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cAlnOfficial Journalofthe c.AmericanHeart cjlssociation
cAlnOfficial Journalofthe c.AmericanHeart cjlssociation

... biochemical techniques are applied to tissue homogenates, and different standards are frequently used to classify receptors.P 7 After many years of research, two distinct dopamine receptor subtypes, DA, and DA2, were identified conclusively by classical criteria in physiologic preparations.5 DA rece ...
Lecture 3 - Renin Angiotensin Pathway
Lecture 3 - Renin Angiotensin Pathway

... • The renin-angiotensin pathway is integral to controlling blood volume and pressure. Pathway overactivation causes hypertension. • It is controlled by the action of two main enzymes renin and angiotensin-converting enzyme (ACE). • Drugs have been developed as ACE inhibitors, angiotensin II receptor ...
multiple-choice tests in pharmacology
multiple-choice tests in pharmacology

... b) Binding of substances with plasma proteins c) Accumulation of substances in a tissue d) Process of physicochemical and biochemical alteration of a drug in the body 026. Biotransformation of the drugs is to render them: a) Less ionized b) More pharmacologically active c) More lipid soluble d) Less ...
Revisiting AMPA receptors as an antiepileptic drug target
Revisiting AMPA receptors as an antiepileptic drug target

... inhibit calcium influx stimulated by the selective kainate receptor agonist (2S,4R)-4-methylglutamic acid (SYM2081), indicating a weak effect on kainate receptors. To date, perampanel has not been found to interact with other molecular targets, including NMDA receptors, at relevant concentrations. R ...
Revisiting AMPA Receptors as an Antiepileptic Drug Target
Revisiting AMPA Receptors as an Antiepileptic Drug Target

... inhibit calcium influx stimulated by the selective kainate receptor agonist (2S,4R)-4-methylglutamic acid (SYM2081), indicating a weak effect on kainate receptors. To date, perampanel has not been found to interact with other molecular targets, including NMDA receptors, at relevant concentrations. R ...
Mitigation of calcium channel blocker-related oedema
Mitigation of calcium channel blocker-related oedema

... Table 1 shows the rates of oedema from eight relevant clinical trials. Although the incidence of oedema recorded in the CCB monotherapy groups varies widely (range, 4.9–34.4%), the data are consistent in showing lower rates of this side effect in the patients who receive ACEI/CCB or ARB/CCB combinat ...
Sulodexide - Wiley Online Library
Sulodexide - Wiley Online Library

... bound to fibrin or incorporated into the thrombus. In contrast, the inhibition of fibrinbound thrombin by the HCII/DS complex is not impaired (50). In an in vivo study (8), it was determined that pretreatment with heparin, 10 antithrombin units per 1 kg (10 U/kg), inhibited clot formation to the sam ...
Pharm of the Adrenal Cortex
Pharm of the Adrenal Cortex

...  Withdrawal from glucocorticoid treatment – long term glucocorticoid therapy suppresses release of CRH and ACTH  atrophy of adrenal cortex o Abrupt cessation of glucocorticoid treatment  acute adrenal insufficiency o Months are required to reactivate HPA axis and more time may be needed for atrop ...
Pharmacologic Advances in Canine and Feline Reproduction TOPICAL REVIEW
Pharmacologic Advances in Canine and Feline Reproduction TOPICAL REVIEW

... and fertilization and specific changes in the maternal physiology is essential when providing clinical services such as breeding management and determination of gestational time for surgical intervention. Although canine gestational time is consistent with the timing of hormone surges, it is not pre ...
Interactions between antihypertensive drugs and
Interactions between antihypertensive drugs and

... only in undernourished animals.23 However, no studies concerning potential interactions between the drug and food in humans are developed. With respect to beta-blockers, the BA of bevantolol, metoprolol when administered as sustained release form, propranolol when administered as sustained release f ...
Introduction - Wiley-VCH
Introduction - Wiley-VCH

... Huang, now known as Ephedra sinica [9]. The chief active ingredient, ephedrine, is a sympathomimetic amine, and therefore it is clear in this case also that the use of Ma Huang as a stimulant had a rational basis. The ephedrine molecule is simple and contains two chiral centers; the compound from ep ...
New antiarrhythmic agents for atrial fibrillation
New antiarrhythmic agents for atrial fibrillation

... with AF and congestive cardiac failure. Monotherapy is often found to be inadequate in 24 h and exercise-induced heart rate control, whereas combination therapy (e.g., digoxin plus βblocker or rate-limiting calcium antagonist [37]) should be considered as it may be useful not only in achieving satis ...
IDrugs The Investigational Drugs Journal
IDrugs The Investigational Drugs Journal

... with relief lasting up to one year. Bone marrow toxicity was also much less than comparable therapies. Two multi-center, double-blind, randomized clinical trials are currently in progress in 100 prostate cancer patients and 75 patients with osteolytic bone metastases (including breast and lung). Thi ...
Я-Adrenergic Blockade Affects Initial Drug Distribution Due to
Я-Adrenergic Blockade Affects Initial Drug Distribution Due to

... peripheral blood flow distribution on early drug concentration history after rapid intravenous administration (Krejcie et al., 1996a). Using this model in mildly and moderately hypovolemic dogs, we were able to demonstrate that the increase in the area under the drug concentration versus time relati ...
GABA Receptors: Subtypes, Regional Distribution, and Function
GABA Receptors: Subtypes, Regional Distribution, and Function

... amma-aminobutyric acid (GABA) is the most widely distributed inhibitory neurotransmitter in the central nervous system (CNS).1 As such, GABA limits the excitability of neuronal activity in all areas of the brain.2 Excessive GABAergic signaling results in sedation, amnesia, and ataxia, whereas the mi ...
Module 1. General Clinical Pharmacy.Clinical Pharmacy in
Module 1. General Clinical Pharmacy.Clinical Pharmacy in

... B. An often fatal form of arrhythmia characterized by rapid, irregular fibrillar twitching of the ventricles of the heart instead of normal contractions, resulting in a loss of pulse C. The cardiovascular condition in which the heart ability to pump blood weakens D. All of the above E. None of the ...
Management of b-Adrenergic Blocker and Calcium Channel Antagonist Toxicity
Management of b-Adrenergic Blocker and Calcium Channel Antagonist Toxicity

... compromise, many will have abrupt central nervous system depression with loss of airway protective reflexes and require intubation and mechanical ventilation. For patients that present with hallmark bradycardia and hypotension, atropine and normal saline fluid bolus are reasonable initial therapies. I ...
Update on pharmacotherapy for pulmonary hypertension
Update on pharmacotherapy for pulmonary hypertension

... be referred to a specialised PH centre for diagnosis and treatment. Patient education and use of expert centre support are essential for optimal outcomes and minimal side effects using currently available drug treatments (Box 3). Calcium channel blockers There is a small group of patients with iPAH ...
Naloxone fails to produce conditioned place aversion in
Naloxone fails to produce conditioned place aversion in

... DOR is not involved in mediating NLX aversion. The likelihood of an involvement of the DOR in hedonic homeostasis is further reduced given the result of the second experiment in which a high dose of NTD failed to produce a CPA in C57BL/6 mice, a dose that was e¡ective in reducing locomotor activity. ...
Calcium Channel Blocking Agents
Calcium Channel Blocking Agents

... Onset of Action ...
Toxicant – Receptor Interactions: Fundamental - UNC
Toxicant – Receptor Interactions: Fundamental - UNC

... endogenous ligand (antagonist actions). Third, the toxicant may produce allosteric effects on receptors; for example, it has been shown that some toxicants, rather than binding to the same site as endogenous ligands, bind instead to an adjacent part of the macromolecule (see Section 19.2.2 and Figur ...
A new, simple and robust radioligand binding method
A new, simple and robust radioligand binding method

... Kinetic on and off rate constants for many receptor ligands are difficult to determine with regular radioligand binding technique since only few of the ligands are available in labeled form. Here we developed a new and simple radioligand binding method for determining the kinetic off-rate constant fo ...
Angiotensin Converting Enzyme Inhibitors
Angiotensin Converting Enzyme Inhibitors

... By the same token, all ACE inhibitors share a number of potential adverse reactions that are inherent in their mechanism of action. Excessive hypotension is always a possibility, especially in patients with malignant hypertension who may have intense renindependent vasoconstriction, in patients with ...
Hypertensive Disorders of Pregnancy
Hypertensive Disorders of Pregnancy

... sia may involve multiple organs, and many of its nonhypertensive complications can be life-threatening, even when blood pressure elevations are mild. The pathophysiology of preeclampsia can be divided into two stages: alterations in placental perfusion (stage 1) and the maternal syndrome (stage 2) ...
Bioisosterism: A Rational Approach in Drug Design
Bioisosterism: A Rational Approach in Drug Design

... The ability of a group of bioisosteres to elicit similar biological activity has been attributed to common physicochemical properties. In this review an attempt has been made to quantitate, in specific instances, physicochemical effects such as electronegativity, steric size, and lipophilicity and t ...
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Discovery and development of beta-blockers

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