Benzazepines: Compounds with BENZENE fused to AZEPINES.Fenoldopam: A dopamine D1 receptor agonist that is used as an antihypertensive agent. It lowers blood pressure through arteriolar vasodilation.Receptors, Dopamine: Cell-surface proteins that bind dopamine with high affinity and trigger intracellular changes influencing the behavior of cells.Encyclopedias as Topic: Works containing information articles on subjects in every field of knowledge, usually arranged in alphabetical order, or a similar work limited to a special field or subject. (From The ALA Glossary of Library and Information Science, 1983)Dopamine: One of the catecholamine NEUROTRANSMITTERS in the brain. It is derived from TYROSINE and is the precursor to NOREPINEPHRINE and EPINEPHRINE. Dopamine is a major transmitter in the extrapyramidal system of the brain, and important in regulating movement. A family of receptors (RECEPTORS, DOPAMINE) mediate its action.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.Receptors, Adrenergic, beta: One of two major pharmacologically defined classes of adrenergic receptors. The beta adrenergic receptors play an important role in regulating CARDIAC MUSCLE contraction, SMOOTH MUSCLE relaxation, and GLYCOGENOLYSIS.Dose-Response Relationship, Drug: The relationship between the dose of an administered drug and the response of the organism to the drug.Domperidone: A specific blocker of dopamine receptors. It speeds gastrointestinal peristalsis, causes prolactin release, and is used as antiemetic and tool in the study of dopaminergic mechanisms.Galactogogues: Substances that induce LACTATION.Gastrointestinal Motility: The motor activity of the GASTROINTESTINAL TRACT.Gastroesophageal Reflux: Retrograde flow of gastric juice (GASTRIC ACID) and/or duodenal contents (BILE ACIDS; PANCREATIC JUICE) into the distal ESOPHAGUS, commonly due to incompetence of the LOWER ESOPHAGEAL SPHINCTER.Suppositories: Medicated dosage forms that are designed to be inserted into the rectal, vaginal, or urethral orifice of the body for absorption. Generally, the active ingredients are packaged in dosage forms containing fatty bases such as cocoa butter, hydrogenated oil, or glycerogelatin that are solid at room temperature but melt or dissolve at body temperature.Gastrointestinal Diseases: Diseases in any segment of the GASTROINTESTINAL TRACT from ESOPHAGUS to RECTUM.MedlinePlus: NATIONAL LIBRARY OF MEDICINE service for health professionals and consumers. It links extensive information from the National Institutes of Health and other reviewed sources of information on specific diseases and conditions.Consumer Health Information: Information intended for potential users of medical and healthcare services. There is an emphasis on self-care and preventive approaches as well as information for community-wide dissemination and use.Social Media: Platforms that provide the ability and tools to create and publish information accessed via the INTERNET. Generally these platforms have three characteristics with content user generated, high degree of interaction between creator and viewer, and easily integrated with other sites.Dissent and Disputes: Differences of opinion or disagreements that may arise, for example, between health professionals and patients or their families, or against a political regime.Internet: A loose confederation of computer communication networks around the world. The networks that make up the Internet are connected through several backbone networks. The Internet grew out of the US Government ARPAnet project and was designed to facilitate information exchange.Peer Review: An organized procedure carried out by a select committee of professionals in evaluating the performance of other professionals in meeting the standards of their specialty. Review by peers is used by editors in the evaluation of articles and other papers submitted for publication. Peer review is used also in the evaluation of grant applications. It is applied also in evaluating the quality of health care provided to patients.Neuropharmacology: The branch of pharmacology dealing especially with the action of drugs upon various parts of the nervous system.Levodopa: The naturally occurring form of DIHYDROXYPHENYLALANINE and the immediate precursor of DOPAMINE. Unlike dopamine itself, it can be taken orally and crosses the blood-brain barrier. It is rapidly taken up by dopaminergic neurons and converted to DOPAMINE. It is used for the treatment of PARKINSONIAN DISORDERS and is usually given with agents that inhibit its conversion to dopamine outside of the central nervous system.Seasons: Divisions of the year according to some regularly recurrent phenomena usually astronomical or climatic. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 6th ed)Parkinson Disease: A progressive, degenerative neurologic disease characterized by a TREMOR that is maximal at rest, retropulsion (i.e. a tendency to fall backwards), rigidity, stooped posture, slowness of voluntary movements, and a masklike facial expression. Pathologic features include loss of melanin containing neurons in the substantia nigra and other pigmented nuclei of the brainstem. LEWY BODIES are present in the substantia nigra and locus coeruleus but may also be found in a related condition (LEWY BODY DISEASE, DIFFUSE) characterized by dementia in combination with varying degrees of parkinsonism. (Adams et al., Principles of Neurology, 6th ed, p1059, pp1067-75)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.Receptors, Dopamine D3: A subtype of dopamine D2 receptors that are highly expressed in the LIMBIC SYSTEM of the brain.Receptors, Dopamine D2: A subfamily of G-PROTEIN-COUPLED RECEPTORS that bind the neurotransmitter DOPAMINE and modulate its effects. D2-class receptor genes contain INTRONS, and the receptors inhibit ADENYLYL CYCLASES.Periodicals as Topic: A publication issued at stated, more or less regular, intervals.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.Hemolysin Factors: Plasmids controlling the synthesis of hemolysin by bacteria.Mesoridazine: A phenothiazine antipsychotic with effects similar to CHLORPROMAZINE.Neuroleptic Malignant Syndrome: A potentially fatal syndrome associated primarily with the use of neuroleptic agents (see ANTIPSYCHOTIC AGENTS) which are in turn associated with dopaminergic receptor blockade (see RECEPTORS, DOPAMINE) in the BASAL GANGLIA and HYPOTHALAMUS, and sympathetic dysregulation. Clinical features include diffuse MUSCLE RIGIDITY; TREMOR; high FEVER; diaphoresis; labile blood pressure; cognitive dysfunction; and autonomic disturbances. Serum CPK level elevation and a leukocytosis may also be present. (From Adams et al., Principles of Neurology, 6th ed, p1199; Psychiatr Serv 1998 Sep;49(9):1163-72)Thioridazine: A phenothiazine antipsychotic used in the management of PHYCOSES, including SCHIZOPHRENIA.Phenothiazines: Compounds containing dibenzo-1,4-thiazine. Some of them are neuroactive.Akathisia, Drug-Induced: A condition associated with the use of certain medications and characterized by an internal sense of motor restlessness often described as an inability to resist the urge to move.Dyskinesia, Drug-Induced: Abnormal movements, including HYPERKINESIS; HYPOKINESIA; TREMOR; and DYSTONIA, associated with the use of certain medications or drugs. Muscles of the face, trunk, neck, and extremities are most commonly affected. Tardive dyskinesia refers to abnormal hyperkinetic movements of the muscles of the face, tongue, and neck associated with the use of neuroleptic agents (see ANTIPSYCHOTIC AGENTS). (Adams et al., Principles of Neurology, 6th ed, p1199)Designer Drugs: Drugs designed and synthesized, often for illegal street use, by modification of existing drug structures (e.g., amphetamines). Of special interest are MPTP (a reverse ester of meperidine), MDA (3,4-methylenedioxyamphetamine), and MDMA (3,4-methylenedioxymethamphetamine). Many drugs act on the aminergic system, the physiologically active biogenic amines.N-Methyl-3,4-methylenedioxyamphetamine: An N-substituted amphetamine analog. It is a widely abused drug classified as a hallucinogen and causes marked, long-lasting changes in brain serotonergic systems. It is commonly referred to as MDMA or ecstasy.Street Drugs: Drugs obtained and often manufactured illegally for the subjective effects they are said to produce. They are often distributed in urban areas, but are also available in suburban and rural areas, and tend to be grossly impure and may cause unexpected toxicity.Imitative Behavior: The mimicking of the behavior of one individual by another.Carbidopa: An inhibitor of DOPA DECARBOXYLASE, preventing conversion of LEVODOPA to dopamine. It is used in PARKINSON DISEASE to reduce peripheral adverse effects of LEVODOPA. It has no antiparkinson actions by itself.Dopa Decarboxylase: One of the AROMATIC-L-AMINO-ACID DECARBOXYLASES, this enzyme is responsible for the conversion of DOPA to DOPAMINE. It is of clinical importance in the treatment of Parkinson's disease.Dihydroxyphenylalanine: A beta-hydroxylated derivative of phenylalanine. The D-form of dihydroxyphenylalanine has less physiologic activity than the L-form and is commonly used experimentally to determine whether the pharmacological effects of LEVODOPA are stereospecific.Stereoisomerism: The phenomenon whereby compounds whose molecules have the same number and kind of atoms and the same atomic arrangement, but differ in their spatial relationships. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)Aminoquinolines: Quinolines substituted in any position by one or more amino groups.Dopamine Agonists: Drugs that bind to and activate dopamine receptors.Aromatic-L-Amino-Acid Decarboxylases: An enzyme group with broad specificity. The enzymes decarboxylate a range of aromatic amino acids including dihydroxyphenylalanine (DOPA DECARBOXYLASE); TRYPTOPHAN; and HYDROXYTRYPTOPHAN.Awards and PrizesBenserazide: An inhibitor of DOPA DECARBOXYLASE that does not enter the central nervous system. It is often given with LEVODOPA in the treatment of parkinsonism to prevent the conversion of levodopa to dopamine in the periphery, thereby increasing the amount that reaches the central nervous system and reducing the required dose. It has no antiparkinson actions when given alone.Benzothiepins2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine: A selective D1 dopamine receptor agonist used primarily as a research tool.Receptors, Dopamine D1: A subfamily of G-PROTEIN-COUPLED RECEPTORS that bind the neurotransmitter DOPAMINE and modulate its effects. D1-class receptor genes lack INTRONS, and the receptors stimulate ADENYLYL CYCLASES.Benzocycloheptenes

Plasticity of first-order sensory synapses: interactions between homosynaptic long-term potentiation and heterosynaptically evoked dopaminergic potentiation. (1/1467)

Persistent potentiations of the chemical and electrotonic components of the eighth nerve (NVIII) EPSP recorded in vivo in the goldfish reticulospinal neuron, the Mauthner cell, can be evoked by afferent tetanization or local dendritic application of an endogenous transmitter, dopamine (3-hydroxytyramine). These modifications are attributable to the activation of distinct intracellular kinase cascades. Although dopamine-evoked potentiation (DEP) is mediated by the cAMP-dependent protein kinase (PKA), tetanization most likely activates a Ca2+-dependent protein kinase via an increased intracellular Ca2+ concentration. We present evidence that the eighth nerve tetanus that induces LTP does not act by triggering dopamine release, because it is evoked in the presence of a broad spectrum of dopamine antagonists. To test for interactions between these pathways, we applied the potentiating paradigms sequentially. When dopamine was applied first, tetanization produced additional potentiation of the mixed synaptic response, but when the sequence was reversed, DEP was occluded, indicating that the synapses potentiated by the two procedures belong to the same or overlapping populations. Experiments were conducted to determine interactions between the underlying regulatory mechanisms and the level of their convergence. Inhibiting PKA does not impede tetanus-induced LTP, and chelating postsynaptic Ca2+ with BAPTA does not block DEP, indicating that the initial steps of the induction processes are independent. Pharmacological and voltage-clamp analyses indicate that the two pathways converge on functional AMPA/kainate receptors for the chemically mediated EPSP and gap junctions for the electrotonic component or at intermediaries common to both pathways. A cellular model incorporating these interactions is proposed on the basis of differential modulation of synaptic responses via receptor-protein phosphorylation.  (+info)

Ergoline derivative LEK-8829-induced turning behavior in rats with unilateral striatal ibotenic acid lesions: interaction with bromocriptine. (2/1467)

LEK-8829 [9,10-didehydro-N-methyl-(2-propynyl)-6-methyl-8- aminomethylergoline bimaleinate] is an antagonist of dopamine D2 receptors and serotonin (5-HT)2 and 5-HT1A receptors in intact animals and a D1 receptor agonist in dopamine-depleted animals. In the present study, we used rats with unilateral striatal lesions with ibotenic acid (IA) to investigate the dopamine receptor activities of LEK-8829 in a model with innervated dopamine receptors. The IA-lesioned rats circled ipsilaterally when challenged with apomorphine, the mixed agonist on D1/D2 receptors. LEK-8829 induced a dose-dependent contralateral turning that was blocked by D1 receptor antagonist SCH-23390. The treatment with D1 receptor agonist SKF-82958 induced ipsilateral turning, whereas the treatment with D2 receptor antagonist haloperidol induced contralateral posture. The combined treatment with SKF-82958 and haloperidol resulted in a weak contralateral turning, indicating the possible receptor mechanism of contralateral turning induced by LEK-8829. Bromocriptine induced a weak ipsilateral turning that was blocked by haloperidol. The ipsilateral turning induced by bromocriptine was significantly potentiated by the coadministration of a low dose but not by a high dose of LEK-8829. The potentiation of turning was blocked either by SCH-23390 or by haloperidol. The potentiation of ipsilateral turning suggests the costimulation of D2 and D1 receptors by bromocriptine and LEK-8829, respectively, whereas the lack of potentiation by the highest dose of LEK-8829 may be explained by the opposing activity of LEK-8829 and bromocriptine at D2 receptors. We propose that the D2 and 5HT2 receptor-blocking and D1 receptor-stimulating profile of LEK-8829 is promising for the treatment of negative symptoms of schizophrenia.  (+info)

Behavioral, toxic, and neurochemical effects of sydnocarb, a novel psychomotor stimulant: comparisons with methamphetamine. (3/1467)

Sydnocarb (3-(beta-phenylisopropyl)-N-phenylcarbamoylsydnonimine) is a psychostimulant in clinical practice in Russia as a primary and adjunct therapy for a host of psychiatric disorders, including schizophrenia and depression. It has been described as a stimulant with an addiction liability and toxicity less than that of amphetamines. The present study undertook to evaluate the psychomotor stimulant effects of sydnocarb in comparison to those of methamphetamine. Sydnocarb increased locomotor activity of mice with reduced potency (approximately 10-fold) and efficacy compared with methamphetamine. Sydnocarb blocked the locomotor depressant effects of haloperidol at doses that were inactive when given alone. The locomotor stimulant effects of both methamphetamine and sydnocarb were dose-dependently blocked by the dopamine D1 and D2 antagonists SCH 39166 and spiperone, respectively; blockade generally occurred at doses of the antagonists that did not depress locomotor activity when given alone. In mice trained to discriminate methamphetamine from saline, sydnocarb fully substituted for methamphetamine with a 9-fold lower potency. When substituted for methamphetamine under self-administration experiments in rats, 10-fold higher concentrations of sydnocarb maintained responding by its i.v. presentation. Sydnocarb engendered stereotypy in high doses with approximately a 2-fold lower potency than methamphetamine. However, sydnocarb was much less efficacious than methamphetamine in inducing stereotyped behavior. Both sydnocarb and methamphetamine increased dialysate levels of dopamine in mouse striatum; however, the potency and efficacy of sydnocarb was less than methamphetamine. The convulsive effects of cocaine were significantly enhanced by the coadministration of nontoxic doses of methamphetamine but not of sydnocarb. Taken together, the present findings indicate that sydnocarb has psychomotor stimulant effects that are shared by methamphetamine while demonstrating a reduced behavioral toxicity.  (+info)

Electrical and mechanical responses to diltiazem in potassium depolarized myocardium of the guinea pig. (4/1467)

Effects of diltiazem on the electrical and mechanical activities of guinea pig papillary muscle were investigated in K-rich Tyrode's solution (Kc1 12.7 mM). The electrical properties of cell membrane in K-rich solution were also examined in the ventricular muscle fibers. It was found that the overshoot as well as the maximum rate of rise (Vmax) of the action potential were highly sensitive to the extracellular concentration of CaC12 in K-rich solution. Vmax was also affected by NaC1. Diltiazem at a lower concentration (1.1 X 10(-7) M) caused a reduction in the contractile force of K-depolarized papillary muscle without producing significant changes in the resting and action potentials. In the presence of a higher concentration of diltiazem (1.1 X 10(-5) M), the contractile force decreased concurrently with the change in the action potential. Addition of CaC12 restored the original strength of contraction in parallel to the recovery of the action potential, especially in its overshoot and Vmax. From these results, it is inferred that diltiazem may decrease the contractile force of guinea pig papillary muscle either by interfering with the intrasmembrane calcium influx or by intracellularly reducing the free calcium ion concentration in the myoplasm.  (+info)

Vasopressin V2 receptor enhances gain of baroreflex in conscious spontaneously hypertensive rats. (5/1467)

The aim of the present study was to determine the receptor subtype involved in arginine vasopressin (AVP)-induced modulation of baroreflex function in spontaneously hypertensive rats (SHR) and Wistar-Kyoto (WKY) rats using novel nonpeptide AVP V1- and V2-receptor antagonists. Baroreceptor heart rate (HR) reflex was investigated in both SHR and WKY rats which were intravenously administered the selective V1- and V2-receptor antagonists OPC-21268 and OPC-31260, respectively. Baroreflex function was assessed by obtaining alternate pressor and depressor responses to phenylephrine and sodium nitroprusside, respectively, to construct baroreflex curves. In both SHR and WKY rats baroreflex activity was tested before and after intravenous administration of vehicle (20% DMSO), OPC-21268 (10 mg/kg), and OPC-31260 (1 and 10 mg/kg). Vehicle did not significantly alter basal mean arterial pressure (MAP) and HR values or baroreflex function in SHR or WKY rats. The V1-receptor antagonist had no significant effect on resting MAP or HR values or on baroreflex parameters in both groups of rats, although this dose was shown to significantly inhibit the pressor response to AVP (5 ng iv; ANOVA, P < 0.05). In SHR but not WKY rats the V2-receptor antagonist significantly attenuated the gain (or slope) of the baroreflex curve (to 73 +/- 3 and 79 +/- 7% of control for 1 and 10 mg/kg, respectively), although AVP-induced pressor responses were also attenuated with the higher dose of the V2-receptor antagonist. These findings suggest that AVP tonically enhances baroreflex function through a V2 receptor in the SHR.  (+info)

Characteristics of tetrahydroprotoberberines on dopamine D1 and D2 receptors in calf striatum. (6/1467)

AIM: To study the characteristics of tetrahydroprotoberberines (THPB) on dopamine D1 and D2 receptors and elucidate their structure-activity relationship. METHODS: Radioligand assay in vitro with a two-site model program analysis. RESULTS: Four THPB with two hydorxyl groups on C2 and C9 or C2 and C10 exhibited RH and RL two binding sites to D1 receptors and guanosine triphosphate regulated the RH binding site of SPD and THPB-132A in competition assay, while eleven THPB including nonhydroxy-THPB, monohydroxy-THPB, and THPB with two hydroxyl groups attaching to C3 and C10 showed one binding site to D1 receptors under the same conditions. However, the tested eleven THPB all manifested one binding site to D2 receptors in competition assay, and the 2-hydroxy-THPB had the most potent affinity for D2 receptors. CONCLUSION: Dihydroxy-THPB with two hydroxyl groups attaching to C2 and C9 or C2 and C10 possess the intrinsic activity of agonist to D1 receptors, while the other THPB do not. The tested eleven THPB all are the antagonists of D2 receptors.  (+info)

Comparison of two aquaretic drugs (niravoline and OPC-31260) in cirrhotic rats with ascites and water retention. (7/1467)

kappa-Opioid receptor agonists (niravoline) or nonpeptide antidiuretic hormone (ADH) V2 receptor antagonists (OPC-31260) possess aquaretic activity in cirrhosis; however, there is no information concerning the effects induced by the chronic administration of these drugs under this condition. To compare the renal and hormonal effects induced by the long-term oral administration of niravoline, OPC-31260, or vehicle, urine volume, urinary osmolality, sodium excretion, and urinary excretion of aldosterone (ALD) and ADH were measured in basal conditions and for 10 days after the daily oral administration of niravoline, OPC-31260, or vehicle to cirrhotic rats with ascites and water retention. Creatinine clearance, serum osmolality, ADH mRNA expression, and systemic hemodynamics were also measured at the end of the study. Niravoline increased water excretion, peripheral resistance, serum osmolality, and sodium excretion and reduced creatinine clearance, ALD and ADH excretion, and mRNA expression of ADH. OPC-31260 also increased water metabolism and sodium excretion and reduced urinary ALD, although the aquaretic effect was only evident during the first 2 days, and no effects on serum osmolality, renal filtration, and systemic hemodynamics were observed. Therefore, both agents have aquaretic efficacy, but the beneficial therapeutic effects of the long-term oral administration of niravoline are more consistent than those of OPC-31260 in cirrhotic rats with ascites and water retention.  (+info)

G-protein activation by putative antagonists at mutant Thr373Lys alpha2A adrenergic receptors. (8/1467)

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

We read with interest the article by Rimoldi et al [1] describing the increase in central aortic blood pressure (CBP) with ivabradine. The study is significant as it extends observations of attenuated reduction in CBP with beta-blockers compared with peripheral pressure [2] and shows increase in CBP with reduction of heart rate (HR) following 6 months ivabradine treatment. We wish to reconsider some of the findings and concepts in this study in the context that (i) HR values reported in patients treated with ivabradine in the study might benefit from further clarification and (ii) that the degree of relative increase in CBP observed with beta-blockers may potentially be more related to action of beta blockade than to intrinsic reduction of HR. Findings from the study by Rimoldi et al [1] are at variance with other studies investigating changes in central and peripheral pressure with ivabradine. In a recent double-blind, cross-over trial [3], ivabradine was associated with reduction in HR, but no ...
The principal findings of our study in hypertensive patients with stable CAD are that after a follow-up of 6 months, HR lowering with ivabradine was associated with an increase of 11 mm Hg in directly measured central systolic pressure. Further, there was an inverse correlation between the decrease in HR and the increase in central systolic pressure, indicating that the greater the negative chronotropic effect of ivabradine, the greater was the increase in central pressure. Moreover, the HR-lowering effect of ivabradine was associated with an increase in stroke volume without significant changes in cardiac output. Conceivably, the observed increase in central pressure could be because of a ventricular-vascular mismatch or of an increase in stroke volume.17 Under physiological conditions, when there is ventricular-vascular coupling, the reflected pulse wave returns to the left ventricle in diastole and serves to increase coronary perfusion. When HR is slowed down by a negative chronotropic drug, ...
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In the present dose-response study, we investigated short-term effects of tolvaptan on renal tubular function, vasoactive hormones and systemic hemodynamics during basal conditions and during tolvaptan with NO-inhibition in healthy subject. The present study is a continuation and expansion of a previous randomized, double-blinded, placebo-controlled crossover, single-dose study conducted by our laboratory [12].. At baseline, tolvaptan increased renal water excretion dose-dependently up to 30 mg, without affecting sodium excretion. During L-NMMA infusion, tolvaptan decreased water excretion dose-dependently, whereas sodium excretion decreased independently of the dose. In the post infusion period, water excretion remained reduced during all tolvaptan doses, but increased during placebo. Tolvaptan increased sodium excretion to a higher level.. Recent dose-response trials have shown that oral administration of tolvaptan 30 mg led to a fast increase in the effective concentration in plasma. This ...
Our proposal will enable us to study cocaine patients to determine whether varenicline can weaken brain arousal to drug cues in an fMRI imaging setting, which is what we theorize. This supplement supports a pilot imaging study in cocaine dependence. It will evaluate the impact of varenicline on the brain response to ultra-brief drug and comparison cues in an event-related fMRI paradigm. This is a pilot study.. We will additionally examine the impact of varenicline on addiction-relevant behavioral probes of impulsivity, inhibition, attentional and affective bias. The proposed study will provide the first brain-behavioral probes of vareniclines cocaine-relevant actions in humans, and will provide the critical scientific rationale to move the agent into future collaborative clinical trials. ...
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Benazepril, brand name Lotensin (Novartis), is an ACE inhibitor used primarily in treatment of hypertension, congestive heart failure, and heart attacks, and also in preventing the renal and retinal complications of diabetes. ACE inhibitors relax blood vessels, and decrease blood volume, which lowers blood pressure and decreases oxygen demand from the heart. They inhibit angiotensin-converting enzyme, which is part of the renin-angiotensin-aldosterone system. Benazepril is a prodrug which is metabolized by the liver into its active form benazeprilat via cleavage of the drugs ester group. Patients with advanced renal insufficiency taking benazepril show "substantial" kidney benefits. A long-term study of patients kidney disease revealed patients who took benazepril had better kidney function and slower progressions of kidney disease than their peers who took a placebo drug. This is notable because this category of pharmaceuticals has long been thought to cause further kidney damage or increase ...
Ivabradine has been found to reduce admission rates for MI and coronary revascularisation in patients with a heart rate ?70bpm when used in addition to standard care.. The BEAUTIFUL trial was designed to assess the impact of ivabradine on cardiac outcomes in patients with coronary disease and LV dysfunction. The study recruited 10,917 patients from 33 countries, who were randomised to ivabradine or placebo in addition to best medical therapy, which included aspirin, ACE inhibitors and beta-blockers. Patients were followed up for a median of 19 months. The primary endpoint was a composite of cardiovascular death and admission for acute MI or new onset/worsening heart failure.. There was no significant difference in the primary endpoint between the two groups (HR 1.00, 95% CI 0.91-1.1, P=0.94). However, ivabradine did reduce admission rates for MI and coronary revascularisation in a subgroup of patients with a heart rate ? 70bpm at baseline (HR 0.64, 95% CI 0.49-0.84, P=0.001 and HR 0.70, 95% CI ...
Circulation is published on behalf of the American Heart Association, Inc., by Wolters Kluwer. This is an open access article under the terms of the Creative Commons Attribution Non-Commercial-NoDervis License (http://creativecommons.org/licenses/by-nc-nd/3.0/), which permits use, distribution, and reproduction in any medium, provided that the original work is properly cited, the use is noncommercial, and no modifications or adaptations are made ...
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A synthetic route toward tetrahdro-3-benzazepines 1a-f starting with 2a and 2b in modest total yield is described. The facile route was carried by Henry reaction of aldehydes 3a-e with nitroalkanes and NH₄OAc at reflux, reduction of the resulting nitroalkenes 4a-h with LAH at rt followed by protection with K₂CO₃ and PhSO₂Cl at rt, one-pot oxidative cleavage annulation of olefins 5a-h with the one ...
The IUPHAR/BPS Guide to Pharmacology. alsterpaullone ligand page. Quantitative data and detailed annnotation of the targets of licensed and experimental drugs.
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Benazepril: Benazepril belongs to the class of medications called ACE inhibitors. It is used for the treat high blood pressure. It works by relaxing blood vessels and reducing the workload of the heart. Benazepril may be used in addition to diuretics (water pills) known as thiazide diuretics (e.g., hydrochlorothiazide) when one medication has not been found to control blood pressure satisfactorily.
What should I avoid while taking benazepril Lotensin? How to use Benazepril HCL Take this medication by mouth with or without food as directed by your doctor, usually once or twice daily. The absence of a warning for a given drug or drug combination in no way should be construed to indicate that the drug or drug combination is safe, effective or appropriate for any given patient. This medicine is a pink, oblong, scored tablet imprinted with "" and "" and is manufactured by Torrent Pharma, Inc.. Benazepril is used in the treatment of high blood pressure; diabetic kidney disease; heart failure; left ventricular dysfunction and belongs to the drug class Angiotensin Converting Enzyme Inhibitors. ...
· High blood pressure. Benazepril tablets may be taken before, during or after meals, taking foods that do not alter the bioavailability but delaying absorption. Benazepril is administered as a daily intake. Hypertension, essential In the absence of depletion, pre-hydrosodic or renal insufficiency (in common practice): the effective dosage is 10 mg per day in a single dose. | Br|
Procoralan works by affecting your hearts electrical activity in order to slow the heart rate. Ivabradine is used in certain people with chronic heart failure, to help lower the risk of needing to be hospitalized when symptoms get worse. Ivabradine is not for use if you already have heart failure symptoms that recently got worse before starting this medicine. Ivabradine may also be used for purposes not listed in this medication guide.. Generic Procoralan (Ivabradine 5 Mg) # Your Online Doctor @ Help Point Hub. Help Point Hub
Benazepril is an ACE inhibitor that is used to treat high blood pressure (hypertension). Lowering blood pressure may lower your risk of a stroke or heart attack. Benazepril may also be used for purposes not listed in this medication guide.
The Lancet has published the results of the SHIFT study which aimed to assess the effect of heart rate reduction using ivabradine (Procoralan®) in patients with heart failure. The results of this study have been reported in the general media (BBC).. The study recruited and treated 6,505 participants in symptomatic heart failure (NYHA II-IV) with an ejection fraction of 35% or less. They were all in sinus rhythm with a pulse rate of at least 70 beats per minute. Participants were on stable background treatment which included a beta-blocker, if tolerated. Treatment was randomly assigned to ivabradine titrated to a maximum of 7·5 mg twice daily or matching placebo.. The primary outcome of the study was a composite of cardiovascular death or hospital admission for worsening heart failure. Mean follow up was 22.9 months.. 793/3,241 (24%) patients in the ivabradine group and 937/3,264 (29%) of those taking placebo had a primary endpoint event (HR 0·82, 95% CI 0·75-0·90, p,0·0001, NNT ~24). The ...
The study took place from October 2009 through January 2014, with 123 people randomized to varenicline and 125 to placebo. After eliminating people who did not start treatment, the modified intention-to-treat (mITT) analysis included 102 people on varenicline and 111 on placebo. Age averaged 46 in the varenicline arm and 44 in the placebo arm: 83% were men, 73% had an undetectable viral load, and median CD4 count stood at 617. These people had smoked for a median of 25 or 26 years, smoking a median of 20 cigarettes daily. More than 80% of participants had tried to quit at least once ...
Kristi Tinsbloom, Mercer University College of Pharmacy 2015 It is estimated that smoking-related diseases account for 443,000 deaths each year in the United States. There are numerous diseases and conditions that can be caused by smoking including chronic obstructive pulmonary disease (COPD), stroke, coronary heart disease, peptic ulcer disease, and various forms of cancer. Cigarette…
In his editorial, Hays notes that the increased risk of cardiovascular events must be tempered by the rarity of these events (around 1%), and the absolute difference between varenicline and placebo is only 0.24%. He also points out that in most of the studies included in the meta-analysis the rate of participants lost to follow-up was greater in the placebo than the treatment arm, which introduces bias, and that cardiac events were not adjudicated. "These results represent a significant degree of uncertainty about the relative good or harm from varenicline, leaving the issue unsettled," he writes. Commenting on the study for heartwire, Bonow agreed that the absolute cardiovascular risk appeared low. "I dont want to minimize the risks. I think theyre there but they are small. But even if this drug just enables 1 in 10 to give up smoking, I think that is OK, if it avoids the downstream risks associated with smoking ...
... is a prescription medicine that is licensed to help people stop smoking. This article from the eMedTV archives explains how varenicline works, offers general dosing information, and describes the effects of the medication.
Benazepril is used alone or together with other medicines to treat high blood pressure (hypertension). High blood pressure adds to the workload of the heart and arteries. If it continues for a long time, the heart and arteries may not function properly. This can damage the blood vessels of the brain, heart, and kidneys, resulting in a stroke, heart failure, or kidney failure. Lowering blood pressure reduces the risk of strokes and heart attacks. ...
Benazepril (Lotensin) is an oral medication used to treat high blood pressure. Learn about side effects, warnings, dosage, and more.
Varenicline (var-EN-i-kleen) Helps you quit smoking, as part of a support program. Brand Name(s): Chantix, Chantix Starting Month Pak
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A lot will depend on how the situation with the Brexit progresses. The "soft Brexit" option, which involves retention of some form of free trade between the UK and the EU, would be much milder on the pound than its "hard Brexit" alternative. The Bank of England was quite optimistic in its latest projections regarding the UK economy and the course of its monetary policy. However, with no rate cut expectations in the market, it will now be easier for a surprise interest rate reduction or a similar monetary action to affect the pound adversely.. Personally, I believe that GBP/USD has still a long way to parity. Even if it embarks on this way, losing 20% of value in a year without such a disruptive event as the Brexit vote on the horizon, looks improbable to me. I expect GBP/USD stay well above parity in 2017. And how about you?. ...
In a high tech company like ASML, being able to predict future outcomes is very important but also increasingly difficult. The assignment is to develop predictability models to identify improvement opportunities that will result in significant DOA rate reductions.
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Chantix Champix is used to help individuals quit their smoking habit. It contains Varenicline as its main ingredient and used as an anti-smoking agent.
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In this randomized, double-blind, placebo-controlled trial, varenicline was efficacious for smoking cessation among patients with stable CVD. Varenicline more than tripled the tobacco CAR after 12 weeks of treatment compared with placebo. At that point, more than half of the smokers in the varenicline group (54.1%) were tobacco abstinent compared with 18.1% in the placebo group. Although many participants resumed smoking after treatment ended, the superiority of varenicline over placebo was maintained for 1 year. Varenicline was well tolerated and was not associated with increases in cardiovascular events, deaths, blood pressure, or heart rate. Rates of psychiatric AEs, about which concern has been raised in postmarketing surveillance,7,16,17 were low and similar in the varenicline and placebo groups.. The trial results are comparable to those of 2 previous phase III varenicline trials that had very similar protocols but enrolled generally healthy smokers.9,10 In the present trial, the OR for ...
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This is a pilot project using functional magnetic resonance imaging (fMRI) to examine the influence of varenicline on reward processing, cognitive control, and regulation of craving in adolescent smokers. We hypothesize that adolescent smokers receiving varenicline, when compared with those receiving placebo, will have increased activation of the ventral striatum (VS) in response to anticipation of rewards in the Monetary Incentive Delay Task (MIDT), decreased activation of the dorsolateral prefrontal cortex (dlPFC) during exposure to incongruent stimuli in the Stroop task, and reduced activation of the ventral striatum in response to tobacco cues, and increased activation of the dlPFC during regulation of responses to tobacco cues during the Regulation of Craving (ROC) task. The results of this pilot project will have important implications regarding the use of varenicline for treating tobacco dependence and understanding vareniclines neurobiological effects in adolescent smokers ...
Insertion of Allenes into the Pd-C Bond of Ortho-Palladated Primary Arylamines of Biological Relevance: Phenethylamine, Phentermine, (L)-Phenylalanine Methyl Ester, and (L)-Tryptophan Methyl Ester. Synthesis of Tetrahydro-3-benzazepines and Their Salts. García-López, J. A.; Saura-Llamas, I.; McGrady, J. E.; Bautista, D.; Vicente, J. Organometallics 2012, 31, 8333.. http://dx.doi.org/10.1021/om300928j. From Chelate C,N-Cyclopalladated Oximes to C,N,N -, C,N,S-, or C,N,C -Pincer Palladium(II) Complexes by Formation of Oxime Ether Ligands. Abellán-López, A.; Chicote, M. T.; Bautista, D.; Vicente, J. Organometallics 2012, 31, 7434.. http://dx.doi.org/10.1021/om3007213. The First Complexes with Two Metallacycles Fused Around a Common Aryl Substituent: "Akimbo" Complexes. Chicote, M. T.; Vicente-Hernández, I.; Jones, P. G.; Vicente, J. Organometallics 2012, 31, 6252.. http://dx.doi.org/10.1021/om300545k. Reactivity toward CO of Eight-Membered Palladacycles Derived from the Insertion of Alkenes ...
Use of varenicline significantly increased abstinence compared with placebo (39.9% v. 29.1%) 52 weeks after hospital admission for acute coronary syndrome. This finding is important given the substantial reduction in cardiovascular risk conferred by smoking cessation in this high-risk population.1,2,18,19 In addition, rates of serious adverse events (24.5% v. 21.9%) and major adverse cardiovascular events (8.6% v. 9.3%) were similar between varenicline and placebo arms. This suggests that varenicline is safe for use in these patients. However, new strategies for smoking cessation are still needed, given that 60% of smokers who received treatment with varenicline returned to smoking by 1 year after their acute coronary syndrome.. The use of varenicline in the EVITA trial differed in one significant way from the usual method of administration recommended. Typically, patients are instructed to begin taking the drug 8-14 days before a quit date to allow time for titration and bioaccumulation.20 In ...
What is amlodipine and benazepril? Learn about amlodipine and benazepril side effects, how to take amlodipine and benazepril and more.
Methods 120 hospitalised CHF patients were randomly divided into A, B, C (three groups of 40 cases). A group (conventional treatment group) had routine treatment including: oxygen, low-salt diet, rest, cardiac, diuretic and vasodilator; B group (benazepril group) had benazapril combined with the conventional therapy, (Benazepril hydrochloride Plymouth (Lotensin), dose-long l times/day); C group (combined treatment group) were given metoprolol, benazepril and conventional therapy. Metoprolol tartrate was started at 6.25-25 mg 2 times/day, and gradually titrated every 2 weeks up to 25 mg 2 times/day. The three groups were treated for 12 weeks. The parameters assessed in each group before and after treatment included plasma renin activity (PRA), angiotensin II (AgII), endothelin (ET), brain natriuretic peptide (BNP), cardiac functional class and ultrasonic echocardiographic parameters: left ventricular ejection fraction (LVEF), left ventricular fractional shortening (FS), E peak velocity (PEV), E/A ...
Results Of those receiving Ivabradine 52% had HR,65 bpm on arrival in the CT room as compared to only 13% in the ββ group. The final HR in Ivabradine group was significantly lower, as compared to Metoprolol (57.6±3.1 vs 62.1±2.9, p,0.001). Mean % reduction in HR was significantly greater with Ivabradine (32.1% vs 28.1%, p ,0.001). Ivabradine had no significant effect on Systolic or diastolic BP (SBP1, SBP2 135.1±10.2, 134.3+9.1 mm Hg; DBP1, DBP2: 85.1±7, 84.2+6.7 mm Hg, p=ns). Metoprolol demonstrated significant reduction in both SBP and DBP (SBP1, SBP2: 134.3±12.2, 117.1±7.1; DBP1, DBP2: 87.1±6.4, 83.1+3.9, p,0.001 for both).. The need for additional doses of the drug was significantly higher in the ββ group (87% vs 48%, p ,0.01). In the Ivabradine group, 34/100 (34%) required one additional dose and 14/100 patients (14%) required two additional doses to achieve the target HR of ≤65 bpm. In the ββ group, 40/100 patients (40%) required one additional dose while 47/100 patients ...
TY - JOUR. T1 - The Effects of Long-Term Varenicline Administration on Ethanol and Sucrose Seeking and Self-Administration in Male P Rats. AU - Czachowski, Cristine L.. AU - Froehlich, Janice C.. AU - DeLory, Michael. PY - 2018/2/1. Y1 - 2018/2/1. N2 - Background: Varenicline, a partial agonist at α4β2 and full agonist at α7 nicotinic cholinergic receptors, is FDA-approved for treatment of smoking cessation and has been found to reduce alcohol craving in clinical populations. In rodents, varenicline decreases free-choice ethanol (EtOH) intake with somewhat mixed findings in operant paradigms that utilize a combined appetitive/consummatory response. Methods: The present experiment utilized an operant paradigm that procedurally separates appetitive from consummatory responding and a "reward-blocking" approach (i.e., rats were able to consume EtOH during treatment) to better understand the efficacy of varenicline as a treatment for EtOH self-administration and subsequent EtOH seeking. Separate ...
At the University of Massachusetts Medical School, 46% of the 22 member placebo group were still not smoking at 12 weeks compared to 50% for the 22 member varenicline group. Hardly an impressive victory. New Yorks Medical and Behavioral Health Research witnessed 35% of the 17 member placebo group still smoke-free at 12 weeks compared to only 6% of the 16 member varenicline group.. Did counseling sessions at these study sites place greater emphasis on front-end quitting tips such as the importance of stabilizing blood sugar, overcoming time distortion, handling alcohol, understanding elevated blood serum caffeine levels, and recognizing emotional loss? Would doing so have allowed a far greater percentage of placebo group members to successfully navigate the up to three days needed to rid their body of all nicotine and endure the worst of withdrawal?. Did sites generating dismal placebo group rates fail to counsel participants on the fact the reason they could skip meals while still smoking and ...
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There was a 20% reduction in the primary endpoint of cardiovascular mortality, stroke, MI, coronary revascularization, unstable angina, and resuscitation from death in the amlodipine/benazepril arm (9.6%) compared with the HCTZ/benazepril arm (11.8%) (p < 0.001). Cardiovascular death, stroke, and MI were also reduced by 21% (p = 0.002). Fatal and nonfatal MI were significantly reduced in the amlodipine/benazepril arm (2.2%) compared with the HCTZ/benazepril arm (2.8%) (p = 0.04). Other endpoints, including cardiovascular mortality, stroke, and resuscitated sudden death were similar between the two groups. On further analysis, the combination of amlodipine and benazepril was superior to the combination of HCTZ and benazepril for older patients, men and women, and presence or absence of diabetes ...
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Ivabradine is a novel heart rate lowering medicine for the symptomatic management of stable angina pectoralis and symptomatic chronic heart failure. Ivabradine, brand name Corlanor, was approved by the FDA in April 2015 for the treatment of chronic heart failure in patients with an ejection fraction of ≤35%, in sinus rhythm with resting heart rate ≥70 beats per minute, who are not on beta-blockers due to contraindications or already receiving maximum beta-blocker dose. Ivabradine acts by selectively inhibiting the
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TY - JOUR. T1 - Changes in renal function during hospitalization and soon after discharge in patients admitted for worsening heart failure in the placebo group of the EVEREST trial. AU - Blair, John E.A.. AU - Pang, Peter S.. AU - Schrier, Robert W.. AU - Metra, Marco. AU - Traver, Brian. AU - Cook, Thomas. AU - Campia, Umberto. AU - Ambrosy, Andrew. AU - Burnett, John C.. AU - Grinfeld, Liliana. AU - Maggioni, Aldo P.. AU - Swedberg, Karl. AU - Udelson, James E.. AU - Zannad, Faiez. AU - Konstam, Marvin A.. AU - Gheorghiade, Mihai. PY - 2011/10. Y1 - 2011/10. N2 - Aim: To provide an in-depth clinical characterization and analysis of outcomes of the patients hospitalized for heart failure (HF) who subsequently develop worsening renal function (WRF) during hospitalization or soon after discharge. Methods and results: Of the 4133 patients hospitalized with worsening HF and reduced left ventricular ejection fraction (LVEF) (≤40) in the EVEREST trial, 2072 were randomized to tolvaptan, a selective ...
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Varenicline increases the chances of a successful quit attempt by twofold compared with unassisted smoking cessation. However, at the population level, most smokers quit unassisted. The number needed to treat with varenicline for one additional person to successfully quit smoking is estimated to be 10 (95% CI 8-13). Assuming a baseline risk of serious adverse cardiovascular events of 5.57% per year (among smokers with stable cardiovascular disease), the number needed to harm (the number needed to cause one additional serious cardiovascular event) with varenicline is estimated to be 28 (95% CI 13 to 213) per year. The risk of additional serious adverse events associated with varenicline use includes the potential for serious neuropsychiatric symptoms such as depressed mood, agitation and suicidal thoughts ...
Efficacy of Varenicline for Smoking Cessation between Smokers with and without Psychiatric Disorders: A 12-week Observational Study, Han-Ting Wei, Wei-Chen Lin, Ying-Sheue Chen, Yi
This placebo-controlled study assessed the efficacy and respiratory tolerability of ivabradine in patients with chronic obstructive pulmonary disease (COPD) or
Procoralan agisce sullattività elettrica del muscolo cardiaco, rallentando la frequenza del battito. Livabradina è impiegata in specifici soggetti con insufficienza cardiaca cronica, per contribuire a ridurre il rischio di necessità di ricovero a seguito del peggioramento della sintomatologia. Livabradina non è indicata per chi presenta un peggioramento dei sintomi da insufficienza cardiaca già in atto prima di assumere il farmaco. Livabradina può essere impiegata anche per scopi diversi da quelli elencati in questa guida.. Generico Procoralan (Ivabradine 5mg) € 1.13 pillola - Malattie Cardiovascolari @ MyMedsBuy.com - Official Drug Store Online. buy viagra online
Do not drive or operate machinery while taking varenicline if it makes you feel drowsy.. There have been reports of a number of people experiencing feelings of depression and suicidal thoughts after beginning treatment with varenicline. While there is no evidence that these symptoms are directly linked to the medication, if you do feel depressed or have thoughts of suicide, stop taking varenicline immediately as a precaution, and contact your GP.. Nicotine-assisted reduction. If you do not yet feel ready to stop smoking completely, your GP may suggest a method of quitting known as nicotine-assisted reduction to stop. This involves using NRT to progressively reduce the number of cigarettes you smoke, before eventually stopping smoking altogether.. If your GP suggests using nicotine-assisted reduction to stop, you will be prescribed NRT gum or an inhalator to use in between cigarettes. These forms of NRT are best for use between cigarettes because they release a short burst of nicotine rather than ...
Do not drive or operate machinery while taking varenicline if it makes you feel drowsy.. There have been reports of a number of people experiencing feelings of depression and suicidal thoughts after beginning treatment with varenicline. While there is no evidence that these symptoms are directly linked to the medication, if you do feel depressed or have thoughts of suicide, stop taking varenicline immediately as a precaution, and contact your GP.. Nicotine-assisted reduction. If you do not yet feel ready to stop smoking completely, your GP may suggest a method of quitting known as nicotine-assisted reduction to stop. This involves using NRT to progressively reduce the number of cigarettes you smoke, before eventually stopping smoking altogether.. If your GP suggests using nicotine-assisted reduction to stop, you will be prescribed NRT gum or an inhalator to use in between cigarettes. These forms of NRT are best for use between cigarettes because they release a short burst of nicotine rather than ...
Visit your doctor or health care professional for regular checks on your progress. Check your blood pressure as directed. Ask your doctor or health care professional what your blood pressure should be and when you should contact him or her. Call your doctor or health care professional if you notice an irregular or fast heart beat.. You may get drowsy or dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how this drug affects you. Do not stand or sit up quickly, especially if you are an older patient. This reduces the risk of dizzy or fainting spells. Alcohol can make you more drowsy and dizzy. Avoid alcoholic drinks.. If you are going to have surgery, tell your doctor or health care professional that you are taking this medicine.. Women should inform their doctor if they wish to become pregnant or think they might be pregnant. There is a potential for serious side effects to an unborn child. Talk to your health care professional or pharmacist for more ...
Im on a low dose of this stuff, 5/10, and my BP was 106/62 at the doc this morning. He said I probably no longer needed it for BP but I should continue to take it for kidney function since Im diabetic. Im a T2 since 2006 but my last A1c was 5.4 and I havent taken any diabetic meds for over a year...
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This trial will evaluate the factors that contribute to the survival of patients with cirrhosis, particularly an improvement in ascites, with tolvaptan
I smoked for 32 years one pack per day and I took Chantix for a week while still smoking, on the eighth day I stopped smoking. The first week was tough cause the Chantix helps but you have to decide to stop. After withdrawals for 2 weeks I got over the hill and been good since. Next week will be 2 months of being a non smoker. This medicine is worth every penny. I did have some dreams and not nauseated as long as I eat first. Good Luck to everyone. This is doable ...
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Gov't, P.H.S. MeSH Terms 2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine/pharmacology Animals Benzazepines/pharmacology Dopamine Agonists/pharmacology Dopamine Antagonists/pharmacology. Dose-Response Relationship, Drug Eating/drug effects Ergolines/pharmacology Food Deprivation/physiology. Haloperidol/pharmacology Male Naltrexone/pharmacology Quinpirole Rats Rats, Sprague-Dawley Receptors, Dopamine D1/drug effects. Receptors, Dopamine D2/drug effects Substances Benzazepines Dopamine Agonists. Pairing naltrexone with SKF-38393 produced reductions of deprivation-induced intake comparable to that of naltrexone alone. Keywords Food deprivation; Naltrexone; SKF-38393; SCH-23390; Quinpirole; Haloperidol; Opioids; D1 Receptor; D2 Receptor Copyright 1994 Published by Elsevier Inc.. Dopamine Antagonists Ergolines Receptors, Dopamine D1 Receptors, Dopamine D2. Quinpirole Naltrexone 2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine Haloperidol Grant Support DA04194/DA/NIDA NIH ...
AMLODIPINE BESYLATE AND BENAZEPRIL HYDROCHLORIDE - amlodipine besylate and benazepril hydrochloride capsule - Prescription (RX) Marketed Drugs Encyclopedia
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Conivaptan reduces the level of a hormone that regulates the balance of water and salt (sodium) in the body. High levels of this hormone can cause an imbalance that results in low sodium levels and fluid retention. Conivaptan is used to treat hyponatremia (low sodium levels). Conivaptan improves urine flow without...
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New data on ivabradine suggested it could cut death rates by up to 39 per cent, while experts said it could prevent between 5,000 and 10,000 deaths a year. The drug was also found to reduce the need for patients to be treated in hospital for heart failure, which affects about 900,000 people in Britain, by 30 per cent. The drug has been approved by European regulators but has yet to be assessed for widespread use on the NHS. It costs £1.40 a day and is already prescribed for patients in this country with angina. Data published today suggested ivabradine, also known as Procoralan, could reduce the risk of death from heart failure by 39 per cent. It could reduce the risk of death from all types of cardiovascular disease by 17 per cent and the risk of death from all causes by 17 per cent. In addition, the drug, which slows down the heart rate, was found to cut the risk of heart failure patients requiring treatment by 30 per cent. The study involved 6,505 people in 37 countries, including Britain ...
Other names: bradycardia, slowing the heartbeat, heart rate reduction Normal heart rate is very individual, an adult at rest should range between about 60 to 80 beats per minute. Lower heart rate, especially in a state of mental and physical relaxation and sleep, is common in trained athletes. A slow heart rate (bradycardia) speak if its rate is less than 60 / min. Can be a symptom of central nervous system: intracranial hemorrhage, increased intracranial pressure, or stroke; It is also a symptom of cardiac conduction disorders (rhythm is poorly transferred from the atria to the ventricles or the heart is controlled by signals generated in the chambers in the atria). Slow heart rate is also a symptom of poisoning by certain drugs (digitalis and soothing drugs) warfare agents and some animal and plant poisons. The culprit may be decreased thyroid function. If there are other signs present, it is not necessary to visit the doctor. To visit the practitioner to decide if you have extra fatigue,
The pharmacokinetic properties of ivabradine have previously been described.63 It is rapidly absorbed (tmax=0.75-1.5 hours) with a bioavailability of 37% to 49%. Ivabradine has extensive tissue distribution with 70% protein binding. It is extensively metabolized by the cytochrome P450 3A4 into several metabolites, including the N-demethylated derivate, which is the major active metabolite. The elimination process occurs by both fecal and urinary pathways. The main half-life of ivabradine is 2 hours, whereas that of its N-demethylated metabolite is 13 hours.. In vitro, ivabradine reduces the spontaneous beating rate in an isolated SAN cell from rabbit using patch clamp technique (see Figure 3).64 In patch-clamp experiments, ivabradine has been shown to block the pacemaker current of isolated SAN cells of rabbits in the low-micromolar range, with minimal or no effects on other potassium and calcium currents.65,66 In a study of healthy volunteers assessing the correlation between bradycardic ...
All current inhibitors of HIV proteases that are used in clinical treatment of AIDS are targeted against dimeric form of protease. Retrovirus M-PMV infects rhesus monkeys and causes simian immunodeficiency syndrom (SAIDS). This virus is an excellent model for investigation of many processes in retroviruses and for development of new drugs against retroviruses. Our previous biochemical and NMR studies have indicated that in the absence of substrate or inhibitors M-PMV PR should fold into a stable monomer. For solution of crystal structure we prepared a protease mutant, which enabled to prepare a highly concentrated sample for crystallography. However, crystallographers in Poznan could not solve the structure by available molecular replacement and Rosetta programmes. A solution was finally obtained, after several years of experiments, by players of the online game FoldIt who were able to generate model of sufficient quality for successful molecular replacement and subsequent structure ...
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Benazepril 10mg (Benace) is an ACE inhibitor used to controll high blood pressure (hypertension). Controlling high blood pressure is important, but many people find they need the assistance of medication to make it happen. Benazepril is one of the medications that many people respond well to. It is an ACE inhibitor and it helps to reduce various elements in the body that cause high blood pressure. Without them in the way, the blood is once again able to successfully flow through the blood vessels like it should ...
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Tolvaptan hyponatremia (low blood sodium level) drug molecule. Atoms are represented as spheres and are colour coded: hydrogen (white), carbon (grey), oxygen (red), nitrogen (blue), chlorine (green). Illustration. - Stock Image F012/9371
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During the early phases (phases 1 and 2), researchers assess safety, side effects, optimal dosages and risks/benefits. In the later phase (phase 3), researchers study whether the treatment works better than the current standard therapy. They also compare the safety of the new treatment with that of current treatments. Phase 3 trials include large numbers of people to make sure that the result is valid. There are also less common very early (phase 0) and later (phase 4) phases. Phase 0 trials are small trials that help researchers decide if a new agent should be tested in a phase 1 trial. Phase 4 trials look at long-term safety and effectiveness, after a new treatment has been approved and is on the market. ...
... Systematic (IUPAC) name 8-chloro-2-(4-hydroxyphenyl)- 4-azabicyclo[5.4.0] undeca-7,9,11-triene-9,10-diol Identifiers CAS number
Belviq (Lorcaserin) is an anorectic medication manufactured by Arena Pharmaceuticals for the long-term management of obesity. As of 2012, the FDA approve
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Title: Lotrel (amlodipine and benazepril)Category: MedicationsCreated: 12/31/1997 12:00:00 AMLast Editorial Review: 9/26/2016 12:00:00 AM (Source: MedicineNet High Blood Pressure General ...
* found in: Z-1,2-diaminoethane·HCl ; |/= 99% (HPLC), Zirconium aluminide, 99% (metals basis), Zinc oxide, 99.9% (metals basis), SIGMA Zatebradine..
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БЕРЛИН - На наших глазах происходят глубинные изменения в механизмах мировой экономики. Растет скорость и интенсивность глобализации, дигитализации, и в результате, все больше и больше экономических процессов приобретают интернациональный характер. Как следствие, все больше компаний адаптируют свою структуру не только к местному, но и к зарубежному налоговому законодательству, к различным правовым системам. Благодаря техническим достижениям цифровой экономики компании могут обслуживать зарубежные рынки, даже не имея там физического ...
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Coronary artery disease and heart failure are both highly prevalent diseases with a global prevalence of 93 million and 40 million. These patients are at increased risk of morbidity and mortality. The management of these patients involves medical therapy, and both diseases can be treated using the heart rate-lowering drug ivabradine. However, the evidence regarding the use of ivabradine in the treatment of coronary artery disease and/or heart failure is unclear. Our objective is to assess the beneficial and harmful effects of ivabradine in the treatment of coronary artery disease and/or heart failure. This protocol for a systematic review was undertaken using the recommendations of The Cochrane Collaboration, the Preferred Reporting Items for Systematic Reviews and Meta-Analysis Protocols (PRISMA-P), and the eight-step assessment procedure suggested by Jakobsen and colleagues. We plan to include all relevant randomised clinical trials assessing the use of ivabradine in the treatment of coronary artery
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... mesylate (Corlopam) is a drug and synthetic benzazepine derivative which acts as a selective D1 receptor partial ... RS)-6-chloro-1-(4-hydroxyphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol ...
... (INN), also known as captodiamine, is an antihistamine sold under the trade names Covatine, Covatix, and Suvren which is used as a sedative and anxiolytic. The structure is related to diphenhydramine.[1] A 2004 study suggested captodiame may be helpful in preventing benzodiazepine withdrawal syndrome in people discontinuing benzodiazepine treatment.[1] In addition to its actions as an antihistamine, captodiamine has been found to act as a 5-HT2C receptor antagonist and σ1 receptor and D3 receptor agonist.[2] It produces antidepressant-like effects in rats.[2] However, captodiamine is unique among antidepressant-like drugs in that it increases brain-derived neurotrophic factor (BDNF) levels in the hypothalamus but not in the frontal cortex or hippocampus.[2] This unique action may be related to its ability to attenuate stress-induced anhedonia and corticotropin-releasing factor (CRF) signaling in the hypothalamus.[2] ...
The hormone prolactin stimulates lactation (production of breast milk). Dopamine, released by the hypothalamus stops the release of prolactin from the pituitary gland. Domperidone, by acting as an anti-dopaminergic agent, results in increased prolactin secretion, and thus promotes lactation (that is, it is a galactogogue). In some nations, including Australia, domperidone is used off-label, based on uncertain and anecdotal evidence of its usefulness, as a therapy for mothers who are having difficulty breastfeeding.[24][25] In the United States, domperidone is not approved for this or any other use.[26][27] A study called the EMPOWER trial was designed to assess the effectiveness and safety of domperidone in assisting mothers of preterm babies to supply breast milk for their infants.[28] The study randomized 90 mothers of preterm babies to receive either domperidone 10 mg orally three times daily for 28 days (Group A) or placebo 10 mg orally three times daily for 14 days followed by domperidone ...
InChI=1S/C18H22F2N4O/c19-15-5-3-14(4-6-15)17(25)2-1-7-23-8-10-24(11-9-23)18-21-12-16(20)13-22-18/h3-6,12-13,17,25H,1-2,7-11H2 ...
Djaldetti Ruth; Giladi Nir; Hassin-Baer Sharon; Shabtai Hertzel; Melamed Eldad (November-December 2003). "Pharmacokinetics of Etilevodopa Compared to Levodopa in Patient's With Parkinson's Disease: An Open-label, Randomized, Crossover Study". Clinical Neuropharmacology. 26 (6): 322-326. doi:10.1097/00002826-200311000-00012. PMID 14646613 ...
... has also been found to increase the analgesic effects of opioid drugs in a dose-dependent manner, in contrast to 5-HT1A agonists such as 8-OH-DPAT which were found to reduce opioid analgesia.[22][23] However, since 5-HT1A agonists were also found to reduce opioid-induced respiratory depression and WAY-100635 was found to block this effect,[24] it is likely that 5-HT1A antagonists might worsen this side effect of opioids. Paradoxically, chronic administration of the very high efficacy 5-HT1A agonist befiradol results in potent analgesia following an initial period of hyperalgesia, an effect most likely linked to desensitisation and/or downregulation of 5-HT1A receptors (i.e. analogous to a 5-HT1A antagonist-like effect).[25][26][27] As with other 5-HT1A silent antagonists such as UH-301 and robalzotan, WAY 100635 can also induce a head-twitch response in rodents.[28] ...
Melis MR, Succu S, Sanna F, Melis T, Mascia MS, Enguehard-Gueiffier C, Hubner H, Gmeiner P, Gueiffier A, Argiolas A (October 2006). "PIP3EA and PD-168077, two selective dopamine D4 receptor agonists, induce penile erection in male rats: site and mechanism of action in the brain". The European Journal of Neuroscience. 24 (7): 2021-30. doi:10.1111/j.1460-9568.2006.05043.x. PMID 17067298 ...
The present meta-analysis was conducted to estimate the magnitude of the effects of methylphenidate and amphetamine on cognitive functions central to academic and occupational functioning, including inhibitory control, working memory, short-term episodic memory, and delayed episodic memory. In addition, we examined the evidence for publication bias. Forty-eight studies (total of 1,409 participants) were included in the analyses. We found evidence for small but significant stimulant enhancement effects on inhibitory control and short-term episodic memory. Small effects on working memory reached significance, based on one of our two analytical approaches. Effects on delayed episodic memory were medium in size. However, because the effects on long-term and working memory were qualified by evidence for publication bias, we conclude that the effect of amphetamine and methylphenidate on the examined facets of healthy cognition is probably modest overall. In some situations, a small advantage may be ...
Most frequent side effects are nausea, orthostatic hypotension, headaches, and vomiting through stimulation of the brainstem vomiting centre.[9] Vasospasms with serious consequences such as myocardial infarction and stroke that have been reported in connection with the puerperium, appear to be extremely rare events.[10] Peripheral vasospasm (of the fingers or toes) can cause Raynaud's Phenomenon. Bromocriptine use has been anecdotally associated with causing or worsening psychotic symptoms (its mechanism is in opposition of most antipsychotics, whose mechanisms generally block dopamine).[11] Pulmonary fibrosis has been reported when bromocriptine was used in high doses for the treatment of Parkinson's disease.[12] Use to suppress milk production after childbirth was reviewed in 2014 and it was concluded that in this context a causal association with serious cardiovascular, neurological or psychiatric events could not be excluded with an overall incidence rate estimated to range between 0.005% ...
... (Serentil) is a piperidine neuroleptic drug belonging to the class of drugs called phenothiazines, used in the treatment of schizophrenia. It is a metabolite of thioridazine. The drug's name is derived from the methylsulfoxy and piperidine functional groups in its chemical structure. It has central antiadrenergic, antidopaminergic, antiserotonergic and weak muscarinic anticholinergic effects. Serious side effects include akathisia, tardive dyskinesia and the potentially fatal neuroleptic malignant syndrome. Mesoridazine was withdrawn from the United States market in 2004 due to dangerous side effects, namely irregular heart beat and QT-prolongation of the electrocardiogram.[1] It currently appears to be unavailable worldwide. ...
InChI=1S/C25H29N3O2/c1-27-14-18(13-26-25(29)30-16-17-7-4-3-5-8-17)11-21-20-9-6-10-22-24(20)19(12-23(21)27)15-28(22)2/h3-10,15,18,21,23H,11-14,16H2,1-2H3,(H,26,29)/t18-,21+,23+/m0/s1 ...
... (MDPPP) is a stimulant designer drug. It was sold in Germany in the late 1990s and early 2000s as an ingredient in imitation ecstasy (MDMA) pills.[1] It shares a similar chemical structure with α-PPP and MDPV,[2][3][4] and has been shown to have reinforcing effects in rats.[5] ...
... is a synthetic compound that acts as a selective antagonist on D2 dopamine receptors.[1] Its selectivity to the cerebral D2 receptors is characterized by its respective Ki-values, which are as follows: 1.8, 3.5, 2400 and 18000 nM for D2, D3, D4 and D1 receptors respectively. It can be radiolabelled with radioisotopes, e.g. 3H or 11C and used as a tracer for in vitro imaging (autoradiography) as well as in vivo imaging positron emission tomography (PET). Images obtained by cerebral PET scanning (e.g. PET/CT or PET/MRI) allow the non-invasive assessment of the binding capacity of the cerebral D2 dopamine receptor, which can be useful for the diagnosis of movement disorders. In particular, cerebral D2 receptor binding as measured by carbon-11-raclopride (11C-raclopride) has shown to reflect disease severity of Huntington's disease, a genetical disease characterized by selective degeneration of cerebral D2 receptors.[2] Other studies have investigated the relationship of D2 receptor ...
In 1960 the Austrian biochemist Oleh Hornykiewicz, while at the University of Vienna, examined results of autopsies of patients who had died with Parkinson's disease. He suggested that the disease was associated with, or caused by, a reduction in the levels of dopamine in the basal ganglia of the brain. Since dopamine itself did not enter the brain, he tried treating twenty patients with a racemic mixture of dihydroxyphenylalanine (DOPA), which could enter the brain and be converted there to dopamine by the action of DOPA decarboxylase. His results were positive, as were those of another trial in Montreal run by André Barbeau. Unfortunately, other investigators were unable to replicate these early results, and the use of DOPA remained in question until 1967, when George Cotzias at the Brookhaven National Laboratories in Upton, New York, used megadoses of DOPA, up to 16 grams per day. Not long after these results became known, Curt Porter at Merck showed that L-DOPA was the active stereoisomer, ...
InChI=1S/C20H33N3O3S/c1-4-10-22-14-17(21-27(25,26)23(5-2)6-3)11-16-12-18-15(13-19(16)22)8-7-9-20(18)24/h7-9,16-17,19,21,24H,4-6,10-14H2,1-3H3/t16-,17+,19-/m1/s1 ...
... crosses the protective blood-brain barrier, whereas dopamine itself cannot. Thus, L-DOPA is used to increase dopamine concentrations in the treatment of Parkinson's disease and dopamine-responsive dystonia. This treatment was made practical and proven clinically by George Cotzias and his coworkers, for which they won the 1969 Lasker Prize.[4][5] Once L-DOPA has entered the central nervous system, it is converted into dopamine by the enzyme aromatic L-amino acid decarboxylase, also known as DOPA decarboxylase. Pyridoxal phosphate (vitamin B6) is a required cofactor in this reaction, and may occasionally be administered along with L-DOPA, usually in the form of pyridoxine.. Besides the central nervous system, L-DOPA is also converted into dopamine from within the peripheral nervous system. Excessive peripheral dopamine signaling causes many of the adverse side effects seen with sole L-DOPA administration. To bypass these effects, it is standard clinical practice to coadminister (with ...
For azepine, benzazepine is the preferred name. Likewise, the compounds with two benzene rings fused to the central heterocycle ...
Adamantanes: Amantadine • Memantine • Rimantadine; Aminotetralins: 7-OH-DPAT • 8-OH-PBZI • Rotigotine • UH-232; Benzazepines: 6 ...
Azepane Benzazepines Diazepine Oxepin Borepin. ...
Adamantanes: Amantadine • Memantine • Rimantadine Aminotetralins: 7-OH-DPAT • 8-OH-PBZI • Rotigotine • UH-232 Benzazepines: 6- ...
Azepine Benzazepines Diazepine Oxepin Borepin CR gas(dibenzoxazepine). ...
Benzazepine Dibenzothiazepine Dibenzothiepin Dibenzoxepin Yagiela, John; Dowd, Frank; Johnson, Bart; Mariotti, Angelo; Neidle, ...
Benzazepine derivatives SCH-23,390 - 100-fold selectivity for D1 over D5 SKF-83,959 - 7-fold selectivity for D1 over D5 with ... Some of the benzazepines have high intrinsic activity whereas others do not. In 2015 the first positive allosteric modulator ... the D5 receptor, but the benzazepines generally are more selective for the D1 and D5 receptors versus the D2-like family. ... To date, most of the known ligands are based on dihydrexidine or the prototypical benzazepine partial agonist SKF-38393 (one ...
Treatment of these compounds with TBAF invokes a ring-expansion that provides the corresponding benzazepines. One variation of ... "Tetrahydroquinolines and Benzazepines through Catalytic Diastereoselective Formal [4 + 2]-Cycloaddition Reactions between Donor ...
5-tetrahydro-1H-3-benzazepines". J Het Chem. 9 (3): 609-616. Alexander Shulgin; Tania Manning; Paul F Daley (2011). The Shulgin ...
Mesoridazine (Serentil) is a piperidine neuroleptic drug belonging to the class of drugs called phenothiazines, used in the treatment of schizophrenia. It is a metabolite of thioridazine. The drugs name is derived from the methylsulfoxy and piperidine functional groups in its chemical structure. It has central antiadrenergic, antidopaminergic, antiserotonergic and weak muscarinic anticholinergic effects. Serious side effects include akathisia, tardive dyskinesia and the potentially fatal neuroleptic malignant syndrome. Mesoridazine was withdrawn from the United States market in 2004 due to dangerous side effects, namely irregular heart beat and QT-prolongation of the electrocardiogram.[1] It currently appears to be unavailable worldwide. ...
Benzazepines are heterocyclic chemical compounds consisting of a benzene ring fused to an azepine ring. Examples include: ... Benazepril Fenoldopam GSK-189,254 Ivabradine Lorcaserin Semagacestat Varenicline Benzodiazepine Dibenzazepine Benzazepines at ...
"Benzazepines" is a descriptor in the National Library of Medicines controlled vocabulary thesaurus, MeSH (Medical Subject ... This graph shows the total number of publications written about "Benzazepines" by people in Harvard Catalyst Profiles by year, ... Below are the most recent publications written about "Benzazepines" by people in Profiles. ... and whether "Benzazepines" was a major or minor topic of these publication. ...
2,3,4,5-Tetrahydro-1,5-methano-1H-3-benzazepine is a drug originally researched as a potential opioid analgesic, but was found ... 5-methano-1H-3-benzazepine, it seems unlikely that this is actually the compound being sold. Corey lactone 4-phenylbenzoate ... 5-methano-1H-3-benzazepines". Journal of Medicinal Chemistry. 22 (4): 455-7. doi:10.1021/jm00190a020. PMID 430484. Singer, R. A ... 5-methano-1H-3-benzazepine via Oxidative Cleavage and Reductive Amination Strategies". Synthesis. 2004 (11): 1755. doi:10.1055/ ...
5-tetrahydro-1H-2-benzazepine hydrochloride; CAS Number: 1803609-55-3; find Enamine-ENA410542800 MSDS, related peer-reviewed ... Home > ENA410542800 6-bromo-2,3,4,5-tetrahydro-1H-2-benzazepine hydrochloride ...
A H2SO4-mediated intramolecular cyclization enables the preparation of biologically important tetrahydro-1-benzazepines from N- ... of Tetrahydro-1-benzazepines. Hua-Shuai Gao, Fei Dou, Ai-Li Zhang, Rui Sun, Li-Ming Zhao*. *School of Chemistry and Chemical ...
Whereas indolo[3,2-d]benzazepine derivatives L 3 and L 4 show the strongest absorption at about 230 nm, the indolo[3,2-c] ... 1), the indolo[3,2-d]benzazepine main skeleton contains one sp 3-hybridized carbon atom, i.e., the methylene group of the seven ... Osmium indolo[3,2-d]benzazepine complex 11 and metal-free indolobenzazepine L 4 show a certain intercalating capacity, which ... A number of ruthenium(II) arene and osmium(II) arene complexes with indolo[3,2-c]quinolines and indolo[3,2-d]benzazepines have ...
Home >> Chemical Listing >> D >> 10,11-Dihydro-N-(2-hydroxyethyl)-N-methyl-5H-pyrido[2,3-c][2]benzazepine-10-carboxamide ... 10,11-Dihydro-N-(2-hydroxyethyl)-N-methyl-5H-pyrido[2,3-c][2]benzazepine-10-carboxamide [1071504-81-8] ... List of Reports Available for 10,11-Dihydro-N-(2-hydroxyethyl)-N-methyl-5H-pyrido[2,3-c][2]benzazepine-10-carboxamide ... Complete supplier list of 10,11-Dihydro-N-(2-hydroxyethyl)-N-methyl-5H-pyrido[2,3-c][2]benzazepine-10-carboxamide. ...
The present experiments employed in vivo microdialysis to further examine the ability of widely used benzazepine-class D1 ... The present data suggest that the ability of intrastriatally applied benzazepine-class D1 agonists to decrease striatal ... The present experiments employed in vivo microdialysis to further examine the ability of widely used benzazepine-class D1 ... Decreased striatal dopamine efflux after intrastriatal application of benzazepine-class D1 agonists is not mediated via ...
1H-1-Benzazepine-1-acetic acid, 3-[[(1S)-1-(ethoxycarbonyl)-3-phenylpropyl]amino]-2,3,4,5-tetrahydro-2-oxo-, (3S)- ... CA Index Name: 1H-1-Benzazepine-1-acetic acid, 3-[[(1S)-1-(ethoxycarbonyl)-3-phenylpropyl]amino]-2,3,4,5-tetrahydro-2-oxo-, (3S ...
benzazepine-4-acetate. A mixture of methyl (±)-8-(3-amino-l-propyloxy)-3-oxo-2,3,4,5-tetrahydro-lH-2-benzazepine-4-acetate ... benzazepine-4-acetate for the methyl (±)-8-[3-[2-(N-oxopyridyl)amino]-l-propyloxy]-3-oxo-2,3,4,5-tetrahydro-2-benzazepine-4- ... lH-2-benzazepine-4-acetate for the methyl (±)-8-hydroxy-3-oxo-2,34,5-tetrahydro-lH-2-benzazepine-4-acetate, the tile compound ... 5-tetrahydro-2-benzazepine-4-acetate. Methyl (±)-8-methoxy-3-oxo-2-(2,2,2-trifluoroethyl)-2,3,4,5-tetrahydro-2-benzazepine-4- ...
Fenoldopam mesylate (Corlopam) is a drug and synthetic benzazepine derivative which acts as a selective D1 receptor partial ... RS)-6-chloro-1-(4-hydroxyphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol ...
Captodiame (INN), also known as captodiamine, is an antihistamine sold under the trade names Covatine, Covatix, and Suvren which is used as a sedative and anxiolytic. The structure is related to diphenhydramine.[1] A 2004 study suggested captodiame may be helpful in preventing benzodiazepine withdrawal syndrome in people discontinuing benzodiazepine treatment.[1] In addition to its actions as an antihistamine, captodiamine has been found to act as a 5-HT2C receptor antagonist and σ1 receptor and D3 receptor agonist.[2] It produces antidepressant-like effects in rats.[2] However, captodiamine is unique among antidepressant-like drugs in that it increases brain-derived neurotrophic factor (BDNF) levels in the hypothalamus but not in the frontal cortex or hippocampus.[2] This unique action may be related to its ability to attenuate stress-induced anhedonia and corticotropin-releasing factor (CRF) signaling in the hypothalamus.[2] ...
The hormone prolactin stimulates lactation (production of breast milk). Dopamine, released by the hypothalamus stops the release of prolactin from the pituitary gland. Domperidone, by acting as an anti-dopaminergic agent, results in increased prolactin secretion, and thus promotes lactation (that is, it is a galactogogue). In some nations, including Australia, domperidone is used off-label, based on uncertain and anecdotal evidence of its usefulness, as a therapy for mothers who are having difficulty breastfeeding.[24][25] In the United States, domperidone is not approved for this or any other use.[26][27] A study called the EMPOWER trial was designed to assess the effectiveness and safety of domperidone in assisting mothers of preterm babies to supply breast milk for their infants.[28] The study randomized 90 mothers of preterm babies to receive either domperidone 10 mg orally three times daily for 28 days (Group A) or placebo 10 mg orally three times daily for 14 days followed by domperidone ...
InChI=1S/C18H22F2N4O/c19-15-5-3-14(4-6-15)17(25)2-1-7-23-8-10-24(11-9-23)18-21-12-16(20)13-22-18/h3-6,12-13,17,25H,1-2,7-11H2 ...
Djaldetti Ruth; Giladi Nir; Hassin-Baer Sharon; Shabtai Hertzel; Melamed Eldad (November-December 2003). "Pharmacokinetics of Etilevodopa Compared to Levodopa in Patients With Parkinsons Disease: An Open-label, Randomized, Crossover Study". Clinical Neuropharmacology. 26 (6): 322-326. doi:10.1097/00002826-200311000-00012. PMID 14646613 ...
WAY-100635 has also been found to increase the analgesic effects of opioid drugs in a dose-dependent manner, in contrast to 5-HT1A agonists such as 8-OH-DPAT which were found to reduce opioid analgesia.[22][23] However, since 5-HT1A agonists were also found to reduce opioid-induced respiratory depression and WAY-100635 was found to block this effect,[24] it is likely that 5-HT1A antagonists might worsen this side effect of opioids. Paradoxically, chronic administration of the very high efficacy 5-HT1A agonist befiradol results in potent analgesia following an initial period of hyperalgesia, an effect most likely linked to desensitisation and/or downregulation of 5-HT1A receptors (i.e. analogous to a 5-HT1A antagonist-like effect).[25][26][27] As with other 5-HT1A silent antagonists such as UH-301 and robalzotan, WAY 100635 can also induce a head-twitch response in rodents.[28] ...
Melis MR, Succu S, Sanna F, Melis T, Mascia MS, Enguehard-Gueiffier C, Hubner H, Gmeiner P, Gueiffier A, Argiolas A (October 2006). "PIP3EA and PD-168077, two selective dopamine D4 receptor agonists, induce penile erection in male rats: site and mechanism of action in the brain". The European Journal of Neuroscience. 24 (7): 2021-30. doi:10.1111/j.1460-9568.2006.05043.x. PMID 17067298 ...
The present meta-analysis was conducted to estimate the magnitude of the effects of methylphenidate and amphetamine on cognitive functions central to academic and occupational functioning, including inhibitory control, working memory, short-term episodic memory, and delayed episodic memory. In addition, we examined the evidence for publication bias. Forty-eight studies (total of 1,409 participants) were included in the analyses. We found evidence for small but significant stimulant enhancement effects on inhibitory control and short-term episodic memory. Small effects on working memory reached significance, based on one of our two analytical approaches. Effects on delayed episodic memory were medium in size. However, because the effects on long-term and working memory were qualified by evidence for publication bias, we conclude that the effect of amphetamine and methylphenidate on the examined facets of healthy cognition is probably modest overall. In some situations, a small advantage may be ...
Most frequent side effects are nausea, orthostatic hypotension, headaches, and vomiting through stimulation of the brainstem vomiting centre.[9] Vasospasms with serious consequences such as myocardial infarction and stroke that have been reported in connection with the puerperium, appear to be extremely rare events.[10] Peripheral vasospasm (of the fingers or toes) can cause Raynauds Phenomenon. Bromocriptine use has been anecdotally associated with causing or worsening psychotic symptoms (its mechanism is in opposition of most antipsychotics, whose mechanisms generally block dopamine).[11] Pulmonary fibrosis has been reported when bromocriptine was used in high doses for the treatment of Parkinsons disease.[12] Use to suppress milk production after childbirth was reviewed in 2014 and it was concluded that in this context a causal association with serious cardiovascular, neurological or psychiatric events could not be excluded with an overall incidence rate estimated to range between 0.005% ...
InChI=1S/C25H29N3O2/c1-27-14-18(13-26-25(29)30-16-17-7-4-3-5-8-17)11-21-20-9-6-10-22-24(20)19(12-23(21)27)15-28(22)2/h3-10,15,18,21,23H,11-14,16H2,1-2H3,(H,26,29)/t18-,21+,23+/m0/s1 ...
3,4-Methylenedioxy-α-pyrrolidinopropiophenone (MDPPP) is a stimulant designer drug. It was sold in Germany in the late 1990s and early 2000s as an ingredient in imitation ecstasy (MDMA) pills.[1] It shares a similar chemical structure with α-PPP and MDPV,[2][3][4] and has been shown to have reinforcing effects in rats.[5] ...
Raclopride is a synthetic compound that acts as a selective antagonist on D2 dopamine receptors.[1] Its selectivity to the cerebral D2 receptors is characterized by its respective Ki-values, which are as follows: 1.8, 3.5, 2400 and 18000 nM for D2, D3, D4 and D1 receptors respectively. It can be radiolabelled with radioisotopes, e.g. 3H or 11C and used as a tracer for in vitro imaging (autoradiography) as well as in vivo imaging positron emission tomography (PET). Images obtained by cerebral PET scanning (e.g. PET/CT or PET/MRI) allow the non-invasive assessment of the binding capacity of the cerebral D2 dopamine receptor, which can be useful for the diagnosis of movement disorders. In particular, cerebral D2 receptor binding as measured by carbon-11-raclopride (11C-raclopride) has shown to reflect disease severity of Huntingtons disease, a genetical disease characterized by selective degeneration of cerebral D2 receptors.[2] Other studies have investigated the relationship of D2 receptor ...
In 1960 the Austrian biochemist Oleh Hornykiewicz, while at the University of Vienna, examined results of autopsies of patients who had died with Parkinsons disease. He suggested that the disease was associated with, or caused by, a reduction in the levels of dopamine in the basal ganglia of the brain. Since dopamine itself did not enter the brain, he tried treating twenty patients with a racemic mixture of dihydroxyphenylalanine (DOPA), which could enter the brain and be converted there to dopamine by the action of DOPA decarboxylase. His results were positive, as were those of another trial in Montreal run by André Barbeau. Unfortunately, other investigators were unable to replicate these early results, and the use of DOPA remained in question until 1967, when George Cotzias at the Brookhaven National Laboratories in Upton, New York, used megadoses of DOPA, up to 16 grams per day. Not long after these results became known, Curt Porter at Merck showed that L-DOPA was the active stereoisomer, ...
InChI=1S/C20H33N3O3S/c1-4-10-22-14-17(21-27(25,26)23(5-2)6-3)11-16-12-18-15(13-19(16)22)8-7-9-20(18)24/h7-9,16-17,19,21,24H,4-6,10-14H2,1-3H3/t16-,17+,19-/m1/s1 ...
  • Benzazepines" is a descriptor in the National Library of Medicine's controlled vocabulary thesaurus, MeSH (Medical Subject Headings) . (harvard.edu)
  • Quick MP, Frohlich R, Schepmann D, Wunsch B . Asymmetric synthesis of 3-substituted tetrahydro-2-benzazepines. (uni-muenster.de)
  • Hasebein P, Frehland B, Lehmkuhl K, Frohlich R, Schepmann D, Wunsch B . Synthesis and pharmacological evaluation of like- and unlike-configured tetrahydro-2-benzazepines with the alpha-substituted benzyl moiety in the 5-position. (uni-muenster.de)
  • More recently this chemical compound is claimed to have been sold as a designer drug under the name A3A,[citation needed] but since the anecdotally reported effects of the product sold under this name do not seem to bear any resemblance to the known pharmacology of genuine 2,3,4,5-tetrahydro-1,5-methano-1H-3-benzazepine, it seems unlikely that this is actually the compound being sold. (wikipedia.org)
  • I want to get the latest chemistry news from C&EN in my inbox every week. (acs.org)