OrganismsDiseasesChemicals and DrugsPhenomena and Processes
Wakefulness-Promoting AgentsReceptors, Adrenergic, alpha-2Antirheumatic AgentsArthritis, RheumatoidReceptors, Tumor Necrosis FactorTumor Necrosis Factor-alphaAntibodies, MonoclonalImmunoglobulin Galpha 1-AntitrypsinReceptors, Adrenergic, alphaHormone AntagonistsDopamine AntagonistsDose-Response Relationship, DrugExcitatory Amino Acid AntagonistsNeurokinin-1 Receptor AntagonistsNarcotic AntagonistsAdrenergic alpha-1 Receptor AntagonistsHistamine H2 AntagonistsInterleukin 1 Receptor Antagonist ProteinRats, Sprague-DawleyHypoxia-Inducible Factor 1, alpha SubunitNicotinic AntagonistsMuscarinic AntagonistsAdrenergic alpha-AntagonistsGABA Antagonistsalpha7 Nicotinic Acetylcholine ReceptorHistamine H1 AntagonistsPurinergic P1 Receptor AntagonistsPiperidinesReceptors, Adrenergic, alpha-1Adrenergic alpha-2 Receptor Antagonists
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.

alpha1-adrenergic receptor subtypes in human peripheral blood lymphocytes. (1/2042)

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)

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

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)

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

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)

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

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)

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

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)

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

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)

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

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)

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

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-blocking agent synonyms, alpha-blocking agent antonyms - FreeThesaurus.comAlpha-blocking agent synonyms, alpha-blocking agent antonyms - FreeThesaurus.com
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Phencyclidine-Induced Deficits in Prepulse Inhibition of Startle are Blocked by Prazosin, an Alpha-1 Noradrenergic Antagonist |...Phencyclidine-Induced Deficits in Prepulse Inhibition of Startle are Blocked by Prazosin, an Alpha-1 Noradrenergic Antagonist |...
Several important results were obtained from the present studies. First, in accordance with many previous reports, PCP was found repeatedly to disrupt PPI (Bakshi and Geyer, 1995; Bakshi et al., 1994; Mansbach and Geyer, 1989; Swerdlow et al., 1996; Wiley, 1994; Varty and Higgins, 1994; Johansson et al., 1994b). Second, the selective alpha-1 noradrenergic antagonist prazosin prevented the PCP-induced deficit in PPI. This effect was produced by multiple prazosin doses, was observed over multiple prepulse intensities and was replicated in a second separate experiment. Finally, selective antagonists for eitheralpha-2 (RX821002), muscarinic M1 (pirenzepine) or GABA-A (pitrazepin) receptors had no effect on the disruption of PPI produced by PCP. Taken together, these results indicate strongly that the impairment of sensorimotor gating induced by PCP involves the presumably indirect activation of alpha-1 adrenergic receptors, but probably not alpha-2, M1 or GABA-A receptors.. To the best of our ...
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Alpha-blockers, also known as α-blockers or α-adrenoreceptor antagonists, are a class of pharmacological agents that act as antagonists on α-adrenergic receptors (α-adrenoceptors). Historically, alpha-blockers were used as a tool for pharmacologic research to develop a greater understanding of the autonomic nervous system. Using alpha blockers, scientists began characterizing arterial blood pressure and central vasomotor control in the autonomic nervous system. Today, they can be used as clinical treatments for a limited number of diseases. Although alpha blockers can only treat a small range of diseases, some of them have clinical uses, such as having the ability to treat hypertension, Raynauds disease, Congestive Heart Failure, erectile dysfunction, etc. Generally speaking, all of these treatments function by binding an α-blocker to α receptors in the arteries and smooth muscle. Ultimately, this relaxes the smooth muscle or blood vessels, which increases fluid flow in these entities. ...
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Effects of β-adrenoceptor antagonists on the hepatic mixed-function oxygenases in the rat - Surrey Research Insight Open AccessEffects of β-adrenoceptor antagonists on the hepatic mixed-function oxygenases in the rat - Surrey Research Insight Open Access
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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NIOSHTIC-2 Publications Search - 20036435 - Acute dilation to alpha(2)-adrenoceptor antagonists uncovers dual constriction and...NIOSHTIC-2 Publications Search - 20036435 - Acute dilation to alpha(2)-adrenoceptor antagonists uncovers dual constriction and...
BACKGROUND AND PURPOSE: In mouse tail arteries, selective alpha(2)-adrenoceptor antagonism with rauwolscine caused powerful dilation during constriction to the alpha(1)-adrenoceptor agonist phenylephrine. This study therefore assessed phenylephrines selectivity at vascular alpha-adrenoceptors and the mechanism(s) underlying dilation to rauwolscine. EXPERIMENTAL APPROACH: Mouse isolated tail arter
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Treating BPH | SexHealthMatters.org
Among medical therapies used to treat BPH, alpha-adrenergic blockers tend to be used most. There are 4 alpha blocker drugs used to treat BPH: Cardura, Flomax, Hytrin, and Uroxatral.
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https://en.wikipedia.org/wiki/Piperoxan
TiamenidineTiamenidine
... relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists". Journal ... Alpha-1 adrenergic receptor agonists, Alpha-2 adrenergic receptor agonists, Antihypertensive agents, Chloroarenes, Imidazolines ... It is a centrally-acting α2 adrenergic receptor agonist (IC50 = 9.1 nM). It also acts as an α1-adrenergic receptor agonist to a ... Roden DM, Nadeau JH, Primm RK (June 1988). "Electrophysiologic and hemodynamic effects of chronic oral therapy with the alpha 2 ...
https://en.wikipedia.org/wiki/Tiamenidine
Urologic chronic pelvic pain syndromeUrologic chronic pelvic pain syndrome
Yang G, Wei Q, Li H, Yang Y, Zhang S, Dong Q (2006). "The effect of alpha-adrenergic antagonists in chronic prostatitis/chronic ...
https://en.wikipedia.org/wiki/Urologic_chronic_pelvic_pain_syndrome
TiodazosinTiodazosin
"The effect of alpha 1-acid glycoprotein on the pharmacological activity of alpha 1-adrenergic antagonists in rabbit aortic ... Tiodazosin is an α1-adrenergic receptor antagonist. Terazosin Chiang, J; Hermodsson, G; Oie, S (1991). " ... Alpha-1 blockers, Quinazolines, Oxadiazoles, Thioethers, All stub articles, Pharmacology stubs). ...
https://en.wikipedia.org/wiki/Tiodazosin
5-HT2A receptor5-HT2A receptor
... related to ketanserin such as ritanserin are more selective 5-HT2A receptor antagonists with low affinity for alpha-adrenergic ... Another antagonist is cyproheptadine. Pizotifen is a non-selective antagonist. LY-367,265 - dual 5-HT2A antagonist / SSRI with ... Trazodone is a potent 5-HT2A antagonist, as well as an antagonist on other serotonin receptors. Brexpiprazole an atypical ... However, there is at least one antagonist at this site which has been shown to up-regulate 5-HT2A receptors. Additionally, a ...
https://en.wikipedia.org/wiki/5-HT2A_receptor
SympatholyticSympatholytic
They are primarily postsynaptic adrenergic receptor antagonists (alpha and beta adrenergic receptor antagonists, or "blockers ... Prazosin is an α1-blocker that acts as an inverse agonist at alpha-1 adrenergic receptors. Raskind and colleagues studied the ... 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 ...
https://en.wikipedia.org/wiki/Sympatholytic
AbanoquilAbanoquil
... is an α1-adrenergic receptor antagonist. Alpha blocker Tham TC, Guy S, Shanks RG, Harron DW (April 1992). "Dose-dependent alpha ... Alpha-1 blockers, Quinolines, Norsalsolinol ethers, All stub articles, Antihypertensive agent stubs, Genito-urinary system drug ... 1-adrenoceptor antagonist activity of the anti-arrhythmic drug, abanoquil (UK-52,046), without reduction in blood pressure in ...
https://en.wikipedia.org/wiki/Abanoquil
Alpha-1B adrenergic receptorAlpha-1B adrenergic receptor
Antagonists L-765,314 Risperidone Brexpiprazole Alpha-1B adrenergic receptor has been shown to interact with AP2M1. A role in ... 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- ...
https://en.wikipedia.org/wiki/Alpha-1B_adrenergic_receptor
Uveitis-glaucoma-hyphema syndromeUveitis-glaucoma-hyphema syndrome
... beta-adrenergic antagonists, alpha-adrenergic agonists, and carbonic anhydrase inhibitors etc. The UGH Syndrome was originally ...
https://en.wikipedia.org/wiki/Uveitis–glaucoma–hyphema_syndrome
Alpha-1 adrenergic receptorAlpha-1 adrenergic receptor
... 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 ... "Renal alpha-1 and alpha-2 adrenergic receptors: biochemical and pharmacological correlations". The Journal of Pharmacology and ... alpha-1 (α1) adrenergic receptors are G protein-coupled receptors (GPCRs) associated with the Gq heterotrimeric G protein. α1- ...
https://en.wikipedia.org/wiki/Alpha-1_adrenergic_receptor
Neurogenic bladder dysfunctionNeurogenic bladder dysfunction
... alpha-adrenergic agonist, alpha 1 antagonists). Urinary symptoms may include frequency, urgency, incontinence or recurrent ... Alpha blockers can also reduce outlet resistance and allow complete emptying if there is adequate bladder muscle function. ...
https://en.wikipedia.org/wiki/Neurogenic_bladder_dysfunction
NaftopidilNaftopidil
... is a drug used in benign prostatic hypertrophy which acts as a selective α1-adrenergic receptor antagonist or alpha-1 blocker. ... Alpha-1 blockers, Antihypertensive agents, Calcium channel blockers, N-(2-methoxyphenyl)piperazines, Naphthol ethers, ...
https://en.wikipedia.org/wiki/Naftopidil
Transurethral needle ablation of the prostateTransurethral needle ablation of the prostate
... needle ablation of the prostate as an alternative to transurethral resection of the prostate when alpha-adrenergic antagonist ...
https://en.wikipedia.org/wiki/Transurethral_needle_ablation_of_the_prostate
CannabigerolCannabigerol
5-HT1A antagonists, Alpha-2 adrenergic receptor agonists, Phytocannabinoids, CB1 receptor antagonists, Resorcinols, Terpeno- ... It appears to be unique among cannabinoid compounds by also having high affinity and activity at alpha-2 adrenergic receptors ... the potent activity of cannabigerol at alpha-2 adrenergic receptors raises concerns about its safety for human consumption, ... plant cannabinoid cannabigerol is a highly potent alpha2-adrenoceptor agonist and moderately potent 5HT1A receptor antagonist ...
https://en.wikipedia.org/wiki/Cannabigerol
C17H19N3OC17H19N3O
... a reversible nonselective Alpha-adrenergic antagonist Piberaline, a psychoactive drug This set index page lists chemical ...
https://en.wikipedia.org/wiki/C17H19N3O
Azinphos-methylAzinphos-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) ...
https://en.wikipedia.org/wiki/Azinphos-methyl
ProstateProstate
In general, treatment often begins with an alpha-1 adrenergic receptor antagonist medication such as tamsulosin, which reduces ... or male chronic pelvic pain syndrome is treated by a large variety of modalities including the medications alpha blockers, ...
https://en.wikipedia.org/wiki/Prostate
Drug classDrug class
5-Alpha-reductase inhibitor Angiotensin II receptor antagonist ACE inhibitor Alpha-adrenergic agonist Beta blocker Cholinergic ... For receptors, these activities include agonist, antagonist, inverse agonist, or modulator. Enzyme target mechanisms include ...
https://en.wikipedia.org/wiki/Drug_class
AripiprazoleAripiprazole
There are no studies to date confirming if aripiprazole function as an agonist or antagonist at alpha-adrenergic receptors such ... 5-HT2B antagonists, 5-HT2C agonists, 5-HT7 antagonists, 7-(4-(4-Phenylpiperazin-1-yl)butoxy)-1H-quinolin-2-ones, Alpha-1 ... D2 antagonists, D2-receptor agonists, D3 antagonists, D3 receptor agonists, H1 receptor antagonists, Mood stabilizers, Otsuka ... but the orthostatic hypotension observed with aripiprazole may be explained by its antagonist activity at adrenergic α1A ...
https://en.wikipedia.org/wiki/Aripiprazole
BenzoctamineBenzoctamine
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 ... Alpha blockers, Anxiolytics, Sedatives, Serotonin receptor antagonists, Tetracyclic antidepressants). ...
https://en.wikipedia.org/wiki/Benzoctamine
Harris IsbellHarris Isbell
1959b) reported that pre-treatment with scopolamine (an acetylcholine antagonist), phenoxybenzamine (an adrenergic alpha ... Clinical Aspects of Opiate Antagonists and Partial Agonists. pp 118-124 in Martin and Isbell(1978). Fraser HF, Wikler A, ... and correlated these effects with their potency as a serotonin antagonist in smooth muscle. With the exception of "ALD-52", all ... the clinical use of opiate antagonists (e.g., nalorphine/Nalline and naloxone/Narcan) as treatment for opiate overdoses, the ...
https://en.wikipedia.org/wiki/Harris_Isbell
BenperidolBenperidol
... it has antihistaminergic and alpha-adrenergic properties. It possesses minimal anticholinergic properties. Benperidol is ... Benperidol is a strong dopamine receptor antagonist (D2 (Ki 0.027 nM) and D4 (Ki 0.066 nM)) with weaker serotonin receptor ...
https://en.wikipedia.org/wiki/Benperidol
DoxepinDoxepin
Alpha-1 blockers, Alpha-2 blockers, Antihistamines, D2 antagonists, Dibenzoxepins, Dimethylamino compounds, Embryotoxicants, ... α1-adrenergic receptor, 5-HT2A and muscarinic acetylcholine receptors Moderate: 5-HT2C and 5-HT1A receptors Weak: α2-adrenergic ... Hypnotics, Muscarinic antagonists, Sedatives, Serotonin receptor antagonists, Serotonin-norepinephrine reuptake inhibitors, ... In fact, doxepin has been said to be the most or one of the most potent H1 receptor antagonists available, with one study ...
https://en.wikipedia.org/wiki/Doxepin
Index of biochemistry articlesIndex of biochemistry articles
... alpha adrenergic receptor - alpha helix - alpha-1 adrenergic receptor - alpha-2 adrenergic receptor - alpha-beta T-cell antigen ... receptor antagonist - receptor protein-tyrosine kinase - recombinant fusion protein - recombinant interferon-gamma - ... receptor - alpha-fetoprotein - alpha-globulin - alpha-macroglobulin - alpha-MSH - Ames test - amide - amine - amino - amino ... beta adrenergic receptor - beta sheet - beta-1 adrenergic receptor - beta-2 adrenergic receptor - beta-thromboglobulin - ...
https://en.wikipedia.org/wiki/Index_of_biochemistry_articles
PheochromocytomaPheochromocytoma
Just as with the alpha antagonists, there are selective (beta-1) and non-selective (beta-1 and beta-2) adrenoceptor antagonists ... van Brummelen P, Jie K, van Zwieten PA (1986). "Alpha-adrenergic receptors in human blood vessels". British Journal of Clinical ... may follow after initiating an alpha-adrenoceptor antagonist. If that is the case, a beta-adrenoceptor antagonist is then ... This complication is related to the impact that alpha and beta-adrenoceptor antagonists have on blood vessels combined with the ...
https://en.wikipedia.org/wiki/Pheochromocytoma
GlaucomaGlaucoma
Topical beta-adrenergic receptor antagonists, such as timolol, levobunolol, and betaxolol, decrease aqueous humor production by ... Less-selective alpha agonists, such as epinephrine, decrease aqueous humor production through vasoconstriction of ciliary body ... Alpha2-adrenergic agonists, such as brimonidine and apraclonidine, work by a dual mechanism, decreasing aqueous humor ... Alpha 2 agonists (brimonidine, apraclonidine) both decrease fluid production (via inhibition of AC) and increase drainage. ...
https://en.wikipedia.org/wiki/Glaucoma
HydroxyzineHydroxyzine
5-HT2A antagonists, Primary alcohols, Alpha-1 blockers, Antiemetics, Anxiolytics, Belgian inventions, D2 antagonists, Ethers, ... and the α1-adrenergic receptor. The weak antiserotonergic effects of hydroxyzine likely underlie its usefulness as an ... H1 receptor antagonists, Chlorcyclizines, Sedatives, Serotonin receptor antagonists, Wikipedia medicine articles ready to ... In addition to its antihistamine activity, hydroxyzine has also been shown to act more weakly as an antagonist of the serotonin ...
https://en.wikipedia.org/wiki/Hydroxyzine
ACTH receptorACTH receptor
MCR's have both endogenous agonists and antagonists. α-MSH and ACTH are both peptides derived from processed POMC, and both ... rabbits respond to alpha and beta MSH's (therefore not using the ACTH receptor), and guinea pigs responding to both ACTH and ... while the ACTH receptor and the β2 adrenergic receptor are relatively distantly-related with a sequence identity of ... Agouti-related protein and Agouti-signaling protein are antagonist peptides to MC2R. ACTH receptor is primarily found in the ...
https://en.wikipedia.org/wiki/ACTH_receptor
NiaprazineNiaprazine
... and was instead found to act as a potent and selective 5-HT2A and α1-adrenergic receptor antagonist (Ki = 75 nM and 86 nM, ... Alpha-1 blockers, Alpha-2 blockers, Fluoroarenes, Hypnotics, Nicotinamides, Phenylpiperazines, Sedatives). ... respectively). It possesses low or no affinity for the 5-HT1A, 5-HT2B, D2, and β-adrenergic, as well as at SERT and VMAT (Ki = ... all > 1 μM), but it does have some affinity for the α2-adrenergic receptor (Ki = 730 nM). Niaprazine has been shown to ...
https://en.wikipedia.org/wiki/Niaprazine
FenoldopamFenoldopam
... although there is evidence that it may have some alpha-1 and alpha-2 adrenoceptor antagonist activity. D1 receptor stimulation ... Since fenoldopam is an intravenous agent with minimal adrenergic effects that improves renal perfusion, in theory it could be ... Martin SW, Broadley KJ (May 1995). "Renal vasodilatation by dopexamine and fenoldopam due to alpha 1-adrenoceptor blockade". Br ...
https://en.wikipedia.org/wiki/Fenoldopam
YohimbineYohimbine
February 2000). "Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, ... It behaves as an antagonist at α1-adrenergic, α2-adrenergic, 5-HT1B, 5-HT1D, 5-HT2A, 5-HT2B, and dopamine D2, and as a partial ... Yohimbine is an α2-adrenergic receptor antagonist, and has been used in a variety of research projects. It is a veterinary drug ... Saenz de Tejada I, Kim NN, Goldstein I, Traish AM (March 2000). "Regulation of pre-synaptic alpha adrenergic activity in the ...
https://en.wikipedia.org/wiki/Yohimbine
MIN-117MIN-117
5-HT1A antagonists, 5-HT2A antagonists, Antidepressants, Benzofuran ethers at the benzene ring, Serotonin-dopamine reuptake ... Dion D (2014). "Some Nerves Surrounding Minerva Neurosciences IPO". Seeking Alpha. Retrieved 2015-05-19. "Minerva Neurosciences ... and α1B-adrenergic receptors. As of May 2015, MIN-117 is in phase II clinical trials for MDD. In December 2019, Minerva ... It is described as a 5-HT1A and 5-HT2A receptor antagonist and inhibitor of serotonin and dopamine reuptake, and is also ...
https://en.wikipedia.org/wiki/MIN-117
RotigotineRotigotine
... as an antagonist at the α2B-adrenergic receptor, and as a partial agonist at the 5-HT1A receptor. Though it has affinity for a ... Adrenergic receptor modulators, Alpha-2 blockers, Aminotetralins, D1-receptor agonists, D2-receptor agonists, D3 receptor ... α1B-adrenergic receptor (Ki = 273 nM) α2A-adrenergic receptor (Ki = 338 nM) α2B-adrenergic receptor (Ki = 27 nM) α2C-adrenergic ... with its α2B-adrenergic and 5-HT1A activity also possibly having some minor relevance. Piribedil Pramipexole Ropinirole Chen JJ ...
https://en.wikipedia.org/wiki/Rotigotine
NantenineNantenine
It is an antagonist of both the α1-adrenergic receptor and the serotonin 5-HT2A receptor, and blocks both the behavioral and ... 5-HT2A antagonists, Alpha-1 blockers, Antidotes, Aporphine alkaloids, Phenol ethers, All stub articles, Nervous system drug ... Chaudhary S, Pecic S, Legendre O, Navarro HA, Harding WW (May 2009). "(+/-)-Nantenine analogs as antagonists at human 5-HT(2A) ... an antagonist of the behavioral and physiological effects of MDMA in mice". Psychopharmacology. 173 (3-4): 270-7. doi:10.1007/ ...
https://en.wikipedia.org/wiki/Nantenine
CorynanthineCorynanthine
... acts as an α1-adrenergic and α2-adrenergic receptor antagonist with approximately 10-fold selectivity for the ... Doxey JC, Lane AC, Roach AG, Virdee NK (February 1984). "Comparison of the alpha-adrenoceptor antagonist profiles of idazoxan ( ... Dual effects of yohimbine, rauwolscine and corynanthine as alpha-adrenoceptor antagonists and 5-HT-receptor agonists". Naunyn- ... Alpha-1 blockers, Alpha-2 blockers, Antihypertensive agents, Tryptamine alkaloids, Indoloquinolizines, Quinolizidine alkaloids) ...
https://en.wikipedia.org/wiki/Corynanthine
AgmatineAgmatine
Nicotinic, imidazoline I1 and I2, α2-adrenergic (no intrinsic activity-neither agonist nor antagonist), glutamate NMDAr, and ... "Agmatine recognizes alpha 2-adrenoceptor binding sites but neither activates nor inhibits alpha 2-adrenoceptors". Naunyn- ... Pineda, J.; Ruiz-Ortega, J. A.; Martín-Ruiz, R.; Ugedo, L. (1996-11-22). "Agmatine does not have activity at alpha 2- ... Agmatine binds to α2-adrenergic receptor and imidazoline receptor binding sites, and blocks NMDA receptors and other cation ...
https://en.wikipedia.org/wiki/Agmatine
PhenoxybenzaminePhenoxybenzamine
Clinically, non-selective alpha antagonists block alpha receptors (but do not differentiate between alpha-1 and alpha-2). They ... Phenoxybenzamine forms a permanent covalent bond with adrenergic receptors. Based on known information about the structures of ... As a non-selective alpha receptor antagonist, it will also affect both the postsynaptic alpha 1 and presynaptic alpha 2 ... 5-HT2A antagonists, Alkylating agents, Alpha-1 blockers, Alpha-2 blockers, IARC Group 2B carcinogens, Irreversible antagonists ...
https://en.wikipedia.org/wiki/Phenoxybenzamine
DosulepinDosulepin
It is also an antagonist of the histamine H1 receptor, α1-adrenergic receptor, serotonin 5-HT2 receptors, and muscarinic ... Alpha-1 blockers, Dimethylamino compounds, Analgesics, Antihistamines, Dibenzothiepines, Muscarinic antagonists, Serotonin ... Guanethidine and other adrenergic neuron blocking drugs can have their antihypertensive effects blocked by dosulepin. ... reported relatively high Ki values of 12 and 15 nM for dosulepin and northiaden at the rat α2-adrenergic receptor and suggested ...
https://en.wikipedia.org/wiki/Dosulepin
List of skin conditionsList of skin conditions
Acquired generalized lipodystrophy (Lawrence syndrome, Lawrence-Seip syndrome) Adiposis dolorosa (Dercum's disease) Alpha-1 ... Acquired C1 esterase inhibitor deficiency Acute urticaria Adrenergic urticaria Anaphylaxis Aquagenic urticaria Cholinergic ... HIV disease-related drug reaction Hydroxyurea dermopathy Injection site reaction Iododerma Leukotriene receptor antagonist- ... alpha-N-acetylgalactosaminidase deficiency) Schinzel-Giedion syndrome Scleroatrophic syndrome of Huriez (Huriez syndrome, ...
https://en.wikipedia.org/wiki/List_of_skin_conditions
AptazapineAptazapine
It is a potent α2-adrenergic receptor antagonist with ~10x the strength of the related compound mianserin and has also been ... January 1983). "CGS 7525A, a new, centrally active alpha 2 adrenoceptor antagonist". Life Sciences. 32 (4): 355-63. doi:10.1016 ... Alpha-2 blockers, H1 receptor antagonists, Noradrenergic and specific serotonergic antidepressants, Serotonin receptor ... "Pharmacological evaluation of in vivo tests for alpha 2-adrenoceptor blockade in the central nervous system and the effects of ...
https://en.wikipedia.org/wiki/Aptazapine
FexofenadineFexofenadine
... also exhibits no anticholinergic, antidopaminergic, alpha 1-adrenergic, or beta-adrenergic receptor-blocking ... Fexofenadine is a selective peripheral H1 receptor antagonist. Blockage prevents the activation of the H1 receptors by ... H1 receptor antagonists, Peripherally selective drugs, Piperidines, Sanofi, World Health Organization essential medicines). ...
https://en.wikipedia.org/wiki/Fexofenadine
Beta (disambiguation)Beta (disambiguation)
... adrenergic receptors Beta, a rank in a community of social animals; See Alpha Beta carbon, in organic chemistry-the second ... an antagonist in the Walking Dead comic series Beta Hirogen, the second in command of a Hirogen hunting party, as seen in Star ... carbon atom in a chain when counting from a functional group; See Alpha and beta carbon Beta cell, a type of cell in the ...
https://en.wikipedia.org/wiki/Beta_(disambiguation)
Alpha-adrenergic agonistAlpha-adrenergic agonist
Cirazoline is an α1 adrenergic agonist and an α2 adrenergic antagonist". Journal of Pharmacology and Experimental Therapeutics ... Alpha-adrenergic agonists have the opposite function of alpha blockers. Alpha adrenoreceptor ligands mimic the action of ... Alpha-adrenergic agonists are a class of sympathomimetic agents that selectively stimulates alpha adrenergic receptors. The ... Medetomidine, an α2 adrenergic agonist. Nonspecific agonists act as agonists at both alpha-1 and alpha-2 receptors. ...
https://en.wikipedia.org/wiki/Alpha-adrenergic_agonist
Noradrenergic and specific serotonergic antidepressantNoradrenergic and specific serotonergic antidepressant
Alpha-2 blockers, Noradrenergic and specific serotonergic antidepressants, Serotonin receptor antagonists). ... By blocking α2-adrenergic autoreceptors and heteroreceptors, NaSSAs enhance adrenergic and serotonergic neurotransmission in ... They act by antagonizing the α2-adrenergic receptor and certain serotonin receptors such as 5-HT2A and 5-HT2C, but also 5-HT3, ... Serotonin antagonist and reuptake inhibitor (SARI) Serotonin modulator and stimulator (SMS) Norepinephrine-dopamine ...
https://en.wikipedia.org/wiki/Noradrenergic_and_specific_serotonergic_antidepressant
IprindoleIprindole
5-HT2 antagonists, Abandoned drugs, Nitrogen heterocycles, Drugs with unknown mechanisms of action, H1 receptor antagonists, ... Iprindole also lacks significant alpha-blocking properties, and hence does not pose a risk of orthostatic hypotension. In ... Bylund DB, Snyder SH (1976). "Beta adrenergic receptor binding in membrane preparations from mammalian brain". Mol. Pharmacol. ... It is presumed to act as an inhibitor or antagonist/inverse agonist of all sites. Considering the range of its therapeutic ...
https://en.wikipedia.org/wiki/Iprindole
Primary polydipsiaPrimary polydipsia
... an alpha-2 adrenergic agonist Irbesartan, an angiotensin II receptor antagonist Propranolol, a sympatholytic beta blocker ... Such medications include antipsychotics, antidepressants, anticonvulsants, alpha agonists and anticholinergics. It should also ... a carbonic anhydrase inhibitor Lithium was previously used for treatment of PPD as a direct competitive ADH antagonist, but is ... Vasopressin receptor antagonists, such as conivaptan Acetazolamide, ...
https://en.wikipedia.org/wiki/Primary_polydipsia
NiguldipineNiguldipine
... is a calcium channel blocker and α1-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 ... Alpha-1 blockers, Calcium channel blockers, Carboxylate esters, Dihydropyridines, Nitrobenzenes, All stub articles, ...
https://en.wikipedia.org/wiki/Niguldipine
Posttraumatic Stress Disorder Medication: Selective serotonin reuptake inhibitors, Beta-blockers, Alpha-1 Receptor Antagonists,...Posttraumatic Stress Disorder Medication: Selective serotonin reuptake inhibitors, Beta-blockers, Alpha-1 Receptor Antagonists,...
Alpha-2 Adrenergic Agonists. Class Summary. Agents in this class may decrease vasomotor tone and heart rate by stimulating ... Alpha-1 Receptor Antagonists. Class Summary. Novel pilot studies in combat veterans suggest alpha-1 antagonists have efficacy ... Prazosin is an alpha-1 adrenergic blocker that is indicated for hypertension. Studies indicate that a nighttime dose of ... Clonidine is a central alpha-adrenergic agonist that is commonly used as an antihypertensive agent. It stimulates alpha2- ...
https://www.medscape.com/answers/288154-99043/which-medications-in-the-drug-class-selective-serotonin-reuptake-inhibitors-are-used-in-the-treatment-of-posttraumatic-stress-disorder
Pediatric Congestive Heart Failure Medication: Diuretics, Loop, Diuretics, Thiazide, Diuretics, Other, Aldosterone Antagonists,...Pediatric Congestive Heart Failure Medication: Diuretics, Loop, Diuretics, Thiazide, Diuretics, Other, Aldosterone Antagonists,...
Carvedilol blocks beta1-, alpha-, and beta2-adrenergic receptor sites, decreasing adrenergic-mediated myocyte damage. ... Alpha/Beta Adrenergic Agonists. Class Summary. These agents may be required for repletion of catecholamines and for the ... In high doses (15-20 ug/kg/min), it acts on alpha-adrenergic receptors to increase systemic vascular resistance and raise blood ... Sympathomimetic amines with both alpha- and beta-adrenergic effects are indicated in cardiogenic shock. Dopamine and dobutamine ...
https://emedicine.medscape.com/article/2069746-medication
KEGG PATHWAY: alpha-Adrenergic receptor agonists/antagonists - Reference pathwayKEGG PATHWAY: alpha-Adrenergic receptor agonists/antagonists - Reference pathway
alpha-Adrenergic receptor agonists/antagonists - Reference pathway [ Pathway menu , Pathway entry , Image file , Help ] ...
https://www.kegg.jp/pathway/map07215+D08662
Different affinity states of alpha-1 adrenergic receptors defined by agonists and antagonists in bovine aorta plasma membranes....Different affinity states of alpha-1 adrenergic receptors defined by agonists and antagonists in bovine aorta plasma membranes....
Different affinity states of alpha-1 adrenergic receptors defined by agonists and antagonists in bovine aorta plasma membranes. ... Different affinity states of alpha-1 adrenergic receptors defined by agonists and antagonists in bovine aorta plasma membranes. ... Different affinity states of alpha-1 adrenergic receptors defined by agonists and antagonists in bovine aorta plasma membranes. ... Different affinity states of alpha-1 adrenergic receptors defined by agonists and antagonists in bovine aorta plasma membranes. ...
https://jpet.aspetjournals.org/content/243/2/430
Adrenergic antagonists: Alpha blockers | OsmosisAdrenergic antagonists: Alpha blockers | Osmosis
Learn and reinforce your understanding of Adrenergic antagonists: Alpha blockers. ... Alpha blockers Videos, Flashcards, High Yield Notes, & Practice Questions. ... Lets focus on alpha receptors, which have two subtypes: alpha-1 and alpha-2. alpha-1 adrenergic receptors are mainly located ... non-selective alpha blockers and selective alpha blockers. Non-selective alpha blockers work on both alpha-1 and alpha-2 ...
https://www.osmosis.org/learn/Adrenergic_antagonists:_Alpha_blockers?from=/md/clerkships/emergency-medicine/medical-and-surgical-emergencies/dermatology-and-plastic-surgery
Modeling the interactions between alpha(1)-adrenergic receptors and their antagonists. | DrugBank OnlineModeling the interactions between alpha(1)-adrenergic receptors and their antagonists. | DrugBank Online
Modeling the interactions between alpha(1)-adrenergic receptors and their antagonists. ... So far three distinct alpha(1)-AR subtypes, alpha(1A), alpha(1B) and alpha(1D), have been characterized by functional analysis ... Modeling the interactions between alpha(1)-adrenergic receptors and their antagonists.. Curr Comput Aided Drug Des. 2010 Sep;6( ... As crucial members of the G-protein coupled receptor (GPCR) superfamily, alpha (1)-adrenergic receptors (alpha(1)-ARs) are ...
https://go.drugbank.com/articles/A5379
Angioedema Medication: Alpha/Beta-Adrenergic Agonists, Antihistamines, 1st-Generation, Antihistamines, 2nd Generation,...
However, the combination of an H1 antagonist with an H2 antagonist has been shown to be more effective than an H1 antagonist ... Alpha/Beta-Adrenergic Agonists. Class Summary. Adrenergic agonist agents cause vasoconstriction and bronchodilation and reduce ... Leukotriene Receptor Antagonists. Class Summary. Leukotriene receptor antagonists may be used as add-on therapy for histamine- ... Effect of the H2-antagonist cimetidine on the pharmacokinetics and pharmacodynamics of the H1-antagonists hydroxyzine and ...
https://www.staging.medscape.com/answers/135208-60646/which-medications-in-the-drug-class-histamine-h2-antagonists-are-used-in-the-treatment-of-angioedema
Case report: nifedipine-rifampicin interaction attenuates the effect on blood pressure in a patient with essential hypertensionCase report: nifedipine-rifampicin interaction attenuates the effect on blood pressure in a patient with essential hypertension
Adrenergic alpha-Antagonists / therapeutic use * Aged * Blood Pressure / drug effects* * Drug Interactions ... Nisoldipine, another calcium antagonist, also failed to lower the patients blood pressure, when given in combination with ... Taken together, these findings indicate that more caution should be urged when calcium antagonist is prescribed along with ...
https://pubmed.ncbi.nlm.nih.gov/1345893/?dopt=Abstract
Carvedilol in Preventing Heart Failure in Childhood Cancer Survivors - Full Text View - ClinicalTrials.govCarvedilol in Preventing Heart Failure in Childhood Cancer Survivors - Full Text View - ClinicalTrials.gov
Adrenergic beta-Antagonists. Adrenergic Antagonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... History of drug sensitivity or allergic reaction to alpha or beta-blockers ... Use of an investigational drug or beta adrenergic blockers, including metoprolol, sotalol, within 30 days of enrollment ...
https://clinicaltrials.gov/show/NCT02717507
Safety and Efficacy of Nyxol (0.75% Phentolamine Ophthalmic Solution) to Reverse Pharmacologically-Induced Mydriasis - Full...Safety and Efficacy of Nyxol (0.75% Phentolamine Ophthalmic Solution) to Reverse Pharmacologically-Induced Mydriasis - Full...
Adrenergic alpha-Antagonists. Adrenergic Antagonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... 0.75% phentolamine ophthalmic solution (Nyxol), a non-selective alpha-1 and alpha-2 adrenergic antagonist ... Initiation of treatment with or any changes to the current dosage, drug or regimen of any systemic adrenergic or cholinergic ... Known hypersensitivity or contraindication to α- and/or β adrenoceptor antagonists.. *Clinically significant systemic disease ...
https://www.clinicaltrials.gov/ct2/show/NCT04620213?term=ocuphire&draw=2
Limitation of coronary reserve after successful angioplasty is prevented by oral pretreatment with an alpha(1)-adrenergic...
... adrenergic antagonist. Rimoldi O;Spyrou N;Foale R;Hackett DR;Gregorini L;CAMICI , PAOLO 2000. Abstract. Coronary ... To ascertain whether pretreatment with the or, adrenergic receptor blocker doxazosin could prevent the limitation of CVR after ... To ascertain whether pretreatment with the or, adrenergic receptor blocker doxazosin could prevent the limitation of CVR after ... Limitation of coronary reserve after successful angioplasty is prevented by oral pretreatment with an alpha(1)- ...
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Phentolamine Mesylate(Phentolamine methanesulfonate) is a reversible and nonselective alpha-adrenergic receptor antagonist, ... Other Adrenergic Receptor Products. * SB225002New. SB225002 is a potent, and selective CXCR2 antagonist with IC50 of 22 nM for ... Adrenergic Receptor antagonist Nebivolol hydrochloride (R-65824) Nebivolol hydrochloride (R-65824). Catalog No.S1549 Synonyms: ... Propranolol HCl (AY-64043, ICI-45520, NCS-91523) is a competitive non-selective beta-adrenergic receptors inhibitor with IC50 ...
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CARDURA is an alpha1 adrenergic antagonist indicated for: (1). *Signs and symptoms of Benign Prostatic Hyperplasia (BPH) ... CARDURA® (doxazosin) is a quinazoline compound that is a selective inhibitor of the alpha1 subtype of alpha-adrenergic ... Like other alpha1-adrenergic blocking agents, doxazosin has a greater effect on blood pressure and heart rate in the standing ... The mechanism of action of CARDURA is selective blockade of the alpha1 (postjunctional) subtype of adrenergic receptors. ...
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Millan et al., 2000, Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR ... ALPHA-2B ADRENERGIC RECEPTOR (ALPHA-2B ADRENOCEPTOR) (ALPHA-2B ADRENORECEPTOR) (SUBTYPE C2). [SOURCE:UNIPROT/SWISSPROT;ACC: ... ALPHA-2B ADRENERGIC RECEPTOR (ALPHA-2B ADRENOCEPTOR) (ALPHA-2B ADRENORECEPTOR) (SUBTYPE C2). [SOURCE:UNIPROT/SWISSPROT;ACC: ... Nash, 1990, Alpha-adrenergic blockers: mechanism of action, blood pressure control, and effects of lipoprotein metabolism., ...
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Pediatric Headache Medication: Analgesics, Other, Sedative/Hypnotics, Serotonin 5-HT-Receptor Agonists, Antiemetic Agents, Beta...Pediatric Headache Medication: Analgesics, Other, Sedative/Hypnotics, Serotonin 5-HT-Receptor Agonists, Antiemetic Agents, Beta...
Ergotamine is an alpha-adrenergic and serotonin (5-HT1) antagonist and partial agonist (depending on the receptor site). It ...
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Combination therapy with an alpha adrenergic antagonist plus a 5 alpha reductase inhibitor produces what? ... How do Alpha 1 adrenergic antagonists work in the treatment of BPH? ... receptor antagonists: flutamide. ---5 alpha reductase inhibitor: Finasteride ---Synthesis inhibitors: ketoconazole. --GnRH ... Testosterone via 5 alpha reductase gets converted to Dihydroxy Testosterone, what are the effects of testosterone and DHT? ...
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Iris morphologic changes related to alpha(1)-adrenergic receptor antagonists implications for intraoperative floppy iris ... Iris morphologic changes related to alpha(1)-adrenergic receptor antagonists implications for intraoperative floppy iris ... CrossRef Issa SA, Hadid OH, Baylis O, Dayan M. Alpha antagonists and intraoperative floppy iris syndrome: a spectrum. Clin ... Zurück zum Zitat Handzel DM, Briesen S, Rausch S, Kälble T. Cataract surgery in patients taking alpha‑1 antagonists: know the ...
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... an alpha-adrenergic antagonist (1 microM), reduced sympathetic constriction in controls, but abolished this response in TiO2 ... The enhanced sensitivity to alpha-adrenergic receptor blockade following TiO2 exposure suggests an augmented responsiveness to ... Nanoparticle inhalation modulates arteriolar sympathetic constriction: role of nitric oxide, prostanoids, and alpha-adrenergic ...
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In terms of pharmacotherapy, the main option available is prazosin, an alpha-adrenergic antagonist that is FDA-approved as a ...
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https://www.verywellhealth.com/rapaflo-silodosin-oral-5248563
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... alpha adrenergic receptor antagonists (alpha blockers), calcium channel blockers (CCBs) etc. are not efficient enough to cure ... Use of diuretics, angiotensin converting enzyme (ACE) inhibitors, beta adrenergic receptor antagonists (beta blockers), ... beta adrenergic receptor antagonists (beta blockers), alpha adrenergic receptor antagonists (alpha blockers), calcium channel ...
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ChemIDplus - 160970-54-7 - PNCPYILNMDWPEY-QGZVFWFLSA-N - Silodosin [INN:BAN] - Similar structures search, synonyms, formulas,...
Adrenergic Agents. *. Adrenergic alpha-1 Receptor Antagonists. *. Adrenergic alpha-Antagonists. *. Adrenergic Antagonists ...
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What do alpha-blockers do to the heart?What do alpha-blockers do to the heart?
Alpha blockers, such as prazosin, are medications that work as alpha-adrenergic receptor antagonists. They cross the blood- ... How do alpha-blockers work for PTSD?. Al- pha blockers are only part of the therapy for PTSD. They act to help improve sleep ... Do alpha-blockers make you tired?. Side effects: Since alpha blockers affect your blood pressure, they can make you feel very ... Beta blockers may be cardioprotective but in contrast to alpha-1 antagonists tend to have adverse effects on plasma lipids. ...
https://www.digglicious.com/uncategorized/what-do-alpha-blockers-do-to-the-heart/
blood pressure drug Archives | Surviving Mesotheliomablood pressure drug Archives | Surviving Mesothelioma
It is marketed in the U.S. under the brand name Flivas and is known as an alpha blocker or an alpha-adrenergic antagonist. In ...
https://survivingmesothelioma.com/tag/blood-pressure-drug/
ReceptorsInhibitorsSelectiveAgonistAgonists and antagonistsBlockersPhentolaminePropranololTamsulosinDopaminePrazosinMedicationsTherapeuticAlpha2YohimbineReceptor blockerConstrictionAffinityNeuronsMedicationTestosteronePhenoxybenzamineSubtypesExposureEffectsWithdrawalProductsEvidenceBlood pressureDrugs
Receptors30
  • Dopamine is a naturally occurring endogenous catecholamine that stimulates beta1- and alpha1-adrenergic and dopaminergic receptors in a dose-dependent fashion. (medscape.com)
  • In midrange doses (5-15 ug/kg/min), it acts on beta-adrenergic receptors to increase heart rate and contractility. (medscape.com)
  • In high doses (15-20 ug/kg/min), it acts on alpha-adrenergic receptors to increase systemic vascular resistance and raise blood pressure. (medscape.com)
  • Different affinity states of alpha-1 adrenergic receptors defined by agonists and antagonists in bovine aorta plasma membranes. (aspetjournals.org)
  • Evidence for a nonlinear relationship between alpha-1 adrenergic receptor occupancy and tissue responses, together with the finding of different affinity states for agonist binding, has raised the possibility of functional heterogeneity of alpha-1 adrenergic receptors. (aspetjournals.org)
  • Alpha blocker and beta blockers are two types of postsynaptic anti-adrenergic medications that prevent their respective receptors from being stimulated by catecholamines, like norepinephrine and epinephrine . (osmosis.org)
  • These two catecholamines activate the adrenergic receptors on the many different organs, which allow the sympathetic nervous system to trigger the fight or flight response that increases the heart rate and blood pressure , as well as slowing digestion. (osmosis.org)
  • the alpha receptors, and beta receptors . (osmosis.org)
  • Let's focus on alpha receptors, which have two subtypes: alpha-1 and alpha-2. (osmosis.org)
  • alpha-1 adrenergic receptors are mainly located on the walls of blood vessels, and when stimulated, they cause vasoconstriction , thus decreasing blood flow to tissues. (osmosis.org)
  • In the eyes, alpha-1 adrenergic receptors also trigger mydriasis , or pupil dilation . (osmosis.org)
  • Now, alpha-2 adrenergic receptors are primarily found on the presynaptic neuron. (osmosis.org)
  • So when a presynaptic nerve ending is stimulated to release noradrenaline in the synaptic cleft, some of that norepinephrine turns around and binds to alpha-2 receptors on the presynaptic membrane. (osmosis.org)
  • And based on the type of receptors they block, they are divided into two main categories - alpha blockers, and beta blockers. (osmosis.org)
  • Non-selective alpha blockers work on both alpha-1 and alpha-2 adrenergic receptors and include phenoxybenzamine and phentolamine . (osmosis.org)
  • By blocking alpha-1 receptors , they cause vasodilation and lower blood pressure . (osmosis.org)
  • In fact, the only way out is to synthesize new adrenergic receptors , which takes about 24 hours. (osmosis.org)
  • Modeling the interactions between alpha(1)-adrenergic receptors and their antagonists. (drugbank.com)
  • As crucial members of the G-protein coupled receptor (GPCR) superfamily, alpha (1)-adrenergic receptors (alpha(1)-ARs) are recognized to intervene the actions of endogenous catecholamines such as norepinephrine and epinephrine. (drugbank.com)
  • Propranolol HCl (AY-64043, ICI-45520, NCS-91523) is a competitive non-selective beta-adrenergic receptors inhibitor with IC50 of 12 nM. (selleckchem.com)
  • It works by attaching to the alpha-1 adrenergic receptors (binding sites). (verywellhealth.com)
  • They cross the blood-brain barrier, antagonise the alpha receptors in the central nervous system, and block the stress response. (digglicious.com)
  • What happens when alpha 2 receptors are blocked? (digglicious.com)
  • They act by blocking alpha-1 receptors in the brain which is thought to lead to better, deeper sleep. (digglicious.com)
  • Nanoparticle inhalation modulates arteriolar sympathetic constriction: role of nitric oxide, prostanoids, and alpha-adrenergic receptors. (cdc.gov)
  • This review synthesizes the current literature about the behavioral, electrophysiological and neurochemical effects of 5-HT2 receptors ligands on the monoaminergic systems but also on adult hippocampal neurogenesis to shed some light on the preclinical evidence supporting the use of 5 -HT2A and/or 5- HT2C receptor antagonists such as antipsychotics, as potential effective adjuncts in SSRIs-resistant depression. (semanticscholar.org)
  • By blocking the alpha2 receptor with Yohimbine, the negative feedback caused by NE binding to the alpha receptors is reduced and fatty acid liberation is increased. (helpyougetgains.com)
  • Coronary responses to adrenergic stimuli were determined in the intact beating heart before and after administration of practolol, 4-(2-hydroxy-3-isopropylaminoproproxy) acetanilide, which in low doses blocks myocardial but not vascular beta receptors. (jci.org)
  • The direct effect of these two stimuli on coronary vessels is minimal and is mediated through stimulation of alpha (vasoconstrictor) receptors. (jci.org)
  • The excitatory effects of the alpha-2 receptor antagonist piperoxane provided evidence that these receptors are of functional significance in vivo. (duke.edu)
Inhibitors3
  • Use of diuretics, angiotensin converting enzyme (ACE) inhibitors, beta adrenergic receptor antagonists (beta blockers), alpha adrenergic receptor antagonists (alpha blockers), calcium channel blockers (CCBs) etc. are not efficient enough to cure hypertension. (scirp.org)
  • Others include monoamine oxidase (MAO) inhibitors, atypical antidepressants, adrenergic alpha-2 receptor antagonists, and selective noradrenaline/dopamine reuptake inhibitors. (forhers.com)
  • SRD5A1 and SRD5A2 are associated with treatment for benign prostatic hyperplasia with the combination of 5a-reductase inhibitors and a-adrenergic receptor antagonists. (cdc.gov)
Selective8
  • non-selective alpha blockers and selective alpha blockers . (osmosis.org)
  • Accordingly, designing subtype-selective antagonists for each of the three alpha(1)-AR subtypes has been an enthusiastic region of medicinal research. (drugbank.com)
  • Even though a large number of studies on GPCRs have been conducted, understanding of how known antagonists bind to alpha(1)-ARs still remains sketchy and has been a serious impediment to search for potent and subtype-selective alpha(1)-AR antagonists because of the lack of detailed experimental structural knowledge. (drugbank.com)
  • SB-334867 is a selective orexin-1 (OX1) receptor antagonist. (selleckchem.com)
  • Isoprenaline HCl (NCI-c55630,Isoproterenol hydrochloride) is a non-selective beta-adrenergic receptor agonist, used for the treatment of bradycardia and heart block. (selleckchem.com)
  • An alpha(1a)-adrenoceptor-selective antagonist. (nih.gov)
  • A 80426 mesylate is a high affinity α 2 -adrenoceptor antagonist and selective 5-HT uptake inhibitor (K i values are 2.01 and 3.77 nM respectively). (bio-techne.com)
  • Giardina A-80426, a potent and selective β 2 -adrenoceptor antagonist with serotonin uptake-blocking activity and putative antidepressant-like effects: II. (bio-techne.com)
Agonist1
  • 9) A child has swallowed the contents of two bottles of a nasal decongestant whose primary ingredient is a potent alpha adrenoceptors agonist drug. (medicomaps.com)
Agonists and antagonists1
  • A series of adrenergic agonists and antagonists was applied by iontophoresis in the vicinity of noradrenergic neurons in the nucleus commissuralis of the rat. (duke.edu)
Blockers11
  • There's some evidence to support alpha-blockers-like silodosin-in treating kidney stones that get stuck in the ureters (tubes that move urine from the kidneys to the bladder). (verywellhealth.com)
  • Generic for Jalyn* can interact with other alpha blockers, antifungal medications, antimalaria medications, HIV/AIDS medicines, and heart or blood pressure medications. (internationaldrugmart.com)
  • What do alpha-blockers do to the heart? (digglicious.com)
  • For high blood pressure (hypertension): alpha-blockers work by relaxing blood vessels. (digglicious.com)
  • How do alpha-blockers work for anxiety? (digglicious.com)
  • Alpha blockers, such as prazosin, are medications that work as alpha-adrenergic receptor antagonists. (digglicious.com)
  • What is difference between alpha and beta-blockers? (digglicious.com)
  • Beta blockers may be cardioprotective but in contrast to alpha-1 antagonists tend to have adverse effects on plasma lipids. (digglicious.com)
  • Do alpha-blockers make you tired? (digglicious.com)
  • Side effects: Since alpha blockers affect your blood pressure, they can make you feel very tired and cause these other things as well: Dizziness. (digglicious.com)
  • How long do alpha-blockers stay in your system? (digglicious.com)
Phentolamine5
  • Antagonist displacement studies yielded a relative potency order of prazosin greater than or equal to WB4104 much greater than phentolamine greater than corynanthine greater than yohimbine greater than or equal to idazoxan greater than rauwolscine. (aspetjournals.org)
  • But what sets these two apart is that phenoxybenzamine is an irreversible, noncompetitive antagonist, while phentolamine is a reversible, competitive antagonist . (osmosis.org)
  • Phentolamine Mesylate(Phentolamine methanesulfonate) is a reversible and nonselective alpha-adrenergic receptor antagonist, used for the prevention or control of hypertensive episodes. (selleckchem.com)
  • Phentolamine, an alpha-adrenergic antagonist (1 microM), reduced sympathetic constriction in controls, but abolished this response in TiO2 exposed rats (max % change -22.3+/-3.1 control, -9.7+/-2.9 TiO2). (cdc.gov)
  • The constriction, in turn, was reduced or reversed by phentolamine, an alpha receptor antagonist. (jci.org)
Propranolol2
  • Propranolol is a nonselective beta-adrenergic receptor blocking agent. (medscape.com)
  • Propranolol, a non-specific β1-and β2-adrenergic receptor antagonist, was recently designated as the first therapeutic (orphan) drug for VHL disease. (nature.com)
Tamsulosin1
  • Tamsulosin is an alpha-adrenergic antagonist that works by relaxing muscles in the prostate and bladder neck, which helps relieve BPH symptoms such as urinary frequency, urinary urgency, and so on. (internationaldrugmart.com)
Dopamine7
  • The acute movement disorders that occur as manifestations of effects of neuroleptics and other dopamine antagonists include akathisia, acute dystonia, and other hyperkinetic dyskinesias. (medscape.com)
  • Acute effects of dopamine antagonists also include parkinsonian syndromes manifested by bradykinesia, rigidity, and pill rolling tremor. (medscape.com)
  • The acute movement disorders resulting from exposure to dopamine antagonists are commonly termed extrapyramidal syndromes (EPSs). (medscape.com)
  • The occurrence of acute movement disorders on exposure to dopamine antagonists is increased in female patients and older patients. (medscape.com)
  • Use of potent dopamine antagonists, prolonged exposure to dopamine antagonists, and prior occurrence of acute movement disorders on exposure to dopamine antagonists are also associated with an increased risk for the occurrence of acute movement adverse effects. (medscape.com)
  • Withdrawal dyskinesias may also occur as treatment with dopamine antagonists is decreased or withdrawn. (medscape.com)
  • In addition to the prototypic orofacial dyskinesia, tardive syndromes also include a spectrum of hyperkinesias occurring during or after prolonged treatment with dopamine antagonists. (medscape.com)
Prazosin1
  • We have conducted studies to examine: 1) binding characteristics of [3H]prazosin, 2) competition of antagonists at these sites and 3) different affinity states of the receptor for agonists and modulation of these states by 5'-guanylylimidodiphosphate [Gpp(NH)p]. (aspetjournals.org)
Medications2
  • Alright, so medications that inhibit peripheral postsynaptic adrenergic neurons are called peripheral postsynaptic anti-adrenergics. (osmosis.org)
  • Tardive dyskinesias (TDs) are involuntary movements of the tongue, lips, face, trunk, and extremities that occur in patients treated with long-term dopaminergic antagonist medications. (medscape.com)
Therapeutic1
  • The alpha(1)-ARs are of therapeutic interest because of their distinct and critical roles in many physiological processes, containing hypertension, benign prostatic hyperplasia, smooth muscle contraction, myocardial inotropy and chronotropy, and hepatic glucose metabolism. (drugbank.com)
Alpha21
  • Yohimbine HCL: Yohimbine is an alpha2 receptor antagonist (Kucio, 1991), which means it inhibits the action of the alpha2 receptor . (helpyougetgains.com)
Yohimbine1
  • Spinal administration of the alpha 1-adrenoceptor antagonist WB-4101 failed to alter the analgesic effects of the opioid, whereas the alpha 2-adrenoceptor antagonist yohimbine completely blocked beta-endorphin-induced elevations in tail-flick latency. (omeka.net)
Receptor blocker1
  • In order to overcome the β1-drawback, the properties of a high specific β2-adrenergic receptor blocker named ICI-118,551 have been studied. (nature.com)
Constriction1
  • METHODS: The ability of both drugs to prevent alpha-adrenoreceptor mediated constriction was tested in vitro in an organ bath in radial artery segments obtained from 20 patients. (ox.ac.uk)
Affinity3
  • Gpp(NH)p was without effect on antagonist affinity. (aspetjournals.org)
  • Nebivolol shows high affinity and selectivity for beta 1-adrenergic receptor sites in a rabbit lung membrane preparation (K i value = 0.9 nM and beta 2/beta 1 ratio = 50). (selleckchem.com)
  • High affinity α 2 antagonist. (bio-techne.com)
Neurons2
  • Alpha-receptor mediated inhibition of A2 noradrenergic neurons. (duke.edu)
  • Alpha-2 receptor-mediated inhibition of these neurons was observed with single-unit recording techniques. (duke.edu)
Medication1
  • It's a member of the alpha-1 adrenergic receptor antagonist medication class, which is also simply called the alpha-blocker class. (verywellhealth.com)
Testosterone2
  • Testosterone via 5 alpha reductase gets converted to Dihydroxy Testosterone, what are the effects of testosterone and DHT? (brainscape.com)
  • V89L polymorphism of the testosterone 5-alpha-reductase II gene and prognostic factors of prostate cancer]. (cdc.gov)
Phenoxybenzamine1
  • CONCLUSIONS: Phenoxybenzamine more effectively prevents alpha-adrenoreceptor mediated spasm of the human radial artery than papaverine. (ox.ac.uk)
Subtypes1
  • So far three distinct alpha(1)-AR subtypes, alpha(1A), alpha(1B) and alpha(1D), have been characterized by functional analysis, radio-ligand binding and molecular biology studies. (drugbank.com)
Exposure1
  • The enhanced sensitivity to alpha-adrenergic receptor blockade following TiO2 exposure suggests an augmented responsiveness to tonic sympathetic activity. (cdc.gov)
Effects1
  • Drugs with combined beta and alpha-1 blocking activity such as labetalol have favorable metabolic effects but postural hypotension remains a problem. (digglicious.com)
Withdrawal1
  • the antagonist activity may provoke withdrawal Sx. (medscape.com)
Products1
  • View all Adrenergic alpha-2 Receptor Antagonists products. (bio-techne.com)
Evidence1
  • Some evidence suggests that the rhabdosphincter in cats has triple innervation, with cholinergic, adrenergic, possibly copeptidergic, and traditional motor endplates. (medscape.com)
Blood pressure1
  • Nisoldipine, another calcium antagonist, also failed to lower the patient's blood pressure, when given in combination with rifampicin. (nih.gov)
Drugs1
  • Combined with experimental data, these computational attempts could improve our understanding of the structural basis of antagonist binding and the molecular basis of receptor activation, thus offering a more reasonable approach in the design of drugs targeting alpha(1)-ARs. (drugbank.com)
Carvedilol in Preventing Heart Failure in Childhood Cancer Survivors - Full Text View - ClinicalTrials.gov
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Hyperaldosteronism Clinical Presentation: History, Physical Examination, Complications
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Hyperaldosteronism: Practice Essentials, Pathophysiology, Etiology
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Urologic Management in Neurologic Disease: Overview, Neuroanatomy of Pelvic Floor, Neurophysiology of Pelvic Floor
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Hypertensive Emergencies: Uncontrolled Blood Pressure, Management of Hypertensive Emergencies
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CREST Syndrome Treatment & Management: Medical Care, Surgical Care, Consultations
CREST Syndrome Treatment & Management: Medical Care, Surgical Care, Consultations (medscape.com)
(emedicine.medscape.com)
DailyMed - CARDURA- doxazosin mesylate tablet CARDURA- doxazosin tablet
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Complex Regional Pain Syndromes Treatment & Management: Medical Care, Surgical Care, Consultations
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Gonadal Hormones: Androgens Flashcards by Nicole Pritchard | Brainscape
Gonadal Hormones: Androgens Flashcards by Nicole Pritchard | Brainscape (brainscape.com)
Adrenergic antagonists: Alpha blockers | Osmosis
Adrenergic antagonists: Alpha blockers | Osmosis (osmosis.org)
Modeling the interactions between alpha(1)-adrenergic receptors and their antagonists. | DrugBank Online
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Hepatorenal Syndrome Treatment & Management: Approach Considerations, Medical Care, Surgical Care
Hepatorenal Syndrome Treatment & Management: Approach Considerations, Medical Care, Surgical Care (medscape.com)
(emedicine.medscape.com)
These highlights do not include all the information needed to use alfuzosin hydrochloride extended-release tablets safely and...
These highlights do not include all the information needed to use alfuzosin hydrochloride extended-release tablets safely and... (dailymed.nlm.nih.gov)
These highlights do not include all the information needed to use DUTASTERIDE CAPSULES safely and effectively. See full...
These highlights do not include all the information needed to use DUTASTERIDE CAPSULES safely and effectively. See full... (dailymed.nlm.nih.gov)
These highlights do not include all the information needed to use ALFUZOSIN HYDROCHLORIDE EXTENDED-RELEASE TABLETS safely and...
These highlights do not include all the information needed to use ALFUZOSIN HYDROCHLORIDE EXTENDED-RELEASE TABLETS safely and... (dailymed.nlm.nih.gov)
These highlights do not include all the information needed to use DUTASTERIDE CAPSULES safely and effectively. See full...
These highlights do not include all the information needed to use DUTASTERIDE CAPSULES safely and effectively. See full... (dailymed.nlm.nih.gov)
These highlights do not include all the information needed to use DUTASTERIDE CAPSULES safely and effectively. See full...
These highlights do not include all the information needed to use DUTASTERIDE CAPSULES safely and effectively. See full... (dailymed.nlm.nih.gov)
These highlights do not include all the information needed to use ALFUZOSIN HYDROCHLORIDE EXTENDED-RELEASE TABLET safely and...
These highlights do not include all the information needed to use ALFUZOSIN HYDROCHLORIDE EXTENDED-RELEASE TABLET safely and... (dailymed.nlm.nih.gov)