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.Prostatitis: Infiltration of inflammatory cells into the parenchyma of PROSTATE. The subtypes are classified by their varied laboratory analysis, clinical presentation and response to treatment.Prostate: A gland in males that surrounds the neck of the URINARY BLADDER and the URETHRA. It secretes a substance that liquefies coagulated semen. It is situated in the pelvic cavity behind the lower part of the PUBIC SYMPHYSIS, above the deep layer of the triangular ligament, and rests upon the RECTUM.Phentolamine: A nonselective alpha-adrenergic antagonist. It is used in the treatment of hypertension and hypertensive emergencies, pheochromocytoma, vasospasm of RAYNAUD DISEASE and frostbite, clonidine withdrawal syndrome, impotence, and peripheral vascular disease.Pelvic Pain: Pain in the pelvic region of genital and non-genital origin and of organic or psychogenic etiology. Frequent causes of pain are distension or contraction of hollow viscera, rapid stretching of the capsule of a solid organ, chemical irritation, tissue ischemia, and neuritis secondary to inflammatory, neoplastic, or fibrotic processes in adjacent organs. (Kase, Weingold & Gershenson: Principles and Practice of Clinical Gynecology, 2d ed, pp479-508)Dihydroergotoxine: A mixture of three different hydrogenated derivatives of ERGOTAMINE: DIHYDROERGOCORNINE; DIHYDROERGOCRISTINE; and DIHYDROERGOCRYPTINE. Dihydroergotoxine has been proposed to be a neuroprotective agent and a nootropic agent. The mechanism of its therapeutic actions is not clear, but it can act as an alpha-adrenergic antagonist and a dopamine agonist. The methanesulfonate salts of this mixture of alkaloids are called ERGOLOID MESYLATES.Chlorthalidone: A benzenesulfonamide-phthalimidine that tautomerizes to a BENZOPHENONES form. It is considered a thiazide-like diuretic.Antihypertensive Agents: Drugs used in the treatment of acute or chronic vascular HYPERTENSION regardless of pharmacological mechanism. Among the antihypertensive agents are DIURETICS; (especially DIURETICS, THIAZIDE); ADRENERGIC BETA-ANTAGONISTS; ADRENERGIC ALPHA-ANTAGONISTS; ANGIOTENSIN-CONVERTING ENZYME INHIBITORS; CALCIUM CHANNEL BLOCKERS; GANGLIONIC BLOCKERS; and VASODILATOR AGENTS.Doxazosin: A prazosin-related compound that is a selective alpha-1-adrenergic blocker.Heart Failure: A heterogeneous condition in which the heart is unable to pump out sufficient blood to meet the metabolic need of the body. Heart failure can be caused by structural defects, functional abnormalities (VENTRICULAR DYSFUNCTION), or a sudden overload beyond its capacity. Chronic heart failure is more common than acute heart failure which results from sudden insult to cardiac function, such as MYOCARDIAL INFARCTION.Diuretics: Agents that promote the excretion of urine through their effects on kidney function.Azasteroids: Steroidal compounds in which one or more carbon atoms in the steroid ring system have been substituted with nitrogen atoms.Priapism: A prolonged painful erection that may lasts hours and is not associated with sexual activity. It is seen in patients with SICKLE CELL ANEMIA, advanced malignancy, spinal trauma; and certain drug treatments.Dizziness: An imprecise term which may refer to a sense of spatial disorientation, motion of the environment, or lightheadedness.Penile Erection: The state of the PENIS when the erectile tissue becomes filled or swollen (tumid) with BLOOD and causes the penis to become rigid and elevated. It is a complex process involving CENTRAL NERVOUS SYSTEM; PERIPHERAL NERVOUS SYSTEMS; HORMONES; SMOOTH MUSCLES; and vascular functions.Prostatic Hyperplasia: Increase in constituent cells in the PROSTATE, leading to enlargement of the organ (hypertrophy) and adverse impact on the lower urinary tract function. This can be caused by increased rate of cell proliferation, reduced rate of cell death, or both.Urination: Discharge of URINE, liquid waste processed by the KIDNEY, from the body.Dry Eye Syndromes: Corneal and conjunctival dryness due to deficient tear production, predominantly in menopausal and post-menopausal women. Filamentary keratitis or erosion of the conjunctival and corneal epithelium may be caused by these disorders. Sensation of the presence of a foreign body in the eye and burning of the eyes may occur.Drug Interactions: The action of a drug that may affect the activity, metabolism, or toxicity of another drug.Rheumatic Heart Disease: Cardiac manifestation of systemic rheumatological conditions, such as RHEUMATIC FEVER. Rheumatic heart disease can involve any part the heart, most often the HEART VALVES and the ENDOCARDIUM.Atrial Fibrillation: Abnormal cardiac rhythm that is characterized by rapid, uncoordinated firing of electrical impulses in the upper chambers of the heart (HEART ATRIA). In such case, blood cannot be effectively pumped into the lower chambers of the heart (HEART VENTRICLES). It is caused by abnormal impulse generation.Rheumatic Fever: A febrile disease occurring as a delayed sequela of infections with STREPTOCOCCUS PYOGENES. It is characterized by multiple focal inflammatory lesions of the connective tissue structures, such as the heart, blood vessels, and joints (POLYARTHRITIS) and brain, and by the presence of ASCHOFF BODIES in the myocardium and skin.Hyperthyroidism: Hypersecretion of THYROID HORMONES from the THYROID GLAND. Elevated levels of thyroid hormones increase BASAL METABOLIC RATE.Heart Atria: The chambers of the heart, to which the BLOOD returns from the circulation.Heart: The hollow, muscular organ that maintains the circulation of the blood.Heart Rate: The number of times the HEART VENTRICLES contract per unit of time, usually per minute.

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)

Synonyms for alpha-blocking agent in Free Thesaurus. Antonyms for alpha-blocking agent. 2 synonyms for alpha: first and last, be-all and end-all. What are synonyms for alpha-blocking agent?
Alpha blockers lower blood pressure by keeping the hormone norepinephrine from tightening the muscles in the walls of smaller arteries and veins. As a result, the vessels remain open and relaxed. This improves blood flow and lowers blood pressure.. Because alpha blockers also relax other muscles throughout the body, these medications also can help improve urine flow in older men with prostate problems.. Alpha blockers are either short-acting or long-acting. Short-acting medications work quickly, but their effects last only a few hours. Long-acting medications take longer to work, but their effects last longer. The alpha blocker thats best for you depends on your health and the condition being treated.. Alpha blockers are also called alpha-adrenergic blocking agents, alpha-adrenergic antagonists, adrenergic blocking agents and alpha-blocking agents.. Examples of alpha blockers used to treat high blood pressure include:. ...
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 ...
Define alpha-blocker. alpha-blocker synonyms, alpha-blocker pronunciation, alpha-blocker translation, English dictionary definition of alpha-blocker. n. A drug that blocks or counteracts the effects of epinephrine and other molecules that stimulate alpha-receptors, leading to various physiological...
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. ...
Ioannides, C, Okine, L and Parke, DV (1979) Effects of β-adrenoceptor antagonists on the hepatic mixed-function oxygenases in the rat ...
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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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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Hytrin is an alpha-adrenergic blocker, which relaxes blood vessels. It is prescribed to treat hypertension and benign prostatic hyperplasia.
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This review evaluates the role of α-adrenoceptor antagonists as a potential treatment of prostate cancer (PCa). Cochrane, Google Scholar and Pubmed were accessed to retrieve sixty-two articles for analysis. In vitro studies demonstrate that doxazosin, prazosin and terazosin (quinazoline α-antagonists) induce apoptosis, decrease cell growth, and proliferation in PC-3, LNCaP and DU-145 cell lines. Similarly, the piperazine based naftopidil induced cell cycle arrest and death in LNCaP-E9 cell lines. In contrast, sulphonamide based tamsulosin did not exhibit these effects. In vivo data was consistent with in vitro findings as the quinazoline based α-antagonists prevented angiogenesis and decreased tumour mass in mice models of PCa. Mechanistically the cytotoxic and antitumor effects of the α-antagonists appear largely independent of α 1-blockade. The proposed targets include: VEGF, EGFR, HER2/Neu, caspase 8/3, topoisomerase 1 and other mitochondrial apoptotic inducing factors. These cytotoxic effects
This review evaluates the role of α-adrenoceptor antagonists as a potential treatment of prostate cancer (PCa). Cochrane, Google Scholar and Pubmed were accessed to retrieve sixty-two articles for analysis. In vitro studies demonstrate that doxazosin, prazosin and terazosin (quinazoline α-antagonists) induce apoptosis, decrease cell growth, and proliferation in PC-3, LNCaP and DU-145 cell lines. Similarly, the piperazine based naftopidil induced cell cycle arrest and death in LNCaP-E9 cell lines. In contrast, sulphonamide based tamsulosin did not exhibit these effects. In vivo data was consistent with in vitro findings as the quinazoline based α-antagonists prevented angiogenesis and decreased tumour mass in mice models of PCa. Mechanistically the cytotoxic and antitumor effects of the α-antagonists appear largely independent of α 1-blockade. The proposed targets include: VEGF, EGFR, HER2/Neu, caspase 8/3, topoisomerase 1 and other mitochondrial apoptotic inducing factors. These cytotoxic effects
Flomax is a drug that is often used to treat benign prostatic hyperplasia (BPH). It is an alpha-blocker and it affects the hormones adrenaline and noradrenaline. There may be side effects, and other drugs may be used. Home remedies can also help relieve symptoms. Find out more about Flomax and other treatment options.
The exact mechanism of the hypotensive action of prazosin is unknown. Prazosin causes a decrease in total peripheral resistance and was originally thought to have a direct relaxant action on vascular smooth muscle. Recent animal studies, however, have suggested that the vasodilator effect of prazosin is also related to blockade of postsynaptic alpha-adrenoceptors. The results of dog forelimb experiments demonstrate that the peripheral vasodilator effect of prazosin is confined mainly to the level of the resistance vessels (arterioles). Unlike conventional alpha-blockers, the antihypertensive action of prazosin is usually not accompanied by a reflex tachycardia. Tolerance has not been observed to develop in long term therapy.. Hemodynamic studies have been carried out in man following acute single dose administration and during the course of long term maintenance therapy. The results confirm that the therapeutic effect is a fall in blood pressure unaccompanied by a clinically significant change ...
Minipress is classified as an alpha-adrenergic blocker. The active ingredient of the medication, Prazosin, stimulates an inevitable action relaxing the arteries and veins. This way, the treatment produces easier blood circulation in the body.
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Hytrin is an alpha-adrenergic blocker, which relaxes blood vessels. It is prescribed to treat hypertension and benign prostatic hyperplasia.
In previous reports from this laboratory, it has been proposed that stress ulceration results from a severe gastric mucosal energy deficit due to shock-induced mucosal ischemia. In the experiments described in this report, the hypothesis was further
Doxazosin is an alpha-adrenergic (AL-fa ad-ren-ER-jik) blockers. Doxazosin relaxes your veins and arteries so that blood can more easily pass through them. It also relaxes the muscles in the prostate and bladder neck, making it easier to urinate. Doxazosin is used to treat hypertension (high blood pressure), or to...
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Prazosin, 1-(4-amino-6,7-dimetoksi-2-hinazolinil)-4-(2-furoil)-piperazin, se sintetiše iz 2-amino-4,5-dimetoksibenzoinske kiseline, koji nakon reakcije sa natrijum cijanatom podleže heterociklizaciji do 2,4-dihidroksi-6,7-dimetoksihinazolina. Supstituisanje hidroksilnih grupa ovog jedinjenja atomima hlora reakcijom sa tionil hloridom, ili smešom fosfor oksihlorida sa fosfor pentahloridom daje 2,4-dihloro-6,7-dimetoksihinazolin. Naknadnom reakcijom sa amonijakom, atom hlora u C4 poziciji pirimidinskog prstena se zamenjuje amino grupom, što dovodi do formiranja 4-amino-2-hloro-6,7-dimetoksihinazolina. Njegovim uvođenjem u reakciju sa 1-(2-furoil)piperazinom formira se prazosin.[3][4][5][6][7][8][9][10][11][12]. ...
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... 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. ...
... 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 ...
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 ...
... 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): ...
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 ...
... 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 ...
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 ...
"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 ...
... 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. ...
... 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 ...
... 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". ...
Yang G, Wei Q, Li H, Yang Y, Zhang S, Dong Q (2006). "The effect of alpha-adrenergic antagonists in chronic prostatitis/chronic ...
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 ...
... 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. ...
... a reversible nonselective alpha-adrenergic antagonist Piberaline, a psychoactive drug. ...
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 ...
... 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. ...
... is a drug used in benign prostatic hypertrophy which acts as a selective α1-adrenergic receptor antagonist or alpha blocker. ...
In addition, it has alpha-adrenergic antagonist activities in vascular tissue, and it has also been reported to have ...
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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- ...
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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 ...
α2-blockers are a subset of the alpha blocker class of drugs and are antagonists to the α2 adrenergic receptor. They are mainly ... Chopin P, Colpaert FC, Marien M (February 1999). "Effects of alpha-2 adrenoceptor agonists and antagonists on circling behavior ... Lemke, KA (June 2004). "Perioperative use of selective alpha-2 agonists and antagonists in small animals". The Canadian ... Haapalinna A, Leino T, Heinonen E (November 2003). "The alpha 2-adrenoceptor antagonist atipamezole potentiates anti- ...
... 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) ...
... by drugs known as neurokinin type 1 antagonists (also termed: SP antagonists, or tachykinin antagonists.) One such drug is ... Azzolina A, Bongiovanni A, Lampiasi N (Dec 2003). "Substance P induces TNF-alpha and IL-6 production through NF kappa B in ... administered through the non-adrenergic, non-cholinergic nervous system (branch of the vagal system). ... Muñoz M, Rosso M, Coveñas R (2010). "A new frontier in the treatment of cancer: NK-1 receptor antagonists". Current Medicinal ...
28] Yang G, Wei Q, Li H, Yang Y, Zhang S, Dong Q. The effect of alpha-adrenergic antagonists in chronic prostatitis/chronic ... Eight randomized placebo-controlled trials have evaluated the use of different alpha-adrenergic antagonists in CP/CPPS patients ... Alpha blocker therapy: We recommend alpha blocker therapy for the newly diagnosed, alpha blocker naïve patients with ... We therefore recommend alpha blocker therapy for the newly diagnosed, alpha blocker naïve patients with significant voiding ...
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Alpha-adrenergic antagonists. Class Summary. These agents are used in the treatment of benign prostatic hypertrophy. Studies ... An alpha-adrenergic blocker, specifically targeting the A1 receptors, tamsulosin has the advantage of causing relatively less ... alpha-Blockers for Treatment of the Prostatitis Syndromes. Rev Urol. 2005. 7 Suppl 8:S18-25. [Medline]. [Full Text]. ... Alpha-blockers reduce bladder outlet obstruction and thus improve voiding dysfunction that may be associated with prostatic ...
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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. ...
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Alpha-1 adrenergic antagonist properties.. Experiments were carried out in rats (270-390 g) that had free access to water and ... Thealpha-1-adrenergic antagonist, prazosin, tested at doses up to 160 mg/kg, was unable to protect from the effects of ... and alpha-1 adrenergic antagonist activity (inhibition of the pressor response induced by methoxamine; ○) after i.p. ... and had a 70-fold separation between its 5-HT1Aagonist and alpha-1 adrenergic antagonist properties (measured as the ability to ...
  • Clinical efficacy and tolerability of alpha-blocker doxazosin as add-on therapy in patients with hypertension and impaired glucose metabolism. (nextbio.com)
  • β2- Adrenergic Receptor-Mediated HIF-1α Upregulation Mediates Blood Brain Barrier Damage in Acute Cerebral Ischemia Disruption of the blood brain barrier (BBB) within the thrombolytic time window is an antecedent event to intracerebral hemorrhage in ischemic stroke. (tripdatabase.com)
  • Acute and chronic intrarenal alpha- and beta- adrenergic receptor stimulation of renin release in the conscious dog. (ahajournals.org)
  • Two yet to be launched products, Forest Laboratories/Cypress Biosciences's antidepressant milnacipran and Schwarz Pharma's sodium ion channel antagonist/CRMP2 modulator lacosamide (Vimpat), will compete for market share as well as provide the benefit of an additional mechanism of action. (massagemag.com)
  • We believe that adrenergic agonists may have a dual mechanism of action: the first one consists of a catecholamine action on its receptor with the formation of a stimulus-receptor complex. (scielo.br)
  • Medications (alpha adrenergic antagonists) that can relax the smooth muscle of the prostate and that reduce the pressure that causes the urethral obstruction are now being tested in Europe and the United States, but have not as yet received necessary Food and Drug Administration approval for use in the United States. (chicagotribune.com)
  • https://www.heart.org/en/health-topics/high-blood-pressure/changes-you-can-make-to-manage-high-blood-pressure/types-of-blood-pressure-medications. (mayoclinic.org)
  • Used in the treatment of iatrogenically induced mydriasis produced by adrenergic (phenylephrine) or parasympatholytic (tropicamide) agents used in certain eye examinations. (pharmacycode.com)
  • This study assessed whether platelet hyperreactivity to epinephrine in hypercholesterolemia is associated with higher alpha 2-adrenergic receptor density or affinity for epinephrine. (nih.gov)
  • Platelet alpha 2-adrenergic receptor density is increased in hypercholesterolemia and directly correlates with plasma total and levels of LDL cholesterol, providing at least a partial explanation for the enhanced platelet response to epinephrine that is observed in hypercholesterolemia. (nih.gov)
  • 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)