha)15 protein. This enhanced response could not be attenuated in the presence of any of the tested alpha2 AR antagonists (10 microM), suggesting that inverse agonist activity did not occur at the mutant alpha2A AR. 3. Ligands that so far have been identified as antagonists at the wt alpha2A AR demonstrated either no intrinsic activity (MK 912, WB 4101, RS 15385, RX 811059 and RX 821002) or positive efficacy [Emax, % vs. 1 microM UK 14304: dexefaroxan (27+/-7), idazoxan (34+/-9), atipamezole (27+/-4), BRL 44408 (59+/-5) and SKF 86466 (54+/-9)] at the mutant alpha2A AR, but only in the presence of the mouse G(alpha)15 protein. The ligand potencies corresponded with their respective pKi values at the mutant alpha2A AR receptor. 4. The partial agonist effect of SKF 86466 was resistant to pertussis toxin treatment (100 ng ml(-1)) and not affected by co-expression of the rat G(alpha)i1 protein. It was virtually absent in the presence of 10 microM RS 15385. SKF 86466 was without intrinsic activity upon co-expression of the mouse G(alpha)q protein. 5. Some putative alpha2 AR antagonists exerted a partial agonist activity that was highly dependent on the presence of specific G-protein alpha-subunits, suggesting that these ligands cause selective G-protein activation at the mutant alpha2A AR.  (+info)

Clonidine evokes vasodepressor responses via alpha2-adrenergic receptors in gigantocellular reticular formation. (3/222)

The gigantocellular depressor area (GiDA) is a functionally defined subdivision of the medullary gigantocellular reticular formation where vasodepressor responses are evoked by glutamate nanoinjections. The GiDA also contains reticulospinal neurons that contain the alpha2A-adrenergic receptor (alpha2A-AR). In the present study, we sought to determine whether nanoinjections of the alpha2-AR agonist clonidine into the GiDA evoke cardiovascular responses and whether these responses can be attributed to the alpha2-AR. We found that nanoinjections of clonidine into the GiDA evoke dose-dependent decreases in arterial pressure and heart rate. These responses were equivalent in magnitude to responses produced by clonidine nanoinjections into the sympathoexcitatory region of the rostral ventrolateral medulla. Furthermore, the vasodepressor and bradycardic responses produced by clonidine injections into the GiDA were blocked in a dose-dependent fashion by the highly selective alpha2-AR antagonist 2-methoxyidazoxan, but not by prazosin, which is an antagonist at both the alpha1-AR and the 2B subtype of the alpha-AR. The antagonism by 2-methoxyidazoxan was site specific because injections of the antagonist into the rostral ventrolateral medulla failed to block the responses evoked by clonidine injections into the GiDA. These findings support the notion that clonidine produces sympathoinhibition through multiple sites within the medullary reticular formation, which is consistent with the wide distribution of the alpha2A-AR in reticulospinal neurons. These data also suggest that clonidine may have multiple mechanisms of action because it evokes a cardiovascular depressive response from regions containing neurons that have been determined to be both sympathoinhibitory and sympathoexcitatory.  (+info)

Effects of GABA on noradrenaline release and vasoconstriction induced by renal nerve stimulation in isolated perfused rat kidney. (4/222)

We examined effects of gamma-aminobutyric acid (GABA) on vasoconstriction and noradrenaline (NA) release induced by electrical renal nerve stimulation (RNS) in the isolated pump-perfused rat kidney. RNS (1 and 2 Hz for 2.5 min each, 0.5-ms duration, supramaximal voltage) increased renal perfusion pressure (PP) and renal NA efflux. GABA (3, 10 and 100 microM) attenuated the RNS-induced increases in PP by 10-40% (P<0.01) and NA efflux by 10-30% (P<0.01). GABA did not affect exogenous NA (40 and 60 nM)-induced increases in PP. The selective GABA(B) agonist baclofen (3, 10 and 100 microM) also attenuated the RNS-induced increases in PP and NA efflux, whereas the RNS-induced responses were relatively resistant to the selective GABA(A) agonist muscimol (3, 10 and 100 microM). The selective GABA(B) antagonist 2-hydroxysaclofen (50 microM), but not the selective GABA(A) antagonist bicuculline (50 microM), abolished the inhibitory effects of GABA (10 microM) on the RNS-induced responses. The selective alpha2-adrenoceptor antagonist rauwolscine (10 nM) enhanced the RNS-induced responses. GABA (3, 10 and 100 microM) potently attenuated the RNS-induced increases in PP by 40-60% (P<0.01) and NA efflux by 20-50% (P<0.01) in the presence of rauwolscine. Prazosin (10 and 30 nM) suppressed the RNS-induced increases in PP by about 70-80%. Neither rauwolscine (10 nM) nor GABA (10 microM) suppressed the residual prazosin-resistant PP response. These results suggest that GABA suppresses sympathetic neurotransmitter release via presynaptic GABA(B) receptors, and thereby attenuates adrenergically induced vasoconstriction in the rat kidney.  (+info)

Blocking effects of phentolamine on L-type calcium current and ATP-sensitive potassium current in guinea pig ventricular myocytes. (5/222)

AIM: To study the effect of phentolamine on L-type calcium currents (ICa) and ATP-sensitive K+ currents (IK,ATP) in ventricular myocytes. METHODS: ICa and IK,ATP were observed using patch clamp techniques in whole-cell recording configuration. RESULTS: Phentolamine reduced ICa of ventricular myocytes in concentration-dependent and voltage-independent manners. Phentolamine 5, 25, and 100 mumol.L-1 decreased ICa from 370 +/- 99 nA to 310 +/- 95 nA (17% block, n = 6, P < 0.01), from 230 +/- 98 nA to 180 +/- 73 nA (23% block, n = 5, P < 0.05), and from 293 +/- 66 nA to 206 +/- 44 nA (30% block, n = 5, P < 0.01), respectively, without affecting the current-voltage relationship. Prazosin 100 mumol.L-1 and yohimbine 100 mumol.L-1, which were specific blockers of alpha 1 and alpha 2 adrenoceptors respectively, did not show the inhibitory effect on ICa. Phentolamine 100 mumol.L-1 also inhibited the IK,ATP induced by 2, 4-dinitrophenol (DNP) at 0 mV from 3.2 +/- 0.6 nA to 0.8 +/- 0.5 nA (75% block, n = 4, P < 0.01). CONCLUSION: Phentolamine directly inhibits ICa and IK,ATP in guinea pig ventricular myocytes.  (+info)

Differential cotransmission in sympathetic nerves: role of frequency of stimulation and prejunctional autoreceptors. (6/222)

Recent reports have suggested that sympathetic nerves may store separately and release independently the cotransmitters ATP and norepinephrine (NE). It is conceivable therefore that the quantity of each neurotransmitter that is released from the nerves is not fixed but rather may vary, possibly with the frequency of stimulation. To test this hypothesis we studied the concomitant release at various frequencies and cooperative postjunctional actions of ATP and NE during the first 10 s of electrical field stimulation of the guinea pig vas deferens. We found that at lower frequencies (8 Hz), prejunctional inhibition of the release of NE, which occurs via alpha2-adrenoceptors, modulates the ultimate composition of the cocktail of cotransmitters by limiting the amount of NE that is coreleased with ATP. As the frequency of stimulation increases (above 8 Hz), the autoinhibition of the release of NE is overridden and the amount of NE relative to ATP increases. The smooth muscle of the guinea pig vas deferens reacts to changes in composition of the sympathetic neurochemical messages by increasing the amplitude of its contractions due to the enhancement by NE of the contractile responses triggered by ATP. This evidence suggests that the prejunctional alpha2-adrenoceptor may function as a sensor that "reads" the frequency of action potentials produced during a burst of neuronal activity and converts that information into discrete neurochemical messages with varying proportions of cotransmitters. The mechanism for decoding the informational content of these messages is based on the cooperative postjunctional interactions of the participating cotransmitters.  (+info)

Electrochemical and electrophysiological characterization of neurotransmitter release from sympathetic nerves supplying rat mesenteric arteries. (7/222)

1. Characteristic features of noradrenaline (NA) and adenosine 5'-triphosphate (ATP) release from postganglionic sympathetic nerves in rat small mesenteric arteries in vitro have been investigated on an impulse-by-impulse basis. NA release was measured using continuous amperometry and ATP release was monitored by intracellular recording of excitatory junction potentials ( 2. Electrical stimuli evoked transient increases in oxidation current. During trains of ten stimuli at 0.5 - 4 Hz there was a depression in the amplitude of oxidation currents evoked following the first stimulus in the train. 3. The neuronal NA uptake inhibitor, desmethylimipramine (1 microM), increased the amplitude of the summed oxidation current evoked by ten stimuli at 1 Hz and slowed the decay of oxidation currents evoked by trains of ten stimuli at 1 and 10 Hz. 4. The alpha2-adrenoceptor antagonist, idazoxan (1 microM), increased the amplitudes of the oxidation currents evoked during trains of ten stimuli at 0.5 - 10 Hz but had no effect on the oxidation currents evoked by the first stimulus in the train. 5. Idazoxan (1 microM) increased the amplitude of all evoked during trains of stimuli at 0.5 and 1 Hz. In addition, the facilitatory effect of idazoxan on was significantly greater than that on oxidation currents. 6. The findings indicate that NA release from sympathetic nerves supplying small mesenteric arteries is regulated by activation of presynaptic alpha2-adrenoceptors and that clearance of released NA in this tissue depends, in part, upon neuronal uptake. The different effects of idazoxan on the oxidation currents and may indicate that the release of NA and ATP is differentially modulated.  (+info)

Enhanced cortical dopamine output and antipsychotic-like effects of raclopride by alpha2 adrenoceptor blockade. (8/222)

Clozapine exerts superior clinical efficacy and markedly enhances cortical dopamine output compared with classical antipsychotic drugs. Here the alpha2 adrenoceptor antagonist idazoxan was administered to rats alone or in combination with the D2/3 dopamine receptor antagonist raclopride. Dopamine efflux in the medial prefrontal cortex and conditioned avoidance responding were analyzed. Idazoxan selectively potentiated the cortical output of dopamine and augmented the suppression of conditioned avoidance responding induced by raclopride. These results challenge basic assumptions underlying the dopamine hypothesis of schizophrenia and provide insight into clozapine's mode of action.  (+info)

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Atipamezole HCl is a selective α2-adrenergic receptor antagonist (Ki values are 1.1, 1.0, 0.89, 1300 and 6500 nM for α2A, α2B, α2C, α1A and α1B receptors respectively). Has been shown to be a brain penetrant.
As described in the accompanying paper, the novel ligand S18327 (1-{2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)piperid-1-yl]ethyl}3-phenyl imidazolin-2-one) displays pronounced antagonist properties at α1-adrenergic receptors (ARs), serotonin [5-hydroxytryptamine (5-HT)2A], and D4 receptors, as well as less potent antagonist actions at α2-AR and D1and D2 receptors. Interestingly, the α2-AR antagonist properties of S18327 underlie a generalized enhancement of cerebral adrenergic transmission and a preferential facilitation of the activity of frontocortical compared with subcortical dopaminergic pathways. On the other hand, the inhibitory influence of S18327 on the activity of serotonergic neurons originating in the dorsal raphe nucleus may be attributed to its antagonist actions at α1-ARs. Notably, S18327 only weakly accelerates striatal turnover of dopamine (DA). In light of these observations, in the present study we examined the activity of S18327 in paradigms predictive of the control of ...
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Stress promotes a shift from goal-directed action-outcome learning toward habitual stimulus-response learning. This shift is mediated by an interaction of noradrenergic activity and glucocorticoid stress hormones. In the present experiment, we examined the neural correlates of the stress (hormone)-induced shift from goal-directed to habit learning in the human brain. Healthy participants were administered hydrocortisone, the α2-adrenoceptor antagonist yohimbine, or both before they were trained in two instrumental actions leading to two distinct food rewards. After training, one of the rewards was devalued by feeding participants to satiety on that food. Finally, participants were presented the two instrumental actions in extinction. We collected functional magnetic resonance images both during instrumental training and during extinction testing. Our behavioral data confirmed that the simultaneous administration of hydrocortisone and yohimbine renders instrumental behavior insensitive to the ...
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Ioannides, C, Okine, L and Parke, DV (1979) Effects of β-adrenoceptor antagonists on the hepatic mixed-function oxygenases in the rat ...
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Yohimbine Hydrochloride Alias: Corynine;Aphrodine CAS No: 65-19-0 Einecs No: 200-600-4 MF: C21H27ClN2O3 MW: 390.91 Purity: 98% Appearance:White crystalline
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Schopnosť vyrábať syntetizovať a vyrábať veľké množstvá Yohimbinu (146-48-5) s kontrolným systémom kvality podľa CGMP výrobných predpisov.
A series of novel Pd(ii) complexes with chelating mono(imidazolin-2-imine) and bis(imidazolin-2-imine) ligands were synthesized. The crystal structures of [Pd(DMEAImiPr)Cl2] and [Pd(DPENImiPr)Cl2] were determined by X-ray diffraction analysis. The reactivity of the six Pd(ii) complexes, namely, [Pd(en)Cl2],
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
Piribedil therapy in Parkinsons disease. Use of the drug in the retard form.: We conducted a 20-week nonblind study to evaluate the efficacy of piribedil in 30
Learn about Yohimbe and Yohimbine HCL Supplements, including potential benefits and side effects. Find out about research and if Yohimbine supplements can help male impotence and help aid weight loss including stubborn fat areas of the body.
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YM 161514 [YM 161511, YM 151], a calcium antagonist and β1-adrenoceptor antagonist, was under investigation with Yamanouchi as a potential treatment for
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Disclosed are nitrosated and nitrosylated α-adrenergic receptor antagonists, compositions of an α-adrenergic receptor antagonist (α-antagonist), which can optionally be substituted with at least one NO or NO 2 moiety, and a compound that donates, transfers or releases nitric oxide as a charged species, i.e., nitrosonium (NO + ) or nitroxyl (NO - ), or as the neutral species, nitric oxide (NO); and uses for each of them in treating human male impotence or erectile dysfunction.
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Four 2-amino-3-methylimidazo[4,5-b][1,x]naphthyridines, x = 5-8 (6-9) have been obtained from aromatic aldehydes (11-14) and 2-amino-1-methyl-2-imidazolin-5-one (15) in one step. The N-1 - and N-3 -methyl isomers of 2-aminoimidazo-[4,5-b]quinoline (5 and 10) were prepared from 2-nitrobenzaldehyde via the isolated E-isomers of imidazolin-5-one (17) and imidazolin-4-one (20).. ...
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Based on the studies we have examined, I recommend working up to 0.2mg/Kg of bodyweight. 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. I would typically start this person at one capsule and work up towards the full dose each consecutive session the person had no undesirable side effects. As I was discussing with Joe Daniels of Swing This Kettlebells, Yohimbine HCls effects work the best in the absence of insulin, and its effects start to diminish the more insulin is present. But this doesnt mean that you cannot eat carbs! Insulin will usually be under control on a lower carb diet, like most trainers will put you on. Obviously, cardio first thing in the morning is a good time (with a scoop of MTS Nutrition Whey in your belly) and even post workout. What you can do is take the Yohimbine HCl DURING your weight training workout 15-20 minutes before you are done. Then, hop ...
Diagnosis Code S65.809 information, including descriptions, synonyms, code edits, diagnostic related groups, ICD-9 conversion and references to the diseases index.
Diagnosis Code S62.90XG information, including descriptions, synonyms, code edits, diagnostic related groups, ICD-9 conversion and references to the diseases index.
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The study document on the Global Yohimbine Market 2020-2027 sheds light on the current trends, methodologies, major technologies and analytical tools
So heres what Im planning on, a topical Yohimburn-type product with a fair amount of caffeine in order to act as a localized diuretic. Since the
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... acts predominantly as a α2-adrenergic receptor antagonist. It has also been shown to function as a 5-HT1A receptor ... Perry BD, U'Prichard DC (December 1981). "[3H]rauwolscine (alpha-yohimbine): a specific antagonist radioligand for brain alpha ... partial agonist and 5-HT2A and 5-HT2B receptor antagonist. Ajmalicine Corynanthine Spegatrine Yohimbine KOHLI JD, DE NN (June ... Wainscott DB, Sasso DA, Kursar JD, Baez M, Lucaites VL, Nelson DL (January 1998). "[3H]Rauwolscine: an antagonist radioligand ...
Perry BD, U'Prichard DC (1981). „[3H]rauwolscine (alpha-yohimbine): a specific antagonist radioligand for brain alpha 2- ... adrenergic receptors". European Journal of Pharmacology. 76 (4): 461-4. PMID 6276200. doi:10.1016/0014-2999(81)90123-0.. ... Rauvolscin deluje predominantno kao antagonist α2-adrenergičnog receptora.[2] On takođe deluje kao parcijalni agonist 5-HT1A ... Wainscott DB, Sasso DA, Kursar JD, Baez M, Lucaites VL, Nelson DL (1998). „[3H]Rauwolscine: an antagonist radioligand for the ...
The alpha1 antagonist prazosin could be effective for PTSD The Alpha-2 adrenergic receptor agonists clonidine and guanfacine ... Jefferson, James W. (1974). "Beta-Adrenergic Receptor Blocking Drugs in Psychiatry". Archives of General Psychiatry. 31 (5): ... Phenibut is a GABAB receptor agonist, as well as an antagonist at α2δ subunit-containing voltage-dependent calcium channels ( ... Beta-receptor blockers such as propranolol and oxprenolol, although not anxiolytics, can be used to combat the somatic symptoms ...
... and dopamine D3 receptors.[31][32] It behaves as an antagonist at α1-adrenergic, α2-adrenergic, 5-HT1B, 5-HT1D, 5-HT2A, 5-HT2B ... February 2000). "Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, ... "Regulation of pre-synaptic alpha adrenergic activity in the corpus cavernosum". Review. International Journal of Impotence ... α1 receptor, 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1F, 5-HT2B, and dopamine D2 receptors, and weak affinity for the 5-HT1E, 5-HT2A, 5-HT ...
... an angiotensin II receptor antagonist Propranolol, a sympatholytic beta blocker Vasopressin receptor antagonists, such as ... Such medications include antipsychotics, antidepressants, anticonvulsants, alpha agonists and anticholinergics. It should also ... and the effects of an adjunctive angiotensin-II receptor blocking drug (irbesartan)". The Australian and New Zealand Journal of ... 66 (2): 283-286. ISSN 1534-7796. PMID 15039516. (subscription required) Lee, H. S.; Kwon, K. Y.; Alphs, L. D.; Meltzer, H. Y. ( ...
... α2-adrenergic antagonist used to reverse the sedative and analgesic effects of alpha-2 adrenergic receptor agonists Albendazole ... dopamine receptor agonist used for the treatment of pituitary pars intermedia dysfunction in horses phenobarbital - anti- ... mu agonist/kappa antagonist, used as a cough suppressant and for a muscle relaxation effect in horses carprofen - COX-2 ... α2-adrenergic agonist, used to temporarily sedate animals yohimbine - used to reverse effects of xylazine, also called an " ...
... an alpha-adrenergic receptor blocker, had a higher incidence of heart failure events, and the doxazosin arm of the study was ... Angiotensin II receptor antagonists work by antagonizing the activation of angiotensin receptors. ... Central alpha agonists lower blood pressure by stimulating alpha-receptors in the brain which open peripheral arteries easing ... On the other hand, β-blockers, diuretics, ACE inhibitors, angiotensin receptor blockers, and aldosterone receptor antagonists ...
Antagonists L-765,314 Risperidone Alpha-1B adrenergic receptor has been shown to interact with AP2M1. A role in regulation of ... The alpha-1B adrenergic receptor (α1B adrenoreceptor), also known as ADRA1B, is an alpha-1 adrenergic receptor, and also ... 1994). "Cloning, expression and characterization of human alpha adrenergic receptors alpha 1a, alpha 1b and alpha 1c". Biochem ... There are 3 alpha-1 adrenergic receptor subtypes: alpha-1A, -1B and -1D, all of which signal through the Gq/11 family of G- ...
... relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists". Journal ... Adrenergic receptor Graham RM, Perez DM, Hwa J, Piascik MT (May 1996). "alpha 1-adrenergic receptor subtypes. Molecular ... The alpha-1 (α1) adrenergic receptor is a G protein-coupled receptor (GPCR) associated with the Gq heterotrimeric G-protein. It ... The α1-adrenergic receptor has several general functions in common with the α2-adrenergic receptor, but also has specific ...
The alpha-2A adrenergic receptor (α2A adrenoceptor), also known as ADRA2A, is an α2 adrenergic receptor, and also denotes the ... the sites for beta-adrenergic receptor kinase-mediated phosphorylation and desensitization of the alpha 2A-adrenergic receptor ... alpha-2A-, receptor". Hein, Lutz; Altman, John D.; Kobilka, Brian K. (1999). "Two functionally distinct α2-adrenergic receptors ... Handy DE, Gavras H (Nov 1992). "Promoter region of the human alpha 2A adrenergic receptor gene". The Journal of Biological ...
Adrenergic receptor Alpha blocker Antagonist Beta blocker List of adrenergic drugs Propanolol Sympathetic nervous system ... An adrenergic antagonist is a drug that inhibits the function of adrenergic receptors. There are five adrenergic receptors, ... Adrenergic competitive antagonists are shorter lasting than the other two types of antagonists. While the antagonists for alpha ... There are few non-cardiovascular uses for adrenergic antagonists. Alpha-adrenergic antagonists are also used for treatment of ...
... also acts as a moderate affinity 5-HT1A receptor antagonist, and low affinity CB1 receptor antagonist). Clonidine (also I1 ... signal through the α2-adrenergic receptor in the central and peripheral nervous systems. The α2A adrenergic receptor is ... where it sits alongside the more plentiful α1-adrenergic receptor. The α2-adrenergic receptor binds both norepinephrine ... presumptively also mediated by α2 adrenergic receptors because it is reversed by yohimbine, an α2 antagonist. α2A selective ...
Cleary L, Murad K, Bexis S, Docherty JR (2005). "The alpha (1D)-adrenoceptor antagonist BMY 7378 is also an alpha (2C)- ... The alpha-1D adrenergic receptor (α1D adrenoreceptor), also known as ADRA1D, is an alpha-1 adrenergic receptor, and also ... This gene encodes alpha-1D-adrenergic receptor. Similar to alpha-1B-adrenergic receptor gene, this gene comprises 2 exons and a ... 1994). "Cloning, expression and characterization of human alpha adrenergic receptors alpha 1a, alpha 1b and alpha 1c". Biochem ...
... ketanserin such as ritanserin are more selective 5-HT2A receptor antagonists with low affinity for alpha-adrenergic receptors. ... Silent antagonistsEdit. *Trazodone is a potent 5-HT2A antagonist, as well as an antagonist on other serotonin receptors. ... but through its high affinity for alpha1 adrenergic receptors. It also has high affinity for H1 histaminergic receptors equal ... G-protein coupled receptor activity. • virus receptor activity. • signal transducer activity. • drug binding. • G-protein alpha ...
Cleary L, Murad K, Bexis S, Docherty JR (2005). "The alpha (1D)-adrenoceptor antagonist BMY 7378 is also an alpha (2C)- ... The alpha-2C adrenergic receptor (α2C adrenoceptor), also known as ADRA2C, is an alpha-2 adrenergic receptor, and also denotes ... "Entrez Gene: ADRA2C adrenergic, alpha-2C-, receptor". "ADRA2C adrenoceptor alpha 2C [Homo sapiens (human)] - Gene - NCBI". www. ... Klein U, Ramirez MT, Kobilka BK, von Zastrow M (1997). "A novel interaction between adrenergic receptors and the alpha-subunit ...
... are a subset of the alpha blocker class of drugs and are antagonists to the α2 adrenergic receptor. They are mainly used in ... Alpha-2 blockers increase noradrenaline release. Yohimbine, historically used as an aphrodisiac, is sometimes used in ... Chopin P, Colpaert FC, Marien M (February 1999). "Effects of alpha-2 adrenoceptor agonists and antagonists on circling behavior ... Lemke, KA (June 2004). "Perioperative use of selective alpha-2 agonists and antagonists in small animals". The Canadian ...
Antibodies against the Alpha 1 adrenergic receptor and muscarinic acetylcholine M4 receptor[4][5][6]. ... Vasopressin receptor antagonist Helps retain water, Increase blood volume Desmopressin (DDAVP) [95] ... Alpha-1 adrenergic receptor agonist Constrict the peripheral blood vessels aiding venous return. Midodrine[17][89][90][91] ... elevated levels of autoantibodies against the adrenergic alpha 1 receptor and against the muscarinic acetylcholine M4 receptor. ...
The adrenergic receptors exert opposite physiologic effects in the vascular smooth muscle under activation: alpha-1 receptors. ... Antagonists of alpha-1 receptors (doxazosin, prazosin) cause vasodilation (a decrease in vascular smooth muscle tone with ... See also receptor antagonist) alpha-2 receptors. Agonists of alpha-2 receptors in the vascular smooth muscle lead to ... Under NE binding alpha-1 receptors cause vasoconstriction ( contraction of the vascular smooth muscle cells decreasing the ...
... alpha 1b- and alpha 1d-adrenergic receptor mRNA in the rat brain and spinal cord". Journal of chemical neuroanatomy. 13 (2): ... melatonin receptor antagonist blocks melatonin-induced antinociception in rats". Neuroscience Letters. 282 (3): 161-4. PMID ... Osim njegove alfa blokatorske aktivnosti, prazosin je antagonist MT3 receptora (koji nije prisutan kod ljudi). On je selektivan ... Day, H. E.; Campeau, S.; Watson Jr, S. J.; Akil, H. (1997). „Distribution of alpha 1a-, ...
Other adrenergic receptors Alpha-1 adrenergic receptor Alpha-2 adrenergic receptor Beta-1 adrenergic receptor Beta-3 adrenergic ... denotes selective antagonist to the receptor. compound-6FA, PAM at intracellular binding site Beta-2 adrenergic receptor has ... "Insulin stimulates sequestration of beta-adrenergic receptors and enhanced association of beta-adrenergic receptors with Grb2 ... "A C-terminal motif found in the beta2-adrenergic receptor, P2Y1 receptor and cystic fibrosis transmembrane conductance ...
... has been shown to interact with Src. Other adrenergic receptors Alpha-1 adrenergic receptor Alpha-2 ... Nisoli E, Tonello C, Landi M, Carruba MO (1996). "Functional studies of the first selective β3-adrenergic receptor antagonist ... The beta-3 adrenergic receptor (β3-adrenoceptor), also known as ADRB3, is a beta-adrenergic receptor, and also denotes the ... adrenergic receptor Beta-1 adrenergic receptor Beta-2 adrenergic receptor Beta Blocker GRCh38: Ensembl release 89: ...
... is a compound which acts as an antagonist at the α1B-adrenergic receptor. It was one of the first selective antagonists ... Morrow AL, Creese I (April 1986). "Characterization of alpha 1-adrenergic receptor subtypes in rat brain: a reevaluation of [3H ... March 2000). "Alpha 1-adrenoreceptor antagonists bearing a quinazoline or a benzodioxane moiety". Pharmaceutica Acta Helvetiae ... developed for this receptor and was invented in 1969, but is still commonly used in research into adrenergic receptors, ...
... including alpha-1 adrenergic receptors, at which it functions as an antagonist, and GABA-A receptors, through positive ... alpha adrenergic and serotonin receptors. The Ki values for l-THP at D1 and D2 dopamine receptors are approximately 124 nM (D1 ... Along with dopamine receptors, l-THP has been reported to interact with a number of other receptor types, ... In the case of 5-HT1A receptors, l-THP binds with a Ki of approximately 340 nM. Animal experiments have shown that the sedative ...
Naltrexone, a mu opioid receptor antagonist, has shown mixed results for cannabis use disorder-both increasing the subjective ... Combination therapy with dronabinol and the alpha 2 adrenergic receptor agonist lofexidine have shown mixed results, with ... The CB-1 receptor antagonist rimonabant has shown efficacy in reducing the effects of cannabis in users, but with a risk for ... 2 (5): 670-675. doi:10.1001/jamaoncol.2016.0155. PMID 26986677.. *^ a b c Budney AJ, Roffman R, Stephens RS, Walker D (December ...
... is a calcium channel blocker and a1-adrenergic receptor antagonist. Boer R, Grassegger A, Schudt C, Glossmann H ( ... May 1989). "(+)-Niguldipine binds with very high affinity to Ca2+ channels and to a subtype of alpha 1-adrenoceptors". European ...
The CB-1 receptor antagonist rimonabant has shown efficacy in reducing the effects of cannabis in users, but with a risk for ... Combination therapy with dronabinol and the alpha 2 adrenergic receptor agonist lofexidine have shown mixed results, with ... Naltrexone, a mu opioid receptor antagonist, has shown mixed results for cannabis use disorder-both increasing the subjective ... Zolpidem, a GABA-A receptor agonist and "Z-hypnotic" medication, has shown some efficacy in treating insomnia due to cannabis ...
BMY-7,378 is a 5-HT1A receptor weak partial agonist/antagonist and α1D-adrenergic receptor antagonist. Goetz AS, King HK, Ward ... "BMY 7378 is a selective antagonist of the D subtype of alpha 1-adrenoceptors". European Journal of Pharmacology. 272 (2-3): R5- ...
... is an α2-adrenergic receptor antagonist and antagonist of the imidazoline receptor. Fluparoxan Idazoxan Chopin P, ... "Effects of alpha-2 adrenoceptor agonists and antagonists on circling behavior in rats with unilateral 6-hydroxydopamine lesions ... 288 (2): 798-804. PMID 9918591. Media related to Efaroxan at Wikimedia Commons v t e. ...
... of the SP preferring receptor, i.e., by drugs known as neurokinin type 1 antagonists (also termed: SP antagonists, or ... Azzolina A, Bongiovanni A, Lampiasi N (Dec 2003). "Substance P induces TNF-alpha and IL-6 production through NF kappa B in ... administered through the non-adrenergic, non-cholinergic nervous system (branch of the vagal system). ... ReceptorEdit. The endogenous receptor for substance P is neurokinin 1 receptor (NK1-receptor, NK1R).[8] It belongs to the ...
... increase beta adrenergic receptors while decreasing alpha adrenergic receptors- which results in increased levels of ... GnRH antagonists (e.g., cetrorelix). *Progestogens (incl., chlormadinone acetate, cyproterone acetate, hydroxyprogesterone ... Receptor/signaling modulators. Androgens and antiandrogens. Estrogen receptor modulators. Progesterone receptor modulators. ... Androgen receptor modulators. Estrogens and antiestrogens. Progestogens and antiprogestogens. List of androgens/anabolic ...
Glutamate receptor antagonist(英語:Excitatory amino acid antagonist) (NMDA(英語:NMDA receptor antagonist)) ... 腎上腺素受體激動藥 (α(英語:Alpha-adrenergic agonist) ... Cannabinoid receptor antagonist(英語:Cannabinoid receptor antagonist). *Endocannabinoid enhancer(英語:Endocannabinoid enhancer) ( ... Endothelin receptor antagonist(英語:Endothelin receptor antagonist). *NK1 receptor antagonist(英語:NK1 receptor
... although there is evidence that it may have some alpha-1 [7] and alpha-2 adrenoceptor antagonist activity.[5] D1 receptor ... Fenoldopam mesylate (Corlopam) is a drug and synthetic benzazepine derivative which acts as a selective D1 receptor partial ... Antagonists. *Typical antipsychotics: Butaclamol. *Chlorpromazine. *Chlorprothixene. *Flupentixol (flupenthixol) (+melitracen) ... Grenader A, Healy DP (July 1991). "Fenoldopam is a partial agonist at dopamine-1 (DA1) receptors in LLC-PK1 cells". J. ...
SoRI-20040; Antagonist-like: SoRI-20041. *Adrenergic release blockers: Bethanidine. *Bretylium. *Guanadrel ... See also: Receptor/signaling modulators • Monoamine reuptake inhibitors • Adrenergics • Dopaminergics • Serotonergics • ... Clortermine (Voranil) was developed by Ciba in the 1960s[1] and is an anorectic drug of the amphetamine class.[2] It is the 2- ... InChI=1S/C10H14ClN/c1-10(2,12)7-8-5-3-4-6-9(8)11/h3-6H,7,12H2,1-2H3 Y ...
NMDA receptor antagonists (e.g., ketamine, dextromethorphan, methadone). *Opioids (e.g., hydrocodone, morphine, oxycodone, ... adrenergic, dopamine D1 and D2, muscarinic, GABA, histaminergic H1, serotonin 5-HT2, and N-methyl-D-aspartate). Inhibitory ... σ receptors, IC50=145μM. Pharmacokinetics[edit]. The pharmacokinetics of lamotrigine follow first-order kinetics, with a half- ... It also blocks L-, N-, and P-type calcium channels and has weak 5-hydroxytryptamine-3 (5-HT3) receptor inhibition. These ...
... captodiamine has been found to act as a 5-HT2C receptor antagonist and σ1 receptor and D3 receptor agonist.[2] It produces ... Alpha-1 blockers (e.g., prazosin). *Alpha-2 agonists (e.g., clonidine, dexmedetomidine, guanfacine) ... See also: Receptor/signaling modulators • Nicotinic acetylcholine receptor modulators • Acetylcholine metabolism/transport ... enhances hypothalamic BDNF expression in vivo by synergistic 5-HT2c receptor antagonism and sigma-1 receptor agonism". J. ...
... dopamine antagonists, antihistamines, cholinergics, anticholinergics, emetics, cannabinoids, and 5-HT (serotonin) antagonists. ... General: β-receptor blockers ("beta blockers"), calcium channel blockers, diuretics, cardiac glycosides, antiarrhythmics, ... Anti-glaucoma: adrenergic agonists, beta-blockers, carbonic anhydrase inhibitors/hyperosmotics, cholinergics, miotics, ... antifungal, alkalinizing agents, quinolones, antibiotics, cholinergics, anticholinergics, antispasmodics, 5-alpha reductase ...
SoRI-20040; Antagonist-like: SoRI-20041. *Adrenergic release blockers: Bethanidine. *Bretylium. *Guanadrel ... See also: Receptor/signaling modulators • Monoamine reuptake inhibitors • Adrenergics • Dopaminergics • Serotonergics • ... N,alpha-Diethylphenylethylamine. *N-Ethylbuphedrone. *N-Ethylhexedrone. *N,N-Dimethylphenethylamine. *Naphthylamphetamine. * ... InChI=1S/C12H17N/c1-2-4-11(5-3-1)10-12-6-8-13-9-7-12/h1-5,12-13H,6-10H2 Y ...
Similarly, ergoline alkaloids have been shown to exhibit both 5-HT agonist and antagonist behaviors for multiple receptors, ... alpha-Ergocryptine. CH(CH3)2. CH2CH(CH3)2. Leucine ... Adrenergic receptor modulators. α1. *Agonists: 6-FNE. * ... a 5-HT2A/2C antagonist.[15] The selectivity and affinity of ergolines for certain 5-HT receptors can be improved by introducing ... The antagonist or agonist behavior of the ergolines are substrate dependent and mixed agonist/antagonist behaviors of ergoline ...
5-Alpha-reductase inhibitor. *Angiotensin II receptor antagonist. *ACE inhibitor. *Alpha-adrenergic agonist ... For receptors, these activities include agonist, antagonist, inverse agonist, or modulator. Enzyme target mechanisms include ...
Meta-[I-131]iodobenzylguanidine is a radio-labeled analog of the adrenergic blocking agent guanethidine.[37] Radioactivity is ... 978-81-89422-33-2. . Retrieved 6 May 2012.. *^ "Investigating leaks in Dams & Reservoirs" (PDF). Retrieved 6 May 2012 ... 2 (4): 453-6. PMID 4290684.. *^ Woenckhaus, U.; Girlich, C. (2005). "Therapie und Prävention der Hyperthyreose" [Therapy and ... J Nucl Med 25:2-6, 1984 *^ Carpi, Angelo; Mechanick, Jeffrey I. (2016). Thyroid Cancer: From Emergent Biotechnologies to ...
Nasal steroids, antihistamines such as diphenhydramine, cromolyn sodium, leukotriene receptor antagonists such as montelukast, ... For nocturnal symptoms, intranasal corticosteroids can be combined with nightly oxymetazoline, an adrenergic alpha-agonist, or ... Other measures that may be used second line include: decongestants, cromolyn, leukotriene receptor antagonists, and ... and leukotriene receptor antagonists such as montelukast.[5] Medications are, however, not sufficient or are associated with ...
NMDA receptor antagonists (e.g., ketamine, dextromethorphan, methadone). *Opioids (e.g., hydrocodone, morphine, oxycodone, ... In addition, the TCAs interact with adrenergic receptors. This interaction seems to be critical for increased availability of ... Alpha-1 blockers (e.g., prazosin). *Alpha-2 agonists (e.g., clonidine, dexmedetomidine, guanfacine) ... Norepinephrine interacts with postsynaptic α and β adrenergic receptor subtypes and presynaptic α2 autoreceptors. The α2 ...
SoRI-20040; Antagonist-like: SoRI-20041. *Adrenergic release blockers: Bethanidine. *Bretylium. *Guanadrel ... See also: Receptor/signaling modulators • Monoamine reuptake inhibitors • Adrenergics • Dopaminergics • Serotonergics • ... 5-DMA is the alpha-methyl homologue of 2C-H and could be called "DOH" under the DO naming scheme. ... History: 2,5-DMA was first synthesized in Tuckahoe, New York by Richard Baltzly and Johannes S. Buck in 1939.[3] ...
Adrenergic stimulants, such as ephedrine, may act by directly binding and activating the receptors that norepinephrine and ... but other drugs such as CB1 receptor antagonists exist in this class too.[25][26] Drugs used to treat sleep disorders such as ... on adrenergic receptors.[83] It is most usually marketed as the hydrochloride or sulfate salt. ... adrenergic receptors), producing sympathomimetic effects. Some drugs, such as MDMA and derivatives may decrease regulatory ...
Hydroxyzine - Antihistamine, 5-HT2A receptor antagonist.. *Propranolol - Sympatholytic, beta blocker.. *Clonidine - ... Prazosin - Sympatholytic, alpha blocker.. Comorbidity[edit]. GAD and depression[edit]. In the National Comorbidity Survey (2005 ... 5-HT1A receptor partial agonists, such as buspirone and tandospirone.. *Serotonin-norepinephrine reuptake inhibitors (SNRIs), ... 19 (2): 107-116.. ,access-date=. requires ,url=. (help). *^ a b Scott, E. L. (2011, September 6). Anxiety Disorders With ...
SoRI-20040; Antagonist-like: SoRI-20041. *Adrenergic release blockers: Bethanidine. *Bretylium. *Guanadrel ... See also: Receptor/signaling modulators • Monoamine reuptake inhibitors • Adrenergics • Dopaminergics • Serotonergics • ... It is structurally similar to MDA, but without the methyl group at the alpha position. ... However, if MDPEA were either used in high enough of doses (e.g., 1-2 grams), or in combination with a monoamine oxidase ...
See also: Receptor/signaling modulators • GABA receptor modulators • GABA metabolism/transport modulators ... Alpha-1 blockers (e.g., prazosin). *Alpha-2 agonists (e.g., clonidine, dexmedetomidine, guanfacine) ... Serotonin antagonists and reuptake inhibitors *Etoperidone. *Nefazodone. *Trazodone. *Tricyclic antidepressants *Amitriptyline ... InChI=1S/C15H28O2/c1-10(2)8-15(16)17-14-9-12(5)6-7-13(14)11(3)4/h10-14H,6-9H2,1-5H3/t12-,13+,14-/m1/s1 ...
α1(英语:Alpha-1 adrenergic receptor) (A, B, D) · α2(英语:Alpha-2 adrenergic receptor) (A, B, C) · β1 · β2 · β3 ... GR113808: a novel, selective antagonist with high affinity at the 5-HT4 receptor. British Journal of Pharmacology. January 1994 ... 腺苷酸(英语:Adenosine receptor) (A1, A2A, A2B, A3) · P2Y(英语:P2Y receptor) (1(英语:P2RY1), 2(英语:P2RY2), 4(英语:P2RY4), 5(英语:LPAR6), 6(英语: ... 乙酰胆碱 (M1, M2, M3, M4, M5) · 多巴胺(英语:Dopamine receptor) (D1, D2, D3, D4, D5) · 组织胺(英语:Histamine receptor) (H1,
However, β2 adrenergic receptor agonists are not recommended to treat ARDS because it may reduce survival rates and precipitate ... Recombinant activated protein C (drotrecogin alpha) was originally introduced for severe sepsis (as identified by a high APACHE ... and H2 antagonist are useful in a person with risk factors of developing upper gastrointestinal bleeding (UGIB) such as on ... the toll-like receptors, the C-type lectin receptors, the NOD-like receptors, and the RIG-I-like receptors. Invariably, the ...
SoRI-20040; Antagonist-like: SoRI-20041. *Adrenergic release blockers: Bethanidine. *Bretylium. *Guanadrel ... See also: Receptor/signaling modulators • Monoamine reuptake inhibitors • Adrenergics • Dopaminergics • Serotonergics • ... Antagonists: AR-A000002. *Beta blockers (e.g., alprenolol, carteolol, isamoltane, oxprenolol, penbutolol, propranolol, ... Antagonists: ABT-354. *Atypical antipsychotics (e.g., aripiprazole, asenapine, clorotepine, clozapine, fluperlapine, ...
It is an alpha-2 adrenergic agonist that causes sedation and does have some analgesic properties. It has minimal effect on ... Midazolam[5] is a benzodiazepine that acts by stimulating inhibitory GABA receptors. Effects are seen within 2-5 minutes, and ... Additionally, some agents have antagonists, reversal agents, that can be used to reverse the effects or reduce the amount of ... Propofol[5] is a non-barbiturate derivative that is thought to act by stimulating inhibitory GABA receptors and blocking ...
Although their primary mechanisms of action are as NMDA receptor antagonists, ketamine and phencyclidine are also SNDRIs and ... at functionally important adrenergic receptor sites in the brain. However, elation may be associated with an excess of such ... Further support for the monoamine hypothesis came from monoamine depletion studies: Alpha-methyl-p-tyrosine (AMPT) is a ... These include receptor desensitization, alterations in intracellular transduction cascades and gene expression, the induction ...
... drugs which are selective receptor antagonists of CysLTR1 but not CysLTR2.[20][21][22][23] Models of allergic reactions in ... is a G protein-coupled receptor that links to and when bound to its CysLT ligands activates the Gq alpha subunit and/or Ga ... leukotriene receptor activity. • cysteinyl leukotriene receptor activity. • galanin receptor activity. Cellular component. • ... G-protein coupled peptide receptor activity. • signal transducer activity. • G-protein coupled receptor activity. • ...
Among other alkaloids is corynanthine, an alpha-1 adrenergic receptor blocker and raubasine. Extracts from the bark of yohimbe ... ISBN 9789290814955 Doxey, JC; Lane AC; Roach AG; Virdee NK (Feb 1984). "Comparison of the alpha-adrenoceptor antagonist ... The leaves grow in groups of three, with short (about 2 cm) stems. The blades are oval-shaped, 11-47 cm long and 5 - 17 cm wide ... pp 516-519 in Timbers Volume 2; Volume 7 of Plant Resources of Tropical Africa. Eds. Lemmens, R.H.M.J., Louppe, D. & Oteng- ...
3H]rauwolscine (alpha-yohimbine): a specific antagonist radioligand for brain alpha 2-adrenergic receptors.. Perry BD, ... These results suggest that [3H]rauwolscine specifically labels both the high and low affinity states of the alpha 2-receptor in ... 3H]Rauwolscine, a specific and potent alpha 2-antagonist radioligand, was used to characterize alpha 2-receptor binding in ... rauwolscine labeled the alpha 2-receptor. Agonists inhibited [3H]rauwolscine binding in a shallow, GTP-sensitive manner. ...
Adrenergic alpha-Antagonists. Adrenergic Antagonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Serotonin 5-HT2 Receptor Antagonists. Serotonin Antagonists. Serotonin Agents. Dopamine D2 Receptor Antagonists. Dopamine ... A Phase 1, Open-Label, 2-Period, Sequential, Drug-Drug Interaction Study To Determine The Effect Of Lithium 600 Mg BID On The ...
Adrenergic alpha-Antagonists. Adrenergic Antagonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Every subject will be invited to 2 separate sessions. At least 24 hours will apart the two sessions. The test in each session ...
Adrenergic alpha-Antagonists. Adrenergic Antagonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Serotonin 5-HT2 Receptor Antagonists. Serotonin Antagonists. Serotonin Agents. Dopamine D2 Receptor Antagonists. Dopamine ... 2018 Feb;26(2):150-159. doi: 10.1016/j.jagp.2017.08.013. Epub 2017 Oct 10. ...
Histamine H1 Antagonists. Histamine Antagonists. Histamine Agents. Anti-Anxiety Agents. Tranquilizing Agents. Adrenergic alpha- ... Change in Interaction of the serotonin receptor (5-HTR) type-2C Cys23Ser single nucleotide polymorphism (SNP) and a 5-HT2AR ... Change in Interaction of the 5-HT2CR Cys23Ser SNP and a 5-HT2AR antagonist on the functional circuitry underlying cue ... HT2AR antagonist [ Time Frame: Baseline to 1 week ]. Change in fMRI activation with other 5-HT2CR SNPs during Attentional bias ...
Platelet alpha 2-adrenergic receptor density is increased in hypercholesterolemia and directly correlates with plasma total and ... Conclusion: Platelet alpha 2-adrenergic receptor density is increased in hypercholesterolemia and directly correlates with ... Platelet alpha 2-adrenergic receptors in hypercholesterolemia: relationship between binding studies and epinephrine-induced ... A statistically significantly higher alpha 2-adrenergic receptor density was observed in a subgroup of 13 patients with ...
Intracerebroventricular injection of the adrenergic alpha-2-receptor agonist, clonidine, stimulated food intake. ... The present study was designed to investigate the role of brain adrenergic alpha-2-receptors on feeding regulation of layer- ... 0/Adrenergic alpha-Agonists; 0/Adrenergic alpha-Antagonists; 0/Neuropeptide Y; 0/Neurotransmitter Agents; 0/Receptors, ... Adrenergic alpha-Agonists / pharmacology. Adrenergic alpha-Antagonists / pharmacology. Animals. Chickens / physiology*. ...
To test the effects in humans, we assessed autonomic vasomotor tone and baroreflex regulation in 9 normal young adults on 2 ... We observed earlier that central alpha-2 adrenoceptor stimulation in mice greatly augments parasympathetic tone. ... 0/Adrenergic alpha-Agonists; 0/Adrenergic beta-Antagonists; 0/Antihypertensive Agents; 0/Cardiotonic Agents; 0/Receptors, ... Adrenergic alpha-Agonists / pharmacology*. Adrenergic beta-Antagonists / pharmacology. Adult. Antihypertensive Agents / ...
Receptor, Serotonin, 5-HT2A / metabolism* * Receptors, Adrenergic, alpha-2 / metabolism * Receptors, Histamine H3 / metabolism ... receptor antagonists while a selective 5-HT(2B) receptor agonist and a selective 5-HT(2C) receptor agonist were without effect ... receptors because stress had no significant impact on other serotonin receptors, as well as histamine H(3) receptor and alpha(2 ... receptor signaling primarily resulted from receptor downregulation. The stress-induced effect appeared to be specific to 5-HT( ...
0 (Biogenic Monoamines); 0 (RNA, Messenger); 0 (Receptor, Serotonin, 5-HT1B); 0 (Receptors, Adrenergic, alpha-2); 0 (Receptors ... an effect that was not affected by the Mas receptor antagonist A779 (10 nmol/min; >0.05). In the absence of hyperinsulinemia, ... Serotonin 5-HT1 Receptor Antagonists); 0 (Tryptamines); 333DO1RDJY (Serotonin); 422ZU9N5TV (tryptamine); EC (Aromatic- ... Receptor activation in the absence of monoamines results from the production of trace amines (such as tryptamine) by pericytes ...
NMDA receptor antagonists: The NMDA receptor antagonists are available on prescription. Although there is not a legal ... The alpha2-adrenergic receptor agonists: the alpha2-adrenergic receptor agonists are available on prescription. Although there ... Alpha 2-Adrenergic Receptor Agonists. The alpha2-adrenergic receptor agonists have been used extensively in animals to ... NMDA Receptor Antagonists. N-methyl-D-aspartate (NMDA) receptors are important for the transmission of some aspects of pain in ...
... chronic effects of phenylethanolamine N-methyltransferase inhibitors and alpha adrenergic receptor antagonists on brain ... Changes in brain alpha-adrenergic receptors after alpha-methyldopa administration to spontaneously hypertensive rats. ... Modulation of rat brain alpha- and beta-adrenergic receptor populations by lesion of the dorsal noradrenergic bundle. ... Strain differences in rat brain epinephrine synthesis: regulation of alpha-adrenergic receptor number by epinephrine. ...
... an opioid receptor agonist/norepinephrine reuptake inhibitor tapentadol (Ortho-McNeil); a dopamine receptor agonist sodium ... a sodium channel antagonist mexiletine (Boehringer Ingelheim); three glutamate / NMDA antagonists ketamine intranasal (Javelin ... an alpha-2 adrenergic receptor antagonist/norepinehrine reuptake inhibitor reboxetine (Pfizer); ... Eighteen drugs are in Phase III development in the US including two GABA receptor agonists pregabalin (Pfizer) and gabapentin ...
... direct measurements indicate that plasma membrane polypeptide hormone receptors are mobile within the plane of the lipid ... Agonist and antagonist binding to alpha 2-adrenergic receptors in purified mem branes from human platelets. Implications of ... Role of fry subunits of G proteins in targeting the (3-adrenergic receptor kinase to membrane-bound receptors. Science 1992; ... multiple sites of regulation by 3-adrenergic receptor and Mg- studied in reconstituted receptor-G, vesicles. J Biol Chem 1986 ...
Rauwolscine acts predominantly as a α2-adrenergic receptor antagonist. It has also been shown to function as a 5-HT1A receptor ... Perry BD, UPrichard DC (December 1981). "[3H]rauwolscine (alpha-yohimbine): a specific antagonist radioligand for brain alpha ... partial agonist and 5-HT2A and 5-HT2B receptor antagonist. Ajmalicine Corynanthine Spegatrine Yohimbine KOHLI JD, DE NN (June ... Wainscott DB, Sasso DA, Kursar JD, Baez M, Lucaites VL, Nelson DL (January 1998). "[3H]Rauwolscine: an antagonist radioligand ...
... relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists". Journal ... Adrenergic receptor Graham RM, Perez DM, Hwa J, Piascik MT (May 1996). "alpha 1-adrenergic receptor subtypes. Molecular ... The alpha-1 (α1) adrenergic receptor is a G protein-coupled receptor (GPCR) associated with the Gq heterotrimeric G-protein. It ... The α1-adrenergic receptor has several general functions in common with the α2-adrenergic receptor, but also has specific ...
Note to Physician: This product contains an alpha2-adrenergic antagonist.. Precautions. 1. Handling: REVERTIDINE can produce an ... Sedation relapse is more likely to occur in dogs that receive an alpha2-agonist by the IV route, compared to dogs that are ... This is the opposite of the response to alpha2-agonist treatment, and is probably due to atipamezole-induced peripheral ... Atipamezole is a potent alpha2-antagonist which selectively and competitively inhibits alpha2-adrenergic receptors. The result ...
The authors note the limited utility of NMDA receptor antagonists and alpha-2 adrenergic agonists. ... and introduces the concept of COX-2 inhibitors for acute pain management. ...
Cleary L, Murad K, Bexis S, Docherty JR (2005). "The alpha (1D)-adrenoceptor antagonist BMY 7378 is also an alpha (2C)- ... The alpha-1D adrenergic receptor (α1D adrenoreceptor), also known as ADRA1D, is an alpha-1 adrenergic receptor, and also ... This gene encodes alpha-1D-adrenergic receptor. Similar to alpha-1B-adrenergic receptor gene, this gene comprises 2 exons and a ... 1994). "Cloning, expression and characterization of human alpha adrenergic receptors alpha 1a, alpha 1b and alpha 1c". Biochem ...
Assessment of alpha 2 adrenergic autoreceptor function in humans: effects of oral yohimbine. Life Sci 1982;30(23):2033-2041. ... It is significantly more active at presynaptic adrenoceptors than postsynaptic receptors. This action blocks the decrease in ... and peripherally to increase the release of norepinephrine from adrenergic nerve terminals. This increases the plasma ... Alpha 2-antagonist compounds and lipid mobilization: evidence for a lipid mobilizing effect of oral yohimbine in healthy male ...
YOH is suggested to enhance emotional memory by elevating norepinephrine, whereas the β-adrenergic receptor antagonist ... Because alpha-2 adrenoceptors are distributed throughout the brain, the estimation of the BPND is complicated by the absence of ... an α2-adrenergic receptor antagonist, which increases physiological arousal via noradrenaline release) on performance on ... We compared two antagonists with differential selectivity for α1- vs. α2-receptors, yohimbine (YOH, 1:40 selectivity) and ...
Prostaglandin synthesis elicited by adrenergic stimuli in rabbit aorta is mediated via alpha-1 and alpha-2 adrenergic receptors ... Adaptation of brain 5HT2 receptors after mianserin treatment: receptor sensitivity, not receptor binding, more accurately ... RG 12915: a potent 5-hydroxytryptamine-3 antagonist that is an orally effective inhibitor of cytotoxic drug-induced emesis in ... Endothelin receptor-coupling mechanisms in vascular smooth muscle: a role for protein kinase C. N R Danthuluri and T A Brock ...
Alpha1, alpha2 adrenergic, and histaminergic receptors are also antagonized with high affinity. Risperidone has low to moderate ... 9-hydroxyrisperidone is the predominant circulating form and is approximately equal to risperidone in receptor binding activity ... Bipolar mania (monotherapy or as an adjunct to lithium or divalproex): Oral: Initial: 2 to 3 mg once daily; if needed, adjust ... Bipolar I maintenance (monotherapy or as an adjunct to lithium or divalproex): IM: 25 mg every 2 weeks; if unresponsive, some ...
Perry BD, UPrichard DC (1981). „[3H]rauwolscine (alpha-yohimbine): a specific antagonist radioligand for brain alpha 2- ... adrenergic receptors". European Journal of Pharmacology. 76 (4): 461-4. PMID 6276200. doi:10.1016/0014-2999(81)90123-0.. ... Rauvolscin deluje predominantno kao antagonist α2-adrenergičnog receptora.[2] On takođe deluje kao parcijalni agonist 5-HT1A ... Wainscott DB, Sasso DA, Kursar JD, Baez M, Lucaites VL, Nelson DL (1998). „[3H]Rauwolscine: an antagonist radioligand for the ...
... alpha.-adrenergic receptor antagonists, compositions comprising .alpha.-adrenergic receptor antagonists that are optionally ... substituted with at least one NO or NO.sub.2 moiety and compounds that donate, transfer or release nitric oxide or elevate ... A kit comprising an imidazoline .alpha.-adrenergic receptor antagonist, wherein the imidazoline .alpha.-adrenergic receptor ... alpha.-adrenergic receptor antagonists can be avoided by the use of such .alpha.-adrenergic receptorantagonists when nitrosated ...
Norepinephrine Antagonist Serotonin Antagonist Blocks Pre-synaptic Alpha 2 Adrenergic Receptors .. To depression (APA Studies) ... Stage 2 - Behavioral Therapy in order to learn or relearn how to handle emotions. Conclusion: It is necessary to have a close ... Stage 2: Therapy . This is nothing more nor less than relearning (a reeducation) healthy and natural behaviors. The patient ... Stage 2: The relearning of walk, then bicycle. - If we satisfy with stage 1. Then the medical profession will have restored the ...
Antagonist. General Function. Protein heterodimerization activity. Specific Function. This alpha-adrenergic receptor mediates ... G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive ... G-protein coupled amine receptor activity. Specific Function. Dopamine receptor whose activity is mediated by G proteins which ... and acts peripherally to block alpha-receptors. One other possible mechanism is the effect of ergoloid mesylates on neuronal ...
The 5HT1 receptor-selective antagonist methiothepin, but not ketanserin (5HT2-selective) or ICS-205,930 (5HT3-selective), ... The nonselective alpha-adrenergic agonist oxymetazoline inhibits parathyroid hormone (PTH)-stimulated cAMP production in intact ... Desensitization of alpha 2-receptor-mediated inhibition of cAMP production by epinephrine did not alter the response to either ... a receptor in OK cells that is negatively coupled to adenylate cyclase but distinct from the alpha 2-adrenergic receptor. Prior ...
Regulation of autonomic receptors in rat submandibular gland. D B Bylund, J R Martinez and D L Pierce ... Alpha1-adrenergic stimulation of phosphatidylinositol-phosphatidic acid turnover in rat parotid cells. T Uchida, H Ito, B J ... Characterization with agonist and antagonist radioligands and relationship to adenylate cyclase. D J Kahn, J C Mitrius and D C ... Apparent "down-regulation" of human platelet alpha 2-adrenergic receptors is due to retained agonist. J S Karliner, H J ...
ALPHA-T2 is a clean jitter free blend of three POWERFUL and pure ingredients that are combined at perfect doses. Whether you ... Now, when these receptors are blocked a pathway known as the beta-adrenergic pathway is what is actually causing the increase ... 3H]rauwolscine (alpha-yohimbine): a specific antagonist radioligand for brain alpha 2-adrenergic receptors. Eur J Pharmacol. ... , Forum , Supplement Forum , Supplement Companies , PES , Alpha-T2 has been UPGRADED! ...
  • Left ventricular hypertrophy (LVH) is associated with decreased responsiveness of renal α1-adrenoreceptors subtypes to adrenergic agonists. (
  • The responsiveness of renal α1A, α1B and α1D-adrenoceptors in the low dose and high dose phases of 5-MeU, CEC and BMY7378 to adrenergic agonists was increased along with cGMP in the kidney of LVH-NO group. (
  • These findings suggest that exogenous NO precursor up-regulated the renal eNOS/NO/cGMP pathway in LVH rats and resulted in augmented α1A, α1B and α1D adrenoreceptors responsiveness to the adrenergic agonists. (
  • The authors note the limited utility of NMDA receptor antagonists and alpha-2 adrenergic agonists. (
  • Other effects on smooth muscle are contraction in: Ureter Uterus (when pregnant): this is minor compared to the relaxing effects of the β2 receptor, agonists of which - notably albuterol/salbutamol - were formerly[citation needed] used to inhibit premature labor. (
  • Methyl-synephrine and higenamine are beta-3 adrenergic receptor agonists with little to no activity on beta-1 and beta-2 which deal with the heart and lungs respectively. (
  • In our study we have determined that UK-14304 (UK) and norepinephrine (NE), both alpha 2-adrenergic agonists, can augment LPS-stimulated TNF from elicited macrophages (MO). (
  • These investigations support the role of alpha 2 adrenergic agonists as immunostaining compounds that may regulate cytokine production during an inflammatory response. (
  • Such medications include acetylcholinesterase inhibitors, the antipsychotic quetiapine, and adrenergic receptor agonists such as clozapine and yohimbine [51, 161, 162]. (
  • Exogenous GnRH agonists, true to their name, cause signal transduction upon their binding to their receptors and thereby create pronounced release of gonadotrophins from the pituitary gland. (
  • Agonists induce the formation of a guanine nucleotide-sensitive high-affinity state of alpha 2 but not alpha 1 receptors. (
  • α-2-ADRENOCEPTORS are known to mediate analgesia, and α-2-adrenoceptor agonists (such as clonidine) have proven effective in the treatment of pain, such as intractable cancer pain, 1,2 postsurgical pain, 3,4 and sympathetically maintained pain. (
  • 5 However, the systemic use of α-2 agonists for long-term analgesia has been limited by a narrow therapeutic window due to the potential for sedation and cardiovascular depression. (
  • Clonidine and other α-2 agonists used clinically (tizanidine, brimonidine and dexmedetomidine) activate to varying degrees three structurally distinct subtypes of the α-2 receptor: α-2A, α-2B, and α-2C. (
  • however, the α-2A subtype has also been associated with dose-dependent sedation and decreased blood pressure, thus narrowing the therapeutic window of α-2 agonists when used clinically for analgesic activity. (
  • Further research to define the role of various alpha receptor subtypes is needed to identify strategies for separating the analgesic and sedative effects of α-2 agonists. (
  • The α-2A receptor was necessary for the analgesic activity of brimonidine, clonidine, and tizanidine, but a surprising difference identified in the activity of the α-2 agonists in α-2C knockout mice led to investigation of the roles of α-1 and α-2 receptor activation in pain modulation. (
  • INTRATHECAL administration of cholinergic receptor agonists or cholinesterase inhibitors have an antinociceptive effect in a dose-dependent manner, which is mediated by spinal muscarinic receptors in animals, and this analgesic effect has been confirmed in human studies. (
  • Thus, [small alpha, Greek] 2-adrenergic receptor agonists, N-methyl D-aspartate receptor antagonists, [small gamma, Greek]-aminobutyric acid receptor agonists, and adenosine receptor agonists have been shown to have an antiallodynic effect at the spinal cord level. (
  • RESULTS: Stimulation-evoked (but not spontaneous) 3H-norepinephrine release was inhibited by alpha 2-adrenergic, muscarinic, dopaminergic, neuropeptide Y, and prostaglandin agonists and was enhanced by angiotensin II. (
  • Naloxone is a potent antagonist at the mu opioid receptors and produces opioid withdrawal signs and symptoms in individuals physically dependent on full opioid agonists when administered parenterally. (
  • Reverses opioid effects by inhibiting opioid agonists at receptor sites. (
  • Highly concentrated alpha-2 agonists such as medetomidine commonly used in veterinary anesthesia, can potentially cause signific-ant harm or death if accidentally exposed to a human. (
  • The results show that when compared to animals, humans require approximately 10 times less alpha-2 agonists for deep sedation, but 10 times more atipamezole for adequate reversal. (
  • 3H]rauwolscine (alpha-yohimbine): a specific antagonist radioligand for brain alpha 2-adrenergic receptors. (
  • This effect was blocked by co-injection of the alpha-2-receptor antagonist, yohimbine, demonstrating that the alpha-2-receptor is related to stimulation of feeding in layer-type chicks. (
  • Yohimbine acts as an alpha-2 adrenoceptor antagonist. (
  • Yohimbine also inhibits monoamine oxidase, blocks calcium channels, and blocks peripheral serotonin receptors. (
  • Yohimbine acts centrally to increase sympathetic outflow, and peripherally to increase the release of norepinephrine from adrenergic nerve terminals. (
  • In a study of type 1 and type 2 diabetic rats, pretreatment with yohimbine potentiated glucose-induced insulin release in non-diabetic control rats, and an improvement of oral glucose tolerance in type 2 diabetic rats, but not in type 1 diabetic rats. (
  • Yohimbine may act via blockade of postsynaptic alpha-2 adrenoceptors to produce insulinotropic and hypoglycemic effects. (
  • 25 Since alpha-adrenoceptors are located in widespread locations throughout the central and peripheral nervous system, yohimbine has a variety of autonomic and psychic effects (increased noradrenaline release). (
  • We aimed to investigate the relationship of alpha2-receptor dysregulation with learning processes in MDD by conducting a differential fear conditioning paradigm after double-blind administration of the alpha2-receptor antagonist yohimbine versus placebo. (
  • The alpha-2 adrenergic receptor antagonist, yohimbine , can facilitate fear extinction in animals and humans. (
  • Alpha-T2 contains pure Rauwolscine HCl, also known as alpha-yohimbine. (
  • It's the messing with alpha-1 that is cause of criticism/scrutiny on yohimbe/yohimbine. (
  • Yohimbine is an alpha-2 adrenergic antagonist , and has been used in a variety of research projects. (
  • The concentration-effect curve for UK and NE was shifted to the right by the alpha 2-antagonist yohimbine (10(-6) M), with new EC50 of 49.7 +/- 12.2 (p less than 0.001) nM and 10.3 +/- 22 nM. (
  • The presence of a MO alpha-adrenergic receptor was established by demonstrating binding of the alpha 2-adrenergic antagonist 3H-yohimbine to membranes prepared from MO. (
  • 25) reported that the antinociception induced by tricyclic antidepressants was inhibited by reserpine (a drug that decreases the noradrenaline release from adrenergic nerve endings) and yohimbine , an [alpha]-2 adrenergic receptor antagonist), in their study in rats using abdominal contraction and hot-plate tests. (
  • 2 mL (50 mg/mL) naltrexone HCl and 3 ml (5 mg/mL) yohimbine HCl as an antagonist. (
  • Groups of anesthetized mice were pretreated with saline, the alpha(2)-agonist clonidine (1 mg/kg), and the alpha(2)-antagonists RX821002 (1 mg/kg) and yohimbine (1 mg/kg). (
  • Some natural alkaloids from medicinal plants, such as yohimbine and its derivatives, have been reported with adrenoceptor (AR) α 2 subtypes inhibiting activity. (
  • After that, docking and molecular dynamics methods were used to investigate the binding modes of yohimbine and its 2 derivatives in the active pocket of adrenoceptor α 2 subtype A, B, and C. The key interactions between the 3 ligands and the 3 receptors were mapped. (
  • Medically, yohimbine is a pre-synaptic alpha-2-adrenergic blocking agent, also referred to as an alpha 2-adrenergic antagonist. (
  • Yohimbine is known as an alpha-2 antagonist, which means it blocks the alpha-2 receptors. (
  • Unlike many other supplements, yohimbine has been tested in humans, and shown to have a reproducible and significant effect on the reduction of body fat (2,3,4). (
  • [1] Yohimbine is a powerful stimulant and alpha-2 adrenergic receptor antagonist. (
  • Yohimbine is a potent alpha-2 adrenergic antagonist. (
  • In other words, yohimbine decreases fat mass specifically in those stubborn areas that are dense with A2 receptors. (
  • Basically, yohimbine works by preventing the alpha-2 adrenoreceptors from inhibiting or blunting lipolysis while inducing the release of norepinephrine and therefore, lipolysis. (
  • Yohimbine and atropine alone enhanced 3H-norepinephrine output, suggesting that prejunctional alpha 2-adrenergic and muscarinic receptors undergo tonic activation by endogenously released neurotransmitters. (
  • Folklore says that inhibition of a2 adrenergic receptors with Yohimbine treats what? (
  • To avoid confusion, naming was continued with the letter D. Catecholamines like norepinephrine (noradrenaline) and epinephrine (adrenaline) signal through the α1-adrenergic receptor in the central and peripheral nervous systems. (
  • The neurotransmitter norepinephrine has higher affinity for the α1 receptor than does the hormone epinephrine/adrenaline. (
  • In particular, norepinephrine decreases glutamatergic excitatory postsynaptic potentials by the activation of α1-adrenergic receptors. (
  • Norepinephrine also stimulates serotonin release by binding α1-adrenergic receptors located on serotonergic neurons in the raphe. (
  • The beta-mediated regulation of alpha 2-receptor sensitivity at brain norepinephrine synapses may be a mechanism for the homeostatic control of central noradrenergic activity. (
  • Adrenoceptor (AR) is a signal receptor of epinephrine and norepinephrine and is mainly distributed in myocardial, vascular, and nervous system. (
  • 3. _____ Drugs that block the action of norepinephrine and epinephrine on alpha receptors (alpha adrenergic antagonists or alpha-blockers) dilate most blood vessels. (
  • Agonist-induced effects on 3H-norepinephrine overflow were blocked by selective antagonists, where available. (
  • CONCLUSIONS: Human ocular sympathetic nerves express inhibitory alpha 2-adrenergic, muscarinic, dopaminergic, prostaglandin, and neuropeptide Y receptors and facilitatory angiotensin II receptors that control the impulse-evoked release of 3H-norepinephrine. (
  • studied the effect of intravenous AT in healthy, unanesthetized male volunteers at doses of 10, 30 and 100 mg. 11 The authors found that subjects receiving a 100 mg AT intravenous (IV) infusion over 20 minutes had increased plasma norepinephrine (NE) concentrations by 484 +/- 269 %, and elevated systolic and diastolic blood pressure (mean increases 17 +/- 7 and 14 +/- 2 mm Hg, respectively). (
  • This study investigated the impact of nitric oxide (NO) and its potential interaction with the responsiveness of renal α1-adrenoreceptors subtypes to adrenergic stimulation in rats with left ventricular hypertrophy (LVH). (
  • α1-adrenergic receptor subtypes increase inhibition in the olfactory system, suggesting a synaptic mechanism for noradrenergic modulation of olfactory driven behaviors. (
  • There are 3 alpha-1 adrenergic receptor subtypes: alpha-1A, -1B and -1D, all of which signal through the Gq/11 family of G-proteins and different subtypes show different patterns of activation. (
  • Validation and statistical analysis of a computer modeling method for quantitative analysis of radioligand binding data for mixtures of pharmacological receptor subtypes. (
  • It has actions at several 5-HT (serotonin) receptor subtypes. (
  • They are classified into subtypes α 1, α 2 and β according to the pharmacological functions and sequences. (
  • α 1 receptors have subtype A, B, and D. α 2 receptors have subtypes A, B, and C. β receptors have β 1, β 2, β 3 [ 1 , 2 ]. (
  • Both the agonist and the antagonist on different AR subtypes can be leading compounds with pharmacological effects, particularly the significant cardiovascular effect. (
  • The most remarkable activity is selective inhibition on ARs, high affinity for the AR α 2 subtypes, and moderate affinity for the α 1 subtypes. (
  • Adrenergic alpha2 receptors are divided into three subtypes in humans: alpha2A, alpha2B and alpha2C. (
  • The chapter on other drugs used in acute pain highlights the utility of non-opioid adjuncts, emphasizes a practical approach, and introduces the concept of COX-2 inhibitors for acute pain management. (
  • These results can guide the design of new selective AR α 2 inhibitors. (
  • Among the most important and most widely used drugs are thiazide diuretics , calcium channel blockers , ACE inhibitors , angiotensin II receptor antagonists (ARBs), and beta blockers . (
  • In the United States, the JNC8 (Eighth Joint National Committee on the Prevention, Detection, Evaluation, and Treatment of High Blood Pressure) recommends thiazide-type diuretics to be one of the first-line drug treatments for hypertension, either as monotherapy or in combination with calcium channel blockers , ACE inhibitors , or angiotensin II receptor antagonists . (
  • recommends calcium channel blockers to be a first-line treatment either as monotherapy or in combination with thiazide -type diuretics, ACE inhibitors , or angiotensin II receptor antagonists for all patients regardless of age or race. (
  • However, ACE inhibitors (and angiotensin II receptor antagonists ) should not be a first-line treatment for black hypertensives without chronic kidney disease . (
  • Two classes of drugs are used, 5-alpha reductase inhibitors and alpha adrenergic antagonists. (
  • Downregulation of post-synaptic 5-HT 2A receptor is an adaptive process provoked by chronic administration of selective serotonin reuptake inhibitors (SSRIs) and classical antipsychotics. (
  • Moving on to the next class of Anti-Depressant drugs are the 5-HT antagonist/reuptake inhibitors (SARIs). (
  • Given this public health challenge, and that the current approved therapy for AD is limited to symptomatic treatment (i.e., cholinesterase inhibitors and NMDA receptor antagonists), exploration of new molecular pathways as novel therapeutic targets remains an attractive option for disease modifying drug development. (
  • Therefore, the current study was designed (1) to characterize the effects of spinal cholinesterase inhibitors on nerve injury-induced tactile allodynia and [2] to define the pharmacologic nature of the cholinergic receptors that mediate the effects of this family of agents. (
  • This study assessed whether platelet hyperreactivity to epinephrine in hypercholesterolemia is associated with higher alpha 2-adrenergic receptor density or affinity for epinephrine. (
  • Platelet alpha 2-adrenergic receptor density is increased in hypercholesterolemia and directly correlates with plasma total and levels of LDL cholesterol, providing at least a partial explanation for the enhanced platelet response to epinephrine that is observed in hypercholesterolemia. (
  • Desensitization of alpha 2-receptor-mediated inhibition of cAMP production by epinephrine did not alter the response to either 5HT or oxymetazoline, indicating that these compounds do not produce their effect by activating alpha 2-adrenergic receptors. (
  • In addition, the lack of any guanylylimidodiphosphate effect on the l-epinephrine competition curve observed in MHS rats suggests the uncoupling of these receptors from the guanosine 5'-triphosphate binding protein. (
  • The binding properties of two alpha-adrenergic radioligands, [3H]epinephrine (an agonist) and [3H]dihydroergocryptine (an antagonist), were compared in two model systems--membranes derived from human platelets and membranes from rat liver. (
  • 3H]Dihydroergocryptine labels all the alpha receptors, whereas [3H]epinephrine at low concentrations labels predominantly the high-affinity form of the alpha 2 receptor in both platelet and liver. (
  • Thus, in liver membranes the endogenous 'physiological' agonist may not label the physiologically relevant alpha 1 receptors in typical radioligand binding assays using low concentrations of [3H]epinephrine. (
  • These results suggest that [3H]rauwolscine specifically labels both the high and low affinity states of the alpha 2-receptor in brain membranes. (
  • 0.03), but no difference was observed in receptor affinity for the ligand. (
  • Affinity of drugs and peptides for U-69,593-sensitive and -insensitive kappa opiate binding sites: the U-69,593-insensitive site appears to be the beta endorphin-specific epsilon receptor. (
  • Alpha 1 , alpha 2 adrenergic, and histaminergic receptors are also antagonized with high affinity. (
  • Risperidone has low to moderate affinity for 5-HT 1C , 5-HT 1D , and 5-HT 1A receptors, weak affinity for D 1 and no affinity for muscarinics or beta 1 and beta 2 receptors. (
  • It has high affinity for D 2 dopaminergic receptors. (
  • To test for alpha(2) adrenergic modulation of dopamine D(2/3) receptor availability in striatum of living mice using the high-affinity ligand [(18)F]fallypride and microPET. (
  • In the cerebral cortex, no between-strain differences in alpha 1-adrenergic and alpha 2-adrenergic receptor density and affinity were observed in prehypertensive and hypertensive periods. (
  • Compared with their age-matched normotensive controls, MHS rats showed 1) a lower affinity for the antagonist (p less than 0.05) in the prehypertensive period, 2) absence of the normal age-related increase in receptor density, and 3) a lower density of [3H]rauwolscine binding sites (p less than 0.001) in the hypertensive period. (
  • [14] In the pre-molecular-cloning era when radioligand binding and displacement was the only major tool, spiperone and LSD were shown to label two different serotonin receptors, and neither of them displaced morphine, leading to naming of the 5-HT 1 , 5-HT 2 and 5-HT 3 receptors, corresponding to high affinity sites from LSD , spiperone and morphine respectively. (
  • Haloperidol also binds to alpha-1 adrenergic receptors, but with lower affinity, and displays minimal binding to muscarinic cholinergic and histaminergic (H 1 ) receptors. (
  • This was achieved by inserting different D-amino acids in the peptide in position 6 to increase receptor affinity and binding ( Figure 1 ). (
  • These are generally unnatural amino acids ( Figure 1 ) to serve various molecular functions such as high-affinity binding to the receptor and the concomitant blockade of receptor signaling [2]. (
  • It has a high affinity for serotoninergic 5-HT 2 and dopaminergic D 2 receptors. (
  • Risperidone binds also to alpha 1 -adrenergic receptors, and, with lower affinity, to H 1 -histaminergic and alpha 2 -adrenergic receptors. (
  • Risperidone has no affinity for cholinergic receptors. (
  • At one time, there was a subtype known as α1C, but it was found to be identical to the previously discovered α1A receptor subtype. (
  • The present studies examined the possibility that an antagonist action at a particular receptor subtype might be responsible for the interaction between PCP and the clozapine-like antipsychotics by testing whether a selective antagonist at alpha -1, alpha -2, M1 or GABA-A receptors would prevent the PCP-induced deficit in PPI in rats. (
  • In this paper, three-dimensional homology models were built for each AR α 2 subtype. (
  • The mammalian 5-HT 2A receptor is a subtype of the 5-HT 2 receptor that belongs to the serotonin receptor family and is a G protein-coupled receptor (GPCR). (
  • This is the main excitatory receptor subtype among the GPCRs for serotonin , although 5-HT 2A may also have an inhibitory effect [6] on certain areas such as the visual cortex and the orbitofrontal cortex. (
  • 5-HT 2A is thought to correspond to what was originally described as D subtype of 5-HT receptors by Gaddum and Picarelli. (
  • Thus, serotonin primarily acts via 5-HT(2A) receptors to facilitate BLA GABAergic inhibition. (
  • This severe impairment of 5-HT(2A) receptor-mediated facilitation of BLA GABAergic inhibition might result in an amygdala circuitry with hyperexcitability, and a lower threshold of activation, and thus be an important mechanism underlying the emergence of stress-associated psychiatric symptoms. (
  • In contrast to α2-adrenergic receptors, α1-adrenergic-receptors in the arterial vasculature of skeletal muscle are more resistant to inhibition, and attenuation of α1-adrenergic-receptor-mediated vasoconstriction only occurs during heavy exercise. (
  • This inhibition, however, is not blocked by alpha 2-adrenergic receptor antagonists. (
  • Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. (
  • 3H]Rauwolscine, a specific and potent alpha 2-antagonist radioligand, was used to characterize alpha 2-receptor binding in bovine cerebral cortex. (
  • RG 12915: a potent 5-hydroxytryptamine-3 antagonist that is an orally effective inhibitor of cytotoxic drug-induced emesis in the ferret and dog. (
  • We envisage that the combination of glutamate and alpha-2 adrenergic antagonists could be potent therapies against neuronal damage following stroke and cardiac arrest. (
  • Although risperidone is a potent D 2 antagonist, which is considered to improve the positive symptoms of schizophrenia, it causes less depression of motor activity and induction of catalepsy than classical neuroleptics. (
  • Partial opioid agonist and potent antagonist, is a potent analgesic that can be administered once a day to block withdrawal symptoms. (
  • Atipamezole, a drug which is not FDA approved for human use, is a potent alpha-2 specific antagonist, which could be used as lifesaving therapy to reverse the adverse effects of an accidental alpha-2 agonist overdose. (
  • It is therefore likely that brain adrenergic alpha-2-receptors mediate the orexigenic effects of neuropeptide Y and beta-endorphin in layer-type chicks. (
  • α1-receptors primarily mediate smooth muscle contraction, but have important functions elsewhere as well. (
  • During exercise, α1-adrenergic receptors in active muscles are attenuated in an exercise intensity-dependent manner, allowing the β2-adrenergic receptors which mediate vasodilation to dominate. (
  • The stress-induced effect appeared to be specific to 5-HT(2A) receptors because stress had no significant impact on other serotonin receptors, as well as histamine H(3) receptor and alpha(2) adrenoceptor signaling in the BLA. (
  • Pharmacological characterization of histamine receptors mediating the elevation of cyclic AMP. (
  • H 1 receptor antagonist any of a large number of agents that block the action of histamine by competitive binding to the H 1 receptor. (
  • Like other 5-HT 2 antagonists, risperidone also binds at alpha (1)-adrenergic receptors and, to a lesser extent, at histamine H1 and alpha (2)-adrenergic receptors [ 2 ]. (
  • A putative effect was also not unmasked by concomitant angiotensin II type 1 receptor blockade with candesartan. (
  • These findings indicate that the PPI-disruptive effect of PCP may be mediated in part by alpha -1 adrenergic receptors and that antagonism of alpha -1 receptors may play a major role in mediating the blockade of PCP-induced deficits in PPI by certain antipsychotics. (
  • Blockade of dopaminergic D2 receptors in the limbic system alleviates positive symptoms of schizophrenia such as hallucinations, delusions, and erratic behavior and speech. (
  • Blockade of serotonergic 5-HT 2 receptors in the mesocortical tract causes an excess of dopamine, resulting in an increase in dopamine transmission and an elimination of core negative symptoms. (
  • Blockade of a2 receptors increases what? (
  • Incubation of rat cerebral cortical slices with the beta-adrenergic agonist isoproterenol causes an increase in alpha 2-adrenergic receptor binding in addition to a decrease in beta-adrenergic receptor binding. (
  • The effects are rapid and reversible, show a parallel time course, and are blocked by sotalol, a beta-adrenergic receptor antagonist. (
  • Several investigations have demonstrated protection against neuronal damage following global and focal ischemia, using antagonist against the N-methyl-d-aspartate (NMDA) receptor. (
  • However, we have not been able to demonstrate a decrease in neuronal damage in the rat following 10 min of bilateral common carotid artery occlusion combined with hypotension, when the animals were pre- or post-treated with the non-competitive NMDA antagonist MK-801. (
  • We propose that an ischemic insult, severe enough to cause prolonged periods of membrane depolarization, induces changes in the membrane properties leading to cycling of calcium ions across the plasmamembrane, which cannot be blocked by noncompetitive NMDA receptor antagonist. (
  • We observed earlier that central alpha-2 adrenoceptor stimulation in mice greatly augments parasympathetic tone. (
  • We conclude that alpha-2 adrenoceptor stimulation has a differential effect on baroreflex HR and vasomotor regulation. (
  • alpha-2 Adrenoceptor stimulation greatly augments baroreflex-mediated bradycardia, most likely by parasympathetic activation. (
  • Alpha1-adrenergic stimulation of phosphatidylinositol-phosphatidic acid turnover in rat parotid cells. (
  • Compounds that bind to and block the stimulation of ADENOSINE A1 RECEPTORS. (
  • Stimulation of alpha-adrenergic receptor augments the production of macrophage-derived tumor necrosis factor. (
  • Upon receptor stimulation with agonist, Gα q and β-γ subunits dissociate to initiate downstream effector pathways. (
  • A vasopressin antagonist that binds to the V2-receptor of LLC-PK, renal epithelial cells is highly laterally mobile but does not effect ligand-induced receptor immobilization. (
  • 1. a substance that tends to nullify the action of another, as a drug that binds to a cellular receptor for a hormone, neurotransmitter, or another drug blocking the action of that substance without producing any physiologic effect itself. (
  • Rauwolscine is known as an Alpha-2 adrenoceptor antagonist (Alpha-2-adrenoceptor blocker). (
  • Calcium mobilization by muscarinic receptors in human astrocytoma cells: measurements with quin 2. (
  • Heterogeneity of muscarinic receptors coupled to phosphoinositide breakdown in guinea pig brain and peripheral tissues. (
  • [1-7] The mechanisms of this spinal action are not clear, but autoradiographic studies have shown the existence of muscarinic receptors, both M 1 and M 2 , in laminae II and III of the spinal cord. (
  • Characterization of alkaline response induced by cholinergic agents in the rat duodenum: involvement of M2 receptors and the calcium-dependent process. (
  • Muscarinic cholinergic receptors on cultured thyroid cells. (
  • Animals were pretreated with either the alpha -1 antagonist prazosin (0, 0.5, 1.0 or 2.5 mg/kg), the alpha -2 antagonist RX821002 (0, 0.2 or 0.4 mg/kg), the M1 muscarinic antagonist pirenzepine (0, 10 or 30 mg/kg) or the GABA-A antagonist pitrazepin (0, 1.0 or 3.0 mg/kg) and then treated with either saline or PCP (1.5 mg/kg). (
  • Binding of the selective alpha 1-adrenergic antagonist [3H]prazosin and the alpha 2-adrenergic antagonist [3H]rauwolscine was used for receptor studies in tissues of prehypertensive (24-day-old) and hypertensive (60-day-old) rats. (
  • Risperidone is a benzisoxazole atypical antipsychotic with high 5-HT 2 and dopamine-D 2 receptor antagonist activity. (
  • Patients should start with 2 mg/day risperidone. (
  • Risperidone Orodispersible Tablets should be administered on a once daily schedule, starting with 2 mg risperidone. (
  • The film-coated tablets contain 1 mg, or 2 mg risperidone. (
  • 2 mg risperidone tablets: Hypromellose 2910 5 mPa.s, propylene glycol, talc, titanium dioxide, orange yellow S aluminum lake. (
  • Risperidone is a selective monoaminergic antagonist with unique properties. (
  • Risperidone is completely absorbed after oral administration, reaching peak plasma concentrations within 1 to 2 hours. (
  • In plasma, risperidone is bound to albumin and alpha 1 -acid glycoprotein. (
  • These effects were related to the increased serum prolactin levels, resulting from the dopamine D2-receptor blocking activity of risperidone. (
  • The adenylate cyclase-coupled vasopressin V2-receptor is highly laterally mobile in membranes of LLC-PK, renal epithelial cells at physiological temperature. (
  • Jans DA, Peters R, Fahrenholz F. Lateral mobility of the phospholipase-C-activating vasopressin V,-type receptor in A7r5 smooth muscle cells: a comparison with the adenylate cyclase-coupled V2-receptor. (
  • Vasopressin V2-receptor mobile fraction and ligand-dependent adenylate cyclase-activity are directly correlated in LLC-PK, renal epithelial cells. (
  • Tolkovsky AM, Levitzki A. Mode of coupling between the (3-adrenergic receptor and adenylate cyclase in turkey erythrocytes. (
  • Tolkovsky AM, Levitzki A. Coupling of a single adenylate cyclase to two receptors: adenosine and catecholamine. (
  • Tolkovsky A, Braun S, Levitzki A. Kinetics of interaction between 3-receptors, GTP-proteins and the catalytic subunit of turkey erythrocyte adenylate cyclase. (
  • Hanski E, Rimon G, Levitzki A. Adenylate cyclase activation by the 3-adrenergic receptor as a diffusion controlled process. (
  • Oxymetazoline inhibits adenylate cyclase by activation of serotonin-1 receptors in the OK cell, an established renal epithelial cell line. (
  • After excluding several alternate hypotheses to explain this anomalous activity of oxymetazoline, we hypothesized that oxymetazoline activates a receptor in OK cells that is negatively coupled to adenylate cyclase but distinct from the alpha 2-adrenergic receptor. (
  • These data indicate that OK cells express a 5HT1 receptor that is negatively coupled to adenylate cyclase and that oxymetazoline is an agonist at these receptors. (
  • Characterization with agonist and antagonist radioligands and relationship to adenylate cyclase. (
  • This product is an aliquot of membranes from Sf9 cells transfected with the human recombinant alpha 2a Adrenergic Receptor. (
  • 5381.2011 1044 British Journal of Pharmacology Introduction Obsessive-compulsive disorder (OCD) is a common neuropsychiatric disorder, affecting roughly 2% of the adult population worldwide OCD is commonly complicated by the co-occurrence of other 'comorbid' mental disorders, notably depression which supervenes in up to two-thirds of clinical cases Multiple layers of evidence link OCD with dysregulation of fronto-striatal neuro-circuitry and associated monoamine systems. (
  • We investigated the α-adrenergic pharmacology of analgesia using models of tactile hypersensitivity induced with chemical stimuli that sensitize pain pathways at spinal or peripheral sites. (
  • Association, dissociation, and saturation studies revealed one site interactions (k -1/k+1 = 1.2 nM, KD = 2.5 nM, Bmax = 160 fmol/mg protein) and competition studies indicated that [3H]rauwolscine labeled the alpha 2-receptor. (
  • Rauwolscine acts predominantly as a α2-adrenergic receptor antagonist. (
  • By blocking the alpha-2-adrenoceptor with Rauwolscine your body will now INCREASE fat burning and DECREASE fat storage . (
  • Rauwolscine is an alpha-2 adrenergic receptor antagonist with little to no activity on alpha-1. (
  • adrenergic receptor antagonists that are optionally substituted with at least one NO or NO.sub.2 moiety and compounds that donate, transfer or release nitric oxide or elevate levels of endogenous endothelium-derived relaxing factor, and methods for treating sexual dysfunctions in males and females. (
  • 2. The composition of claim 1, wherein the compound that stimulates nitric oxide synthesis is L-arginine or OH-arginine. (
  • Blocking the alpha-2 adrenergic receptors promotes the release of nitric oxide , a vasodilator, which relaxes the penile tissue. (
  • An appropriate therapy for RH can be achieved by the addition of second line antihypertensive drugs: antialdosteronic diuretics, central agents, alpha blockers, direct vasodilating agents, and exogenous nitric oxide donors. (
  • Carlos G. Musso and Jose Alfie, "Resistant Hypertension in the Elderly-Second Line Treatments: Aldosterone Antagonists, Central Alpha-Agonist Agents, Alpha-Adrenergic Receptor Blockers, Direct Vasodilators, and Exogenous Nitric Oxide Donors", Cardiovascular & Hematological Agents in Medicinal Chemistry (2014) 12: 170. (
  • This protein is a member of a subfamily of G protein-coupled receptors that regulate neurotransmitter release from sympathetic nerves and from adrenergic neurons in the central nervous system. (
  • The drug lowers both systolic and diastolic blood pressure by activating the central nervous system alpha-2 adrenoreceptors, which results in reduced sympathetic outflow leading to reduced vascular tone. (
  • In these subgroups plasma total and levels of low-density lipoprotein (LDL) cholesterol were inversely correlated with platelet aggregation but directly correlated with platelet receptor density. (
  • Apparent "down-regulation" of human platelet alpha 2-adrenergic receptors is due to retained agonist. (
  • The platelet contains exclusively alpha 2 and the liver mostly (approximately 80%) alpha 1 receptors. (
  • This in vivo PET evidence for alpha(2)/dopaminergic interaction may be relevant to putative actions of atypical antipsychotic medications via adrenergic receptors. (
  • Intracerebroventricular injection of the adrenergic alpha-2-receptor agonist, clonidine, stimulated food intake. (
  • To test the effects in humans, we assessed autonomic vasomotor tone and baroreflex regulation in 9 normal young adults on 2 occasions, once with and once without clonidine. (
  • Accidental overdose (OD) with an alpha-2 agonist (a2a), such as dexmedetomidine (DEX) medetomidine (MED), or clonidine can potentially be life-threatening. (
  • Napamezole, an alpha-2 adrenergic receptor antagonist and monoamine uptake inhibitor in vitro. (
  • Compounds that selectively bind to and activate ADENOSINE A2 RECEPTORS. (
  • Catechols are compounds containing a 1,2-benzenediol moiety. (
  • These are compounds containing an indole moiety, which consists of pyrrolidine ring fused to benzene to form 2,3-dihydroindole. (
  • In this short review article, we outline the rationale for the use of GnRH antagonists in LUTS associated with BPH, summarize briefly the available clinical data (phase II and III trials) with the different compounds, touch upon the proposed mechanisms of action, and try to set perspectives for this field of research. (
  • Tyrosine kinase and GTP-binding protein activating receptors appear to be essentially different in terms of their lateral mobility properties, and it seems plausible to relate these differences to their distinct signal transduction mechanisms. (
  • 1-8 As discussed in chapter 4, lateral movement of hormone-occupied tyrosine kinase receptors is required to effect receptor dimerization which triggers the association of a variety of cytosolic signaling molecules in order to effect signal transduction. (
  • The mobile receptor hypothesis revisited: a mechanistic role for hormone receptor lateral mobility in signal transduction. (
  • Jans DA, Pavo I. A mechanistic role for polypeptide hormone receptor lateral mobility in signal transduction. (
  • Schlessinger J. Signal transduction by allosteric receptor oligomerization. (
  • Ullrich A, Schlessinger J. Signal transduction by receptors with tyrosine kinase activity. (
  • The 5-HT 2A receptor is known primarily to couple to the Gα q signal transduction pathway. (
  • Antagonists bind strongly to the GnRH receptor without inducing signal transduction. (
  • The nucleus tractus solitarii (NTS) densely expresses angiotensin II type 2 receptors (AT2R), which are mainly located on inhibitory gamma-aminobutyric acid (GABA) neurons. (
  • These latter antipsychotics have antagonistic actions at several receptors, including alpha -1 and alpha -2 adrenergic, M1 muscarinic and γ-aminobutyric acid (GABA)-A receptors. (
  • The antagonists for alpha -2, for M1 and for GABA-A receptors had no effect on base-line PPI or on PCP-induced disruptions in PPI. (
  • Accumulated evidence suggests an upregulation of central alpha2-receptors, leading to decreased noradrenergic activity on a central level in MDD patients. (
  • Adrenergic alpha2 receptors (alpha2-adrenoceptors) are members of the adrenergic receptor group of G-protein-coupled receptors that also includes alpha1A, alpha1B, alpha1D, beta1, beta2 and beta3. (
  • The 5HT1 receptor-selective antagonist methiothepin, but not ketanserin (5HT2-selective) or ICS-205,930 (5HT3-selective), blocked the response to both 5HT and oxymetazoline. (
  • However, its efficacy could be mediated through its activity as an antagonist at central dopamine type 2 receptors. (
  • experiments show that the alkaloid increases sexual motivation even in sexually exhausted rats due to its action on the central α 2 -adrenoreceptors found in the locus coeruleus in the brain. (
  • PCP-induced deficits in PPI in rats are resistant to dopamine and serotonin antagonists but can be antagonized by antipsychotics such as clozapine, olanzapine and Seroquel. (
  • In smooth muscle cells of blood vessels the principal effect of activation of these receptors is vasoconstriction. (
  • Resting muscle will not have its α1-adrenergic receptors blocked, and hence the overall effect will be α1-adrenergic-mediated vasoconstriction. (
  • It stimulates both the alpha- and beta- adrenergic systems, causes systemic vasoconstriction and gastrointestinal relaxation, stimulates the heart, and dilates bronchi and cerebral vessels. (
  • Xylometazoline is a direct acting sympathomimetic adrenergic alpha-agonist used to induce systemic vasoconstriction, thereby decreasing nasal congestion. (
  • 2. ____ Vascular smooth muscle cells of most blood vessels have alpha receptors, and activation of vascular smooth muscle alpha receptors causes vasoconstriction. (
  • Two yet to be launched products, Forest Laboratories/Cypress Biosciences's antidepressant milnacipran and Schwarz Pharma's sodium ion channel antagonist/CRMP2 modulator lacosamide (Vimpat), will compete for market share as well as provide the benefit of an additional mechanism of action. (
  • The marked difference in chemical structure translates into a different mechanism of action that is outlined in Figure 2 . (
  • In contrast, the mechanism of action of the antagonist is much simpler. (
  • Intrarenal noradrenaline, phenylephrine and methoxamine responses were determined in the absence and presence of selective α1-adrenoceptor antagonists, 5- methylurapidil (5-MeU), chloroethylclonidine (CeC) and BMY 7378. (
  • Alpha-2 receptors inhibit the release of catecholamine hormones like adrenaline and noradrenaline, so blocking these receptors means higher levels of these stimulatory hormones. (
  • 9-13 Movement of the hormone-occupied receptor is not required subsequent to dimerization, and consistent with this, activated receptors appear to be aggregated and essentially immobile at physiological temperature (see section E, chapter 4). (
  • Adrenergic receptor trafficking is an active physiological process where adrenergic receptors are relocated from one region of the cell to another or from one type of cell to another. (
  • The purpose of this study was thus to investigate effects of receptor antagonists and MT on feeding behavior and hypothalamic physiology. (
  • exerts partial agonistic effects at the mu opioid receptor in the CNS and antagonistic effects at the kappa opioid receptor. (
  • A method of treating an ocular disorder in a subject includes administering to the subject subtherapeutic amounts of two or more agents that inhibit and/or blocks the activation of Gs- or Gq-protein coupled receptors or Gs- or Gq-signaling cascade in ocular cells of the subject, and/or activates Gi-protein coupled receptors, which is induced or triggered by light induced all-trans-retinal generation. (
  • Buprenorphine is a semisynthetic narcotic mixed agonist-antagonist analgesic. (
  • In control rats, administration of 5-HT or alpha-methyl-5-HT, a 5-HT(2) receptor agonist, to basolateral amygdala (BLA) slices dramatically enhanced frequency and amplitude of spontaneous inhibitory postsynaptic currents (sIPSCs). (
  • In stressed rats, the 5-HT(2A) receptor-mediated facilitative actions were severely impaired. (
  • We studied alpha-adrenergic receptors in the cerebral and renal cortex of Milan hypertensive strain (MHS) and normotensive strain (MNS) rats, a genetic model of spontaneous hypertension linked to a kidney abnormality. (
  • The density of these receptors increased similarly with age in MHS and MNS rats. (
  • In the renal cortex, the differences between MHS and MNS rats concerned alpha 2-adrenergic receptors only. (
  • 3: The method of claim 1, wherein the agents comprise at least two of a Gi-coupled dopamine D2 receptor agonist, a Gs-coupled .beta.1 adrenergic receptor antagonist, or a Gq-coupled .alpha.1 adrenergic receptor blocker. (
  • What's awesome about alpha-2 receptors is they're predominantly found in the lower body, abdominal area, and the lower back. (
  • [7] This receptor was first noted for its importance as a target of serotonergic psychedelic drugs such as LSD . (
  • Nonspecific alpha-2 antagonists (a2ANT) such as tolazoline, and naloxone an opioid antagonist, have also been tried with limited but unpredictable success. (
  • Gonadotropin-releasing hormone (GnRH) antagonists represent a new pharmacological class with several potential clinical indications. (
  • It has also been shown to function as a 5-HT1A receptor partial agonist and 5-HT2A and 5-HT2B receptor antagonist. (
  • The 3,3′-diiodo-l-thyronine in Alpha-T2 is a fast acting metabolism booster and thermogenic. (
  • Users love Alpha-T2 because of its clean and effective fat burning capabilities, powerful thermogenic effects, and strong boost in metabolism. (
  • Block, G.A., Pulsinelli, W.A. (1987) Excitatory amino acid receptor antagonists: Failure to prevent ischemic neuronal damage. (