Wakefulness-Promoting Agents: A specific category of drugs that prevent sleepiness by specifically targeting sleep-mechanisms in the brain. They are used to treat DISORDERS OF EXCESSIVE SOMNOLENCE such as NARCOLEPSY. Note that this drug category does not include broadly-acting central nervous system stimulants such as AMPHETAMINES.Receptors, Adrenergic, alpha-2: A subclass of alpha-adrenergic receptors found on both presynaptic and postsynaptic membranes where they signal through Gi-Go G-PROTEINS. While postsynaptic alpha-2 receptors play a traditional role in mediating the effects of ADRENERGIC AGONISTS, the subset of alpha-2 receptors found on presynaptic membranes signal the feedback inhibition of NEUROTRANSMITTER release.Antirheumatic Agents: Drugs that are used to treat RHEUMATOID ARTHRITIS.Arthritis, Rheumatoid: A chronic systemic disease, primarily of the joints, marked by inflammatory changes in the synovial membranes and articular structures, widespread fibrinoid degeneration of the collagen fibers in mesenchymal tissues, and by atrophy and rarefaction of bony structures. Etiology is unknown, but autoimmune mechanisms have been implicated.Receptors, Tumor Necrosis Factor: Cell surface receptors that bind TUMOR NECROSIS FACTORS and trigger changes which influence the behavior of cells.Tumor Necrosis Factor-alpha: Serum glycoprotein produced by activated MACROPHAGES and other mammalian MONONUCLEAR LEUKOCYTES. It has necrotizing activity against tumor cell lines and increases ability to reject tumor transplants. Also known as TNF-alpha, it is only 30% homologous to TNF-beta (LYMPHOTOXIN), but they share TNF RECEPTORS.Antibodies, Monoclonal: Antibodies produced by a single clone of cells.Immunoglobulin G: The major immunoglobulin isotype class in normal human serum. There are several isotype subclasses of IgG, for example, IgG1, IgG2A, and IgG2B.alpha 1-Antitrypsin: Plasma glycoprotein member of the serpin superfamily which inhibits TRYPSIN; NEUTROPHIL ELASTASE; and other PROTEOLYTIC ENZYMES.Receptors, Adrenergic, alpha: One of the two major pharmacological subdivisions of adrenergic receptors that were originally defined by the relative potencies of various adrenergic compounds. The alpha receptors were initially described as excitatory receptors that post-junctionally stimulate SMOOTH MUSCLE contraction. However, further analysis has revealed a more complex picture involving several alpha receptor subtypes and their involvement in feedback regulation.Hormone Antagonists: Chemical substances which inhibit the function of the endocrine glands, the biosynthesis of their secreted hormones, or the action of hormones upon their specific sites.Dopamine Antagonists: Drugs that bind to but do not activate DOPAMINE RECEPTORS, thereby blocking the actions of dopamine or exogenous agonists. Many drugs used in the treatment of psychotic disorders (ANTIPSYCHOTIC AGENTS) are dopamine antagonists, although their therapeutic effects may be due to long-term adjustments of the brain rather than to the acute effects of blocking dopamine receptors. Dopamine antagonists have been used for several other clinical purposes including as ANTIEMETICS, in the treatment of Tourette syndrome, and for hiccup. Dopamine receptor blockade is associated with NEUROLEPTIC MALIGNANT SYNDROME.Dose-Response Relationship, Drug: The relationship between the dose of an administered drug and the response of the organism to the drug.Excitatory Amino Acid Antagonists: Drugs that bind to but do not activate excitatory amino acid receptors, thereby blocking the actions of agonists.Neurokinin-1 Receptor Antagonists: Compounds that inhibit or block the activity of NEUROKININ-1 RECEPTORS.Narcotic Antagonists: Agents inhibiting the effect of narcotics on the central nervous system.Adrenergic alpha-1 Receptor Antagonists: Drugs that bind to and block the activation of ADRENERGIC ALPHA-1 RECEPTORS.Histamine H2 Antagonists: Drugs that selectively bind to but do not activate histamine H2 receptors, thereby blocking the actions of histamine. Their clinically most important action is the inhibition of acid secretion in the treatment of gastrointestinal ulcers. Smooth muscle may also be affected. Some drugs in this class have strong effects in the central nervous system, but these actions are not well understood.Interleukin 1 Receptor Antagonist Protein: A ligand that binds to but fails to activate the INTERLEUKIN 1 RECEPTOR. It plays an inhibitory role in the regulation of INFLAMMATION and FEVER. Several isoforms of the protein exist due to multiple ALTERNATIVE SPLICING of its mRNA.Rats, Sprague-Dawley: 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.Hypoxia-Inducible Factor 1, alpha Subunit: Hypoxia-inducible factor 1, alpha subunit is a basic helix-loop-helix transcription factor that is regulated by OXYGEN availability and is targeted for degradation by VHL TUMOR SUPPRESSOR PROTEIN.Nicotinic Antagonists: Drugs that bind to nicotinic cholinergic receptors (RECEPTORS, NICOTINIC) and block the actions of acetylcholine or cholinergic agonists. Nicotinic antagonists block synaptic transmission at autonomic ganglia, the skeletal neuromuscular junction, and at central nervous system nicotinic synapses.Muscarinic Antagonists: Drugs that bind to but do not activate MUSCARINIC RECEPTORS, thereby blocking the actions of endogenous ACETYLCHOLINE or exogenous agonists. Muscarinic antagonists have widespread effects including actions on the iris and ciliary muscle of the eye, the heart and blood vessels, secretions of the respiratory tract, GI system, and salivary glands, GI motility, urinary bladder tone, and the central nervous system.Adrenergic alpha-Antagonists: Drugs that bind to but do not activate alpha-adrenergic receptors thereby blocking the actions of endogenous or exogenous adrenergic agonists. Adrenergic alpha-antagonists are used in the treatment of hypertension, vasospasm, peripheral vascular disease, shock, and pheochromocytoma.GABA Antagonists: Drugs that bind to but do not activate GABA RECEPTORS, thereby blocking the actions of endogenous GAMMA-AMINOBUTYRIC ACID and GABA RECEPTOR AGONISTS.alpha7 Nicotinic Acetylcholine Receptor: A member of the NICOTINIC ACETYLCHOLINE RECEPTOR subfamily of the LIGAND-GATED ION CHANNEL family. It consists entirely of pentameric a7 subunits expressed in the CNS, autonomic nervous system, vascular system, lymphocytes and spleen.Histamine H1 Antagonists: Drugs that selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine. Included here are the classical antihistaminics that antagonize or prevent the action of histamine mainly in immediate hypersensitivity. They act in the bronchi, capillaries, and some other smooth muscles, and are used to prevent or allay motion sickness, seasonal rhinitis, and allergic dermatitis and to induce somnolence. The effects of blocking central nervous system H1 receptors are not as well understood.Purinergic P1 Receptor Antagonists: Compounds that bind to and block the stimulation of PURINERGIC P1 RECEPTORS.Piperidines: A family of hexahydropyridines.Receptors, Adrenergic, alpha-1: 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.Adrenergic alpha-2 Receptor Antagonists: Drugs that bind to and block the activation of ADRENERGIC ALPHA-2 RECEPTORS.
(1/2042) alpha1-adrenergic receptor subtypes in human peripheral blood lymphocytes.

We investigated the expression of alpha1-adrenergic receptor subtypes in intact human peripheral blood lymphocytes using reverse transcription-polymerase chain reaction (RT-PCR) and radioligand binding assay techniques combined with antibodies against the three subtypes of alpha1-adrenergic receptors (alpha1A, alpha1B, and alpha1D). RT-PCR amplified in peripheral blood lymphocytes a 348-bp alpha1A-adrenergic receptor fragment, a 689-bp alpha1B-adrenergic receptor fragment, and a 540-bp alpha1D-adrenergic receptor fragment. Radioligand binding assay with [3H]prazosin as radioligand revealed a high-affinity binding with a dissociation constant value of 0. 65+/-0.05 nmol/L and a maximum density of binding sites of 175. 3+/-20.5 fmol/10(6) cells. The pharmacological profile of [3H]prazosin binding to human peripheral blood lymphocytes was consistent with the labeling of alpha1-adrenergic receptors. Antibodies against alpha1A-, alpha1B-, and alpha1D-receptor subtypes decreased [3H]prazosin binding to a different extent. This indicates that human peripheral blood lymphocytes express the three alpha1-adrenergic receptor subtypes. Of the three different alpha1-adrenergic receptor subtypes, the alpha1B is the most represented and the alpha1D, the least. Future studies should clarify the functional relevance of alpha1-adrenergic receptors expressed by peripheral blood lymphocytes. The identification of these sites may represent a step for evaluating whether they represent a marker of alpha1-adrenergic receptors in cardiovascular disorders or for assessing responses to drug treatment on these receptors.  (+info)

(2/2042) Modulation of basal intracellular calcium by inverse agonists and phorbol myristate acetate in rat-1 fibroblasts stably expressing alpha1d-adrenoceptors.

In rat-1 fibroblasts stably expressing alpha1d-adrenoceptors BMY 7378, phentolamine, chloroethylclonidine and 5-methyl urapidil decreased basal [Ca2+]i. WB 4101 induced a very small effect on this parameter but when added before the other antagonists it blocked their effect. All these agents inhibited the action of norepinephrine. Phorbol myristate acetate also blocked the effect of norepinephrine and decreased basal [Ca2+]i. Staurosporine inhibited these effects of the phorbol ester. Our results suggest that: (1) alpha1d-adrenoceptors exhibit spontaneous ligand-independent activity, (2) BMY 7378, phentolamine, chloroethylclonidine and 5-methyl urapidil act as inverse agonists and (3) protein kinase C activation blocks spontaneous and agonist-stimulated alpha1d-adrenoceptor activity.  (+info)

(3/2042) Transcriptional regulation of alpha1-adrenoceptor gene in the rat liver during different phases of sepsis.

Changes in alpha1-adrenoceptor (alpha1AR) gene expression in the rat liver during different phases of sepsis were studied. Sepsis was induced by cecal ligation and puncture (CLP). Septic rats exhibit two metabolically distinct phases: an initial hyperglycemic phase (9 h after CLP, early sepsis) followed by a hypoglycemic phase (18 h after CLP; late sepsis). The [3H]prazosin binding studies show that the density of alpha1AR was increased by 30% during the early phase while it was decreased by 24% during the late phase of sepsis. Western blot analyses reveal that alpha1AR protein level was elevated by 48% during early sepsis but was decreased by 55% during late sepsis. Northern blot analyses depict that the steady-state level of alpha1bAR mRNA was enhanced by 21% during the early phase but was declined by 29% during the late phase of sepsis. Nuclear run-off assays show that the transcription rate of alpha1bAR gene transcript was increased by 76% during early sepsis while it was decreased by 29% during late sepsis. The actinomycin D pulse-chase studies indicate that the half-life of alpha1bAR mRNA remained unaffected during the early and the late phases of sepsis. These findings demonstrate that during the early phase of sepsis, the increase in the rate of transcription of alpha1bAR gene paralleled with the elevations in the alpha1bAR mRNA abundance and alpha1AR protein level, while during the late phase of sepsis, the decrease in the rate of transcription of alpha1bAR gene coincided with the declines in the alpha1bAR mRNA abundance and the alpha1AR protein level in the rat liver. These observations indicate that the altered expression of alpha1AR genes in the rat liver during the progression of sepsis was regulated transcriptionally.  (+info)

(4/2042) Facilitation and depression of ATP and noradrenaline release from sympathetic nerves of rat tail artery.

1. Excitatory junction currents (EJCs) were used to measure ATP release; noradrenaline (NA) oxidation currents and fractional overflow of labelled NA, [3H]NA, were used to monitor the release of endogenous and exogenous NA, respectively, from post-ganglionic sympathetic nerves of rat tail artery. 2. During nerve stimulation with 100 pulses at 5-20 Hz the EJCs initially grew in size (maximally by 23 %, at 2-10 Hz), and then depressed, maximally by 68 % at 20 Hz. 3. The peak amplitude of NA oxidation currents in response to nerve stimulation with 100 pulses at 2-20 Hz grew in size with frequency, while the area was independent of frequency and roughly constant. 4. The size of the NA oxidation currents evoked by nerve stimulation with 4-100 pulses at 20 Hz grew linearly with train length between pulses 4-16. Between pulses 20-100 there was a train length-dependent depression of the signal. 5. Fractional overflow of [3H]NA in response to nerve stimulation with 5-100 pulses at 20 Hz behaved similarly to the EJCs. It initially grew roughly linearly between pulses 5-25, and then showed a dramatic depression similar to that of the EJCs. 6. The alpha2-adrenoceptor antagonists rauwolscine and yohimbine increased the overflow of [3H]NA and the amplitude of NA oxidation currents, but not that of the EJCs. 7. It is concluded that during high-frequency stimulation (i) the release of ATP and NA is first briefly facilitated then markedly depressed, (ii) facilitation and depression of the two transmitters are similar in magnitude and time course, and (iii) alpha2-adrenoceptor antagonists differentially modify EJCs and the NA signals. The results obtained in the absence of drugs are compatible with the hypothesis that ATP and NA are released in parallel, while the effects of alpha2-adrenoceptor antagonists seem to suggest dissociated release.  (+info)

(5/2042) Homologous regulation of the alpha2C-adrenoceptor subtype in human hepatocarcinoma, HepG2.

1. Previous studies of the regulation of the alpha2C-adrenoceptor in OK and in transfected cells have led to discrepant conclusions. In the present work, we examined the homologous regulation of the human alpha2C-adrenoceptor in the hepatocarcinoma cell-line, HepG2; a model which expresses this subtype spontaneously. 2. Short-period treatment of the cells with UK14304 provoked neither a diminution of the potency of the alpha2-agonist to inhibit forskolin-induced cyclic AMP-accumulation nor a change in the degree of receptor coupling to G-proteins. 3. Long-period exposure to UK14304 resulted in a large reduction of [3H]MK912 binding sites (55% decrease). The action of UK14304 was dose-dependent (EC50 = 190 +/- 45 nM), rapid (t1/2 = 4.2 h) and reversible. Receptor down-regulation was also observed with clonidine or (-)adrenaline (38 and 36% decrease, respectively) and was blocked by the addition of alpha2-antagonists. 4. Conversely to that observed with alpha2-agonists, treatment of the cells with RX821002 or yohimbine alone, but not with phentolamine, promoted a significant increase of the receptor expression. 5. The observed alterations of receptor density are not the reflection of changes at the alpha2C4 mRNA level. Estimation of the receptor protein turnover and measurement of its half-life demonstrated that down-regulation by alpha2-agonists and up-regulation by alpha2-antagonists, with inverse-agonist efficacy, are respectively the consequence of increased and decreased rate of receptor degradation. 6. In conclusion, our data show that alpha2C-adrenoceptor does not undergo desensitization but is down-regulated in HepG2. The lack of desensitization agrees with previous results obtained in cells transfected with the alpha2C4 gene, but not with observations made in OK cells. Inversely, down-regulation fits with results obtained in OK but not in transfected cells. The reasons for these discrepancies are discussed. Our results also demonstrated that certain alpha2-antagonists behave as inverse agonist on the HepG2 model and thus provide for the first time evidence of inverse efficacy of antagonists on a cellular model expressing physiological level of a wild-type alpha2-adrenoceptor.  (+info)

(6/2042) Effects of heptanol on the neurogenic and myogenic contractions of the guinea-pig vas deferens.

1. The effects of the putative gap junction uncoupler, 1-heptanol, on the neurogenic and myogenic contractile responses of guinea-pig vas deferens were studied in vitro. 2. Superfusion of 2.0 mM heptanol for 20-30 min produced the following reversible changes in the biphasic neurogenic contractile response (8 trials): (i) suppression of both phases; (ii) delayed development of both the first as well as the second phase, accompanied by complete temporal separation of the two phases; (iii) prominent oscillations of force during the second (noradrenergic) phase only. 3. To eliminate prejunctional effects of heptanol, myogenic contractions were evoked by field stimulation of the vas in the presence of suramin (200 microM) and prazosin (1 microM). Heptanol (2.0 mM) abolished these contractions reversibly. 4. These results show that (i) heptanol inhibits both excitatory junction potential (EJP)-dependent and non EJP-dependent contractions of the vas; (ii) a postjunctional site of action of heptanol, probably intercellular uncoupling of smooth muscle cells, contributes to the inhibition of contraction.  (+info)

(7/2042) Nitric oxide mediates sympathetic vasoconstriction at supraspinal, spinal, and synaptic levels.

The purposes of this study were to investigate the level of the sympathetic nervous system in which nitric oxide (NO) mediates regional sympathetic vasoconstriction and to determine whether neural mechanisms are involved in vasoconstriction after NO inhibition. Ganglionic blockade (hexamethonium), alpha1-receptor blockade (prazosin), and spinal section at T1 were used to study sympathetic involvement. NO was blocked with Nomega-nitro-L-arginine methyl ester (L-NAME). Regional blood flow in the mesenteric and renal arteries and terminal aorta was monitored by electromagnetic flowmetry in conscious rats. L-NAME (3-5 mg/kg iv) increased arterial pressure and peripheral resistance. Ganglionic blockade (25 mg/kg iv) significantly reduced the increase in resistance in the mesentery and kidney in intact and spinal-sectioned rats. Ganglionic blockade significantly decreased hindquarter resistance in intact rats but not in spinal-sectioned rats. Prazosin (200 micrograms/kg iv) significantly reduced the increased hindquarter resistance. We concluded that NO suppresses sympathetic vasoconstriction in the mesentery and kidney at the spinal level, whereas hindquarter tone is mediated at supraspinal and synaptic levels.  (+info)

(8/2042) Facilitatory beta2-adrenoceptors on cholinergic and adrenergic nerve endings of the guinea pig trachea.

Using electrical field stimulation of epithelium-denuded intact guinea pig tracheal tube preparations, we studied the presence and role of prejunctional beta2-adrenoceptors by measuring evoked endogenous acetylcholine (ACh) and norepinephrine (NE) release directly. Analysis of ACh and NE was through two HPLC systems with electrochemical detection. Electrical field stimulation (150 mA, 0.8 ms, 16 Hz, 5 min, biphasic pulses) released 29.1 +/- 2.5 pmol ACh/g tissue and 70.2 +/- 6.2 pmol NE/g tissue. Preincubation for 15 min with the selective beta2-adrenoceptor agonist fenoterol (1 microM) increased both ACh and NE overflow to 178 +/- 28 (P < 0.01) and 165 +/- 12% (P < 0.01), respectively, of control values, increases that were abolished completely by the selective beta2-adrenoceptor antagonist ICI-118551 (1 microM). Further experiments with increasing fenoterol concentrations (0.1-100 microM) and different preincubation periods (1, 5, and 15 min) showed a strong and concentration-dependent facilitation of NE release, with maximum response levels decreasing (from nearly 5-fold to only 2.5-fold of control value) with increasing agonist contact time. In contrast, sensitivity of facilitatory beta2-adrenoceptors on cholinergic nerves to fenoterol gradually increased when the incubation period was prolonged; in addition, a bell-shaped concentration-response relationship was found at 15 min of preincubation. Fenoterol concentration-response relationships (15-min agonist preincubation) in the presence of atropine and yohimbine (1 microM each) were similar in the case of NE release, but in the case of ACh release, the bell shape was lost. The results indicate a differential capacity and response time profile of facilitatory prejunctional beta2-adrenoceptors on adrenergic and cholinergic nerve terminals in the guinea pig trachea and suggest that the receptors on adrenergic nerves are more susceptible to desensitization.  (+info)

*  Alpha blocker
However, the most common type of alpha blocker is usually an α1 blocker. Non-selective α-adrenergic receptor antagonists ... "Alpha-Adrenoceptor Antagonists (Alpha-Blockers)" (PDF). British Hypertension Society. "CV Pharmacology , Alpha-Adrenoceptor ... Bylund, D.B. (February 1, 1992). "Subtypes of alpha 1- and alpha 2-adrenergic receptors". The FASEB Journal. 6: 832-839. ... are a class of pharmacological agents that act as antagonists on α-adrenergic receptors (α-adrenoceptors). Historically, alpha- ...
*  Metazosin
... is an antihypertensive alpha-adrenergic antagonist. Trcka, V; König, J; Mácová, S; Smíd, M; Helfert, I; Votavová, M; ... a novel alpha-adrenergic antagonist". Biopharmaceutics & drug disposition. 10 (6): 581-9. PMID 2575403. ...
*  Tiodazosin
... is an alpha-1 adrenergic antagonist. Terazosin Chiang, J; Hermodsson, G; Oie, S (1991). "The effect of alpha 1-acid ... glycoprotein on the pharmacological activity of alpha 1-adrenergic antagonists in rabbit aortic strips". The Journal of ...
*  Prazosin
A larger controlled Phase II "Clinical Trial of the Adrenergic Alpha-1 Antagonist Prazosin for Alcohol Dependence" is currently ... Day, H. E.; Campeau, S.; Watson Jr, S. J.; Akil, H. (1997). "Distribution of alpha 1a-, alpha 1b- and alpha 1d-adrenergic ... "A pilot trial of the alpha-1 adrenergic antagonist, prazosin, for alcohol dependence". Alcoholism: Clinical and Experimental ... Antagonist of alpha-1 adrenoceptors on vascular smooth muscle, thereby inhibiting the vasoconstrictor effect of circulating and ...
*  Pelvic pain
Yang G, Wei Q, Li H, Yang Y, Zhang S, Dong Q (2006). "The effect of alpha-adrenergic antagonists in chronic prostatitis/chronic ...
*  Chronic prostatitis/chronic pelvic pain syndrome
Yang G, Wei Q, Li H, Yang Y, Zhang S, Dong Q; Wei; Li; Yang; Zhang; Dong (2006). "The effect of alpha-adrenergic antagonists in ... Alpha blockers and/or antibiotics appear to be the most effective with NSAIDs such as ibuprofen providing lesser benefit. ... The effectiveness of alpha blockers (tamsulosin, alfuzosin) is questionable in men with CPPS. A 2006 meta-analysis found that ... He, L.; Wang, Y.; Long, Z.; Jiang, C. (Dec 2009). "Clinical Significance of IL-2, IL-10, and TNF-alpha in Prostatic Secretion ...
*  Olney's lesions
Conversely, coadministration of NMDA-antagonists with alpha-2 adrenergic antagonists, like yohimbine could theoretically ... Drugs that work to suppress NAN include anticholinergics, benzodiazepines, barbiturates and agonists at the alpha-2 adrenergic ... D.Wozniak - NMDA Antagonist Neurotoxicity: Mechanism and Prevention] Olney J, Labruyere J, Wang G, Wozniak D, Price M, Sesma M ... The potency of the drugs in producing these neurotoxic changes corresponded with their potency as NMDA antagonists: i.e. MK-801 ...
*  C17H19N3O
... a reversible nonselective alpha-adrenergic antagonist Piberaline, a psychoactive drug. ...
*  Bunazosin
Systemic Alpha-1 adrenergic receptor antagonists have been implicated in Intraoperative Floppy Iris Syndrome (IFIS). Bunazosin ... Bunazosin (INN) is an alpha 1 antagonist. Bunazosin was initially developed to treat benign prostatic hyperplasia (BPH). It has ...
*  Alpha-1 blocker
Prazosin has been established as an effective and safe, brain active alpha-1 adrenergic receptor antagonist. It can be used ... Alpha-1 blockers (also called alpha-adrenergic blocking agents) constitute a variety of drugs that block alpha-1-adrenergic ... DrugDigest - Alpha blockers RxList.com - Tamsulosin alpha-Adrenergic Blockers at the US National Library of Medicine Medical ... Alpha-1 blockers have no effect on renin release or cardio output. Alpha-1 blocker, blocks alpha receptors and it relaxes the ...
*  Boldine
In addition, it has alpha-adrenergic antagonist activities in vascular tissue, and it has also been reported to have ...
*  Transurethral needle ablation of the prostate
... needle ablation of the prostate as an alternative to transurethral resection of the prostate when alpha-adrenergic antagonist ...
*  Nicergoline
... is an ergot alkaloid derivative that acts as a potent and selective alpha-1A adrenergic receptor antagonist. The ... Persons suffering from acute bleeding, myocardial infarction (heart conditions), hypertension, bradycardia or using alpha or ... "Selective blockade by nicergoline of vascular responses elicited by stimulation of alpha 1A-adrenoceptor subtype in the rat". ...
*  Sympatholytic
They are primarily postsynaptic adrenergic receptor antagonists (alpha and beta adrenergic receptor antagonists, or "blockers ... ICI-118,551 Highly selective β2-adrenergic receptor antagonist - No known clinical applications, but used in experiments due to ... α1 antagonist) Doxazosin (alpha blocker) Beta blockers Non-selective agents Alprenolol Bucindolol Carteolol Carvedilol (has ... preventing postsynaptic adrenergic receptor activation and downstream signaling. Another way to inhibit adrenergic receptor ...
*  Benzoctamine
One study showed that benzoctamine, a serotonin and alpha-adrenergic antagonist, does not reduce blood pressure through a ... A possible treatment for hypertension is blocking peripheral vascular seretonergic neurons or alpha-adrenergic neurons on ... "Evidence that blood pressure reduction by serotonin antagonists is related to alpha receptor blockade in spontaneously ... Other animal studies also point to the drug as a possible mechanism by which to reduce blood pressure through the adrenergic ...
*  Rauwolscine
... a specific antagonist radioligand for brain alpha 2-adrenergic receptors". European Journal of Pharmacology. 76 (4): 461-4. doi ... Rauwolscine acts predominantly as a α2-adrenergic receptor antagonist. It has also been shown to function as a 5-HT1A receptor ... Wainscott DB, Sasso DA, Kursar JD, Baez M, Lucaites VL, Nelson DL (January 1998). "[3H]Rauwolscine: an antagonist radioligand ... Perry BD, U'Prichard DC (December 1981). "[3H]rauwolscine (alpha-yohimbine): ...
*  Azinphos-methyl
... a cholinergic and alpha-1 adrenergic antagonist, to achieve a shorter recovery time. Treatment with a combination of different ... Competitive antagonists of AChE can be used for pre-treatment. They can reduce mortality, which is caused by exposure to AzM. ... These two treatments are also used together, some patients are namely treated with atropine (a competitive antagonist of AChE) ...
*  Methylergometrine
... is a partial agonist/antagonist on serotonergic, dopaminergic and alpha-adrenergic receptors. Its specific ... dopaminergic and adrenergic receptors". In Vladimír Křen,Ladislav Cvak. Ergot: the genus Claviceps. CRC Press. pp. 411-440. ...
*  Naftopidil
... is a drug used in benign prostatic hypertrophy which acts as a selective α1-adrenergic receptor antagonist or alpha blocker. ...
*  Abanoquil
... is an α1-adrenergic receptor antagonist. Alpha blocker Tham, TC; Guy, S; Shanks, RG; Harron, DW (1992). "Dose-dependent alpha 1 ... antagonist activity of the anti-arrhythmic drug, abanoquil (UK-52,046), without reduction in blood pressure in man". British ...
*  Fenmetozole
"Effect of methoxy substitution on the adrenergic activity of three structurally related alpha 2-adrenoreceptor antagonists". ... It acts as an α2-adrenergic receptor antagonist similarly to other imidazoles like idazoxan. It was never marketed. ... Fenmetozole (DH-524) is a drug which was patented as an antidepressant, but was later studied as an antagonist of the effects ...
*  L-765,314
... is a drug which acts as a potent and selective antagonist for the Alpha-1 adrenergic receptor subtype α1B. It has ... Yang XP, Chiba S (August 2002). "Effects of L-765,314, a selective and potent alpha 1B-adrenoceptor antagonist, on periarterial ... a potent and selective alpha1b adrenergic receptor antagonist ". Journal of Medicinal Chemistry. 41 (8): 1205-8. doi:10.1021/ ... alpha(1D)-, and alpha(2)-adrenoceptors". European Journal of Pharmacology. 613 (1-3): 86-92. doi:10.1016/j.ejphar.2009.04.011. ...
*  Tiamenidine
... relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists". Journal ... It acts as a centrally-acting α1 and α2 adrenergic receptor antagonist (with IC50 4.85 μM and 0.0091 μM, respectively). In ... "Electrophysiologic and Hemodynamic Effects of Chronic Oral Therapy With the Alpha 2-agonists Clonidine and Tiamenidine in ...
*  Alpha-1 adrenergic receptor
... relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists". Journal ... The alpha-1 (α1) adrenergic receptor is a G protein-coupled receptor (GPCR) associated with the Gq heterotrimeric G-protein. It ... Note that only active muscle α1-adrenergic receptors will be blocked. Resting muscle will not have its α1-adrenergic receptors ... Adrenergic receptor Graham, Robert (May 1, 1996). "α1-Adrenergic Receptor Subtypes Molecular Structure, Function, and Signaling ...
*  Alpha-1B adrenergic receptor
Antagonists L-765,314 Risperidone Alpha-1B adrenergic receptor has been shown to interact with AP2M1. A role in regulation of ... 1994). "Cloning, expression and characterization of human alpha adrenergic receptors alpha 1a, alpha 1b and alpha 1c". Biochem ... The alpha-1B adrenergic receptor (α1B adrenoreceptor), also known as ADRA1B, is an alpha-1 adrenergic receptor, and also ... There are 3 alpha-1 adrenergic receptor subtypes: alpha-1A, -1B and -1D, all of which signal through the Gq/11 family of G- ...
*  Cannabigerol
CBG has been found to act as a high affinity α2-adrenergic receptor agonist, moderate affinity 5-HT1A receptor antagonist, and ... "Evidence that the plant cannabinoid cannabigerol is a highly potent alpha(2)-adrenoceptor agonist and moderately potent 5HT ... It also binds to the CB2 receptor as an antagonist. CBG does not trigger THC-like activity in mice, rats, gerbils and non-human ... Colon carcinogenesis is inhibited by the TRPM8 antagonist cannabigerol, a Cannabis-derived non-psychotropic cannabinoid ...
*  5-HT2A receptor
... related to ketanserin such as ritanserin are more selective 5-HT2A receptor antagonists with low affinity for alpha-adrenergic ... Other antagonists are MDL-100,907 (prototype of another new series of 5-HT2A antagonists) and cyproheptadine. Pizotifen is a ... Trazodone is a potent 5-HT2A antagonist, as well as an antagonist on other serotonin receptors. Mirtazapine is a 5-HT2A, 5-HT2C ... These cells need to express both the alpha 2-6-linked sialic acid component of the 5-HT2A receptor in order to endocytose JCV. ...
Rev-Eyes
        -
        Adrenergic alpha-Antagonists,  Antimydriatics,  Ophthalmologicals,  ATC:S01EX02  Rev-Eyes - Adrenergic alpha-Antagonists, Antimydriatics, Ophthalmologicals, ATC:S01EX02
Dapiprazole is an alpha-adrenergic blocking agent. It produces miosis by blocking the alpha-adrenergic receptors on the dilator ... Used in the treatment of iatrogenically induced mydriasis produced by adrenergic (phenylephrine) or parasympatholytic ( ...
more infohttp://pharmacycode.com/Rev-Eyes.html
Blavin
        -
        Antineoplastic Agents,  Adrenergic alpha-Antagonists,  Platelet Aggregation Inhibitors,  ATC:G04CA03  Blavin - Antineoplastic Agents, Adrenergic alpha-Antagonists, Platelet Aggregation Inhibitors, ATC:G04CA03
As an alpha-adrenergic blocking agent, terazosin is used to treat hypertension and benign prostatic hypertrophy (BPH). ...
more infohttp://pharmacycode.com/Blavin.html
Familial Dysautonomia Medication: Benzodiazepines, H2 receptor antagonists, Alpha-adrenergic agonists, Corticosteroids  Familial Dysautonomia Medication: Benzodiazepines, H2 receptor antagonists, Alpha-adrenergic agonists, Corticosteroids
Alpha-adrenergic agonists. Class Summary. These agents stimulate alpha-adrenoreceptors in brain stem, activating an inhibitory ... A central alpha-adrenergic agonist that suppresses peripheral release of norepinephrine, resulting in lower blood pressure; ... A pure peripheral alpha-adrenergic agonist, which causes peripheral vasoconstriction and raises blood pressure without ... H2 receptor antagonists. Class Summary. These agents are reversible competitive blockers of histamine at the H2 receptors, ...
more infohttps://emedicine.medscape.com/article/1200921-medication
Frontiers | Acute Urinary Morbidity Following Stereotactic Body Radiation Therapy for Prostate Cancer with Prophylactic Alpha...  Frontiers | Acute Urinary Morbidity Following Stereotactic Body Radiation Therapy for Prostate Cancer with Prophylactic Alpha...
Prophylactic alpha-adrenergic antagonists were initiated five days prior to SBRT and continued until resolution of urinary ... Prophylactic alpha-adrenergic antagonists were initiated five days prior to SBRT and continued until resolution of urinary ... Conclusions: SBRT for localized prostate cancer with utilization of prophylactic alpha-adrenergic antagonist and UDR was well ... rates of acute urinary morbidity following SBRT for localized prostate cancer with prophylactic alpha-adrenergic antagonist ...
more infohttps://www.frontiersin.org/articles/10.3389/fonc.2016.00122/full
Alpha Blockers (Alpha Adrenergic Antagonists)  Alpha Blockers (Alpha Adrenergic Antagonists)
... alpha 1 or alpha 2):. *Selective alpha antagonists only block alpha 1 receptors and are more commonly used for treatment of ... Nonselective alpha antagonists (alpha 1 and alpha 2 blockers) are used in the treatment of various types of peripheral vascular ... Potential side effects of alpha blockers. Selective alpha antagonists (alpha 1 blockers) can cause one or more of the following ... Selective alpha antagonists (alpha 1 blockers) include prazosin, terazosin and doxazosin. These drugs are sometimes used to ...
more infohttp://drugs.nmihi.com/alpha-blockers.htm
Alpha-adrenergic antagonist | Article about alpha-adrenergic antagonist by The Free Dictionary  Alpha-adrenergic antagonist | Article about alpha-adrenergic antagonist by The Free Dictionary
Find out information about alpha-adrenergic antagonist. 1. the first letter in the Greek alphabet , a vowel transliterated as a ... 2. Brit the highest grade or mark, as in an examination 3. a. involving or relating... Explanation of alpha-adrenergic ... alpha. (redirected from alpha-adrenergic antagonist). Also found in: Dictionary, Thesaurus, Medical, Legal, Financial. alpha. 1 ... Alpha-adrenergic antagonist , Article about alpha-adrenergic antagonist by The Free Dictionary https://encyclopedia2. ...
more infohttps://encyclopedia2.thefreedictionary.com/alpha-adrenergic+antagonist
Opioid Abuse Medication: Opioid analgesics, Analgesics, Opioid Partial Agonist, Opioid Partial Agonist/Opioid Antagonist,...  Opioid Abuse Medication: Opioid analgesics, Analgesics, Opioid Partial Agonist, Opioid Partial Agonist/Opioid Antagonist,...
Central alpha-2 adrenergic agonist that binds to receptors on adrenergic neurons, resulting in reduced release of ... Alpha 2 adrenergic agonists. Class Summary. Used for mitigation of withdrawal symptoms to facilitate abrupt opioid ... Buprenorphine is a semisynthetic narcotic mixed agonist-antagonist analgesic. Naloxone is a potent antagonist at the mu opioid ... Opioid Antagonists. Class Summary. Reverses opioid effects by inhibiting opioid agonists at receptor sites. ...
more infohttps://emedicine.medscape.com/article/287790-medication
Imidazoline .alpha.-adrenergic receptor antagonist compounds in combination     with nitric oxide donors, compositions and...  Imidazoline .alpha.-adrenergic receptor antagonist compounds in combination with nitric oxide donors, compositions and...
... alpha.-adrenergic receptor antagonists, compositions comprising .alpha.-adrenergic receptor antagonists that are optionally ... adrenergic receptor antagonists: NO.sub.n -.alpha.-antagonists where n is 1 or 2. The .alpha.-adrenergic antagonists can be ... A kit comprising an imidazoline .alpha.-adrenergic receptor antagonist, wherein the imidazoline .alpha.-adrenergic receptor ... 1. A composition comprising an imidazoline .alpha.-adrenergic receptor antagonist, wherein the imidazoline .alpha.-adrenergic ...
more infohttp://www.patentgenius.com/patent/6514934.html
3H]rauwolscine (alpha-yohimbine): a specific antagonist radioligand for brain alpha 2-adrenergic receptors.  - PubMed - NCBI  3H]rauwolscine (alpha-yohimbine): a specific antagonist radioligand for brain alpha 2-adrenergic receptors. - PubMed - NCBI
3H]rauwolscine (alpha-yohimbine): a specific antagonist radioligand for brain alpha 2-adrenergic receptors.. Perry BD, ... 3H]Rauwolscine, a specific and potent alpha 2-antagonist radioligand, was used to characterize alpha 2-receptor binding in ... These results suggest that [3H]rauwolscine specifically labels both the high and low affinity states of the alpha 2-receptor in ... rauwolscine labeled the alpha 2-receptor. Agonists inhibited [3H]rauwolscine binding in a shallow, GTP-sensitive manner. ...
more infohttps://www.ncbi.nlm.nih.gov/pubmed/6276200
Nuedexta in Treatment-Resistant Major Depression - Full Text View - ClinicalTrials.gov  Nuedexta in Treatment-Resistant Major Depression - Full Text View - ClinicalTrials.gov
Adrenergic alpha-Antagonists. Adrenergic Antagonists. Adrenergic Agents. Anti-Arrhythmia Agents. Antimalarials. Antiprotozoal ... Excitatory Amino Acid Antagonists. Excitatory Amino Acid Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Ketamine - a glutamate N-methyl-d-aspartate (NMDA) receptor antagonist - has now been demonstrated in several studies to bring ... The current project aims to test the safety, tolerability and efficacy of Nuedexta - containing the NMDA antagonist ...
more infohttps://clinicaltrials.gov/show/NCT01882829
Lumbar Spinal Fibrosis and TNF Alpha Inhibition - Full Text View - ClinicalTrials.gov  Lumbar Spinal Fibrosis and TNF Alpha Inhibition - Full Text View - ClinicalTrials.gov
Adrenergic alpha-Antagonists. Adrenergic Antagonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... TNF-alpha is the main cytokine implicated in the formation of lumbar spinal fibrosis. Inhibiting TNF-alpha could significantly ... Lumbar Spinal Fibrosis and TNF Alpha Inhibition. The safety and scientific validity of this study is the responsibility of the ... Efficacy of TNF-alpha Inhibition in Sciatica With Post-operative Lumbar Spinal Fibrosis. ...
more infohttps://www.clinicaltrials.gov/ct2/show/NCT00385086
Hypertension Management for Specific Comorbid Diseases  Hypertension Management for Specific Comorbid Diseases
ADRENERGIC BETA-ANTAGONISTS; ADRENERGIC ALPHA-ANTAGONISTS; ANGIOTENSIN-CONVERTING ENZYME INHIBITORS; CALCIUM CHANNEL BLOCKERS; ... Antihypertensive agents include diuretics, alpha-adrenergic and beta-adrenergic antagonists, angiotensin-converting enzyme ...
more infohttps://fpnotebook.com/CV/Htn/HyprtnsnMngmntFrSpcfcCmrbdDss.htm
Paradoxical effect of phentolamine on aqueous flow in the rabbit.  Paradoxical effect of phentolamine on aqueous flow in the rabbit.
... nonselective alpha-adrenergic blockade on aqueous flow. This study used pentobarbital-anesthetized rabbits (n=7), in which the ... 0/Adrenergic alpha-Antagonists; 50-60-2/Phentolamine From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine ... Adrenergic alpha-Antagonists / pharmacology*. Animals. Aqueous Humor / drug effects*, physiology. Blood Flow Velocity / drug ... PURPOSE: The aim of this study was to assess the effects of acute systemic, nonselective alpha-adrenergic blockade on aqueous ...
more infohttp://www.biomedsearch.com/nih/Paradoxical-effect-phentolamine-aqueous-flow/17341146.html
Nonnoradrenergic mechanism of reflex cutaneous vasoconstriction in men.  Nonnoradrenergic mechanism of reflex cutaneous vasoconstriction in men.
Forearm sites (,1 cm(2)) were pretreated with: 1) yohimbine (Yoh; 5 mM id) to antagonize alpha-adrenergic receptors, 2) ... 0/Adrenergic alpha-Antagonists; 0/Receptors, Adrenergic, alpha; 0/Receptors, Adrenergic, beta; 146-48-5/Yohimbine; 51-41-2/ ... to antagonize alpha-adrenergic receptors, 2) Yoh plus propranolol (5 mM Yoh-1 mM PR id) to block alpha- and beta-adrenergic ... Adrenergic alpha-Antagonists / pharmacology*. Blood Pressure. Forearm / blood supply. Humans. Idazoxan / pharmacology. Laser- ...
more infohttp://www.biomedsearch.com/nih/Nonnoradrenergic-mechanism-reflex-cutaneous-vasoconstriction/11247759.html
Dutasteride Capsules - FDA prescribing information, side effects and uses  Dutasteride Capsules - FDA prescribing information, side effects and uses
Combination with Alpha-adrenergic Antagonist. Dutasteride Capsules in combination with the alpha-adrenergic antagonist, ... Approximately 52% of subjects had previous exposure to 5 alpha-reductase inhibitor or alpha adrenergic antagonist treatment. Of ... Combination with Alpha-adrenergic Antagonist. The recommended dose of dutasteride is 1 capsule (0.5 mg) taken once daily and ... Alpha Adrenergic Antagonists: In a single-sequence, crossover trial in healthy volunteers, the administration of tamsulosin or ...
more infohttps://www.drugs.com/pro/dutasteride-capsules.html
Effects of alpha, beta 1, and beta 2 adrenergic antagonists on...  Effects of alpha, beta 1, and beta 2 adrenergic antagonists on...
... and beta 2 adrenergic antagonists on the Na and K concentrations of sympathetic-nerve stimulated rat saliva.: Selective alpha ... Effects of alpha, beta 1, and beta 2 adrenergic antagonists on the Na and K concentrations of sympathetic-nerve stimulated rat ... Selective alpha and beta 1 and beta 2 adrenergic antagonists were used with electrical stimulation of the sympathetic ...
more infohttps://www.mysciencework.com/publication/show/effects-alpha-beta-1-beta-2-adrenergic-antagonists-na-k-concentrations-sympathetic-nerve-stimulated-rat-saliva-7a4d7ecf
Heart-and-Stroke-Encyclopedia  Heart-and-Stroke-Encyclopedia
These drugs are also called alpha-adrenergic antagonists, alpha-adrenergic blocking agents and alpha-adrenergic blockers. ... alpha-adrenergic antagonists and alpha-adrenergic blockers.. Related: Types of Blood Pressure Medications. alpha blockers Alpha ... alpha adrenergic antagonists Alpha-adrenergic antagonists are drugs used to lower blood pressure. They work by relaxing the ... These drugs are also called alpha blockers, alpha-adrenergic antagonists and alpha-adrenergic blocking agents. ...
more infohttp://www.heart.org/HEARTORG/Encyclopedia/Heart-and-Stroke-Encyclopedia_UCM_445084_Encyclopedia.jsp?levelSelected=27
Heart-Encyclopedia - chain of survival  Heart-Encyclopedia - chain of survival
These drugs are also called alpha-adrenergic antagonists, alpha-adrenergic blocking agents and alpha-adrenergic blockers. ... alpha-adrenergic antagonists and alpha-adrenergic blockers.. Related: Types of Blood Pressure Medications. alpha blockers Alpha ... alpha adrenergic antagonists Alpha-adrenergic antagonists are drugs used to lower blood pressure. They work by relaxing the ... These drugs are also called alpha blockers, alpha-adrenergic antagonists and alpha-adrenergic blocking agents. ...
more infohttp://www.heart.org/HEARTORG/Encyclopedia/Heart-Encyclopedia_UCM_445084_Encyclopedia.jsp?levelSelected=3&title=chain%20of%20survival
  • Therefore, alpha blockers relieve cardiac stress by slowing the heart rate and reducing the force of heart muscle contractions (the pumping action). (nmihi.com)
  • Alpha 1 blockers decrease resistance within blood vessels and increase vein capacity, increasing the flow of blood in the heart and reducing cardiac output - a measure of the heart's workload. (nmihi.com)
  • This study reports rates of acute urinary morbidity following SBRT for localized prostate cancer with prophylactic alpha-adrenergic antagonist utilization and urethral dose reduction (UDR). (frontiersin.org)
  • Stereotactic body radiation therapy for localized prostate cancer with utilization of prophylactic alpha-adrenergic antagonist and UDR was well tolerated as determined by acute urinary function and bother, and symptoms were comparable to those observed following conventionally fractionated external beam radiation therapy (EBRT). (frontiersin.org)
  • Alpha blockers are non-habit-forming medications. (nmihi.com)
  • Because they affect stress hormones, alpha blockers result in a lowering of blood pressure (the force of blood against artery walls). (nmihi.com)
  • Alpha 1 blockers have also been found effective in the prevention and treatment of post-traumatic stress disorder, particularly in reducing trauma-related nightmares. (nmihi.com)
  • Any confirmed increase from the lowest PSA value while on dutasteride may signal the presence of prostate cancer and should be evaluated, even if PSA levels are still within the normal range for men not taking a 5 alpha-reductase inhibitor. (drugs.com)
  • Patients with previously demonstrated, clinically significant hypersensitivity (e.g., serious skin reactions, angioedema) to dutasteride or other 5 alpha-reductase inhibitors [see Adverse Reactions (6.2) ]. (drugs.com)
  • Patients with previously demonstrated, clinically significant hypersensitivity (e.g., serious skin reactions, angioedema) to dutasteride or other 5 alpha-reductase inhibitors. (nih.gov)
  • In 2001, Compaq sold all Alpha intellectual property to Intel and announced it would switch its high-end servers to Intel's Itanium processors by 2004. (thefreedictionary.com)
  • Used in the treatment of iatrogenically induced mydriasis produced by adrenergic (phenylephrine) or parasympatholytic (tropicamide) agents used in certain eye examinations. (pharmacycode.com)
  • These agents stimulate alpha-adrenoreceptors in brain stem, activating an inhibitory neuron, which in turn results in reduced sympathetic outflow. (medscape.com)
  • 5 alpha-reductase inhibitors may increase the risk of development of high-grade prostate cancer. (drugs.com)