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Bioisosterism: A Rational Approach in Drug Design
Bioisosterism: A Rational Approach in Drug Design

... of Substituted 6-(Dimethylamino)-9-benzyl-9H-purines compound ...
CNS Stimulants
CNS Stimulants

... medulla→↑ BP and HR (harmful in HTN patients) Stimulation of parasympathetic ganglia→↑ motor activity of the bowel At higher doses, BP falls & activating ceases in both GIT and bladder ...
Altered Behavioral Response to Dopamine D3 Receptor Agonists 7
Altered Behavioral Response to Dopamine D3 Receptor Agonists 7

... performed. In the case of comparisons for which we had no a priori reason to believe that the null hypothesis was untrue (eg when comparing pretreatment groups following saline injection for the purpose of demonstrating lack of a measurable difference in conditioned locomotion response or change in ...
Unit 11 Sedative, Hypnotic, Analgesics
Unit 11 Sedative, Hypnotic, Analgesics

... • Radiation Therapy - shrinks solid tumors that may be pressing on nerves • Surgery - reduce pain by removing part of or the entire tumor • Nerve Block - injection of alcohol or other neurotoxic substance into neuronal tissue irreversibly stop impulse transmission along treated nerves ...
7-Skeletal_Muscle_Relaxants modified
7-Skeletal_Muscle_Relaxants modified

... Short acting Intermediate acting Long acting ...
40th Anniversary of Opioid Agonist Pharmacotherapy for
40th Anniversary of Opioid Agonist Pharmacotherapy for

... 1) Initial clinical research on mechanisms and treatment using methadone maintenance pharmacotherapy performed at The Rockefeller Hospital of The Rockefeller Institute for Medical Research by Dole, Nyswander, and Kreek in the winter, spring, and early summer of 1964 (presented at the Association of ...
The Biological Model (Medical)
The Biological Model (Medical)

...  A02 – Varenicline: side effects are common, has been ...
Azoles and Barbiturates
Azoles and Barbiturates

... BARBITURATES Barbiturates are central nervous system depressants. They produce wide spectrum of CNS depression, from mild sedation to coma, and have been used as a sedatives, hypnotics, anesthetics and anticonvulsants. ...
Lecture 1 Dr.fatima Principles in the management of poisoned
Lecture 1 Dr.fatima Principles in the management of poisoned

... when N-acetyl cysteine is indicated as the antidote for acute acetaminophen poisoning, but recent studies reported no significant differences in N-acetyl cysteine serum concentration, peak concentration or half-life when given with activated charcoal. Cathartics Saline cathartics are desired to remo ...
Datasheet - Santa Cruz Biotechnology, Inc.
Datasheet - Santa Cruz Biotechnology, Inc.

... The G protein-coupled receptor TGR5 is a 330 amino acid protein that is almost universally expressed in human tissues including heart, skeletal muscle, spleen, kidney, liver, small intestine, placenta and leukocytes, but not in brain, colon (without mucosa), thymus or lung. TGR5 is sensitive to bile ...
Autonomic Nervous System
Autonomic Nervous System

... of acetylcholine (ACh), as of a result of the inactivity (perhaps even inhibition) of acetylcholinesterase, caused by nerve gas, in patients with myasthenia gravis who have overdosed on cholinergic agents, or in surgical candidates, due to an excess of cholinesterase inhibitor given to reverse surgi ...
Research advances in basic mechanisms of seizures and
Research advances in basic mechanisms of seizures and

... Epilepsy is a common neurological disease but the mechanism of seizure generation has been only partially unraveled. Furthermore, almost 30% of epileptic patients are resistant to pharmacological treatment. Therefore, elucidation of the basic mechanism of seizures and search for new antiepileptics i ...
Why do plants make drugs for humans?
Why do plants make drugs for humans?

... Why would plants make drugs that are used by humans? More specifically, why would plants make drugs at all? Perhaps this may be explained by natural selection. The concept of natural selection was proposed by Charles Darwin in the late 1800’s as a cornerstone of his theory of evolution. The theory o ...
Protein-Ligand Binding
Protein-Ligand Binding

Medications for Alcohol and Drug Dependence
Medications for Alcohol and Drug Dependence

... How Do Methadone and Buprenorphine Reduce Opioid Use? • Both activate the opioid receptors • Buprenorphine’s (unlike methadone’s) effect plateaus at higher doses which accounts for its better safety profile ...
Properties of asymmetric (chiral) molecules
Properties of asymmetric (chiral) molecules

... Examples of differential chiral recognition Carvone is the organic molecule responsible for the smell & taste of both spearmint and caraway. How can it be these very different things? • (R)-carvone enantiomer “is” spearmint • (S)-carvone enantiomer “is” caraway Each enantiomer binds only to one spe ...
Histamine and Antihistaminic Agents
Histamine and Antihistaminic Agents

... these receptors is discussed below. It should be noted that some H1-antagonists also block histamine release. However the concentrations required to do so are considerably greater than those required to produce significant histamine receptor blockade. The H1-antagonists do not block antibody product ...
Angiotensin Receptor Blockers - Advantages of the
Angiotensin Receptor Blockers - Advantages of the

... activation of PPAR gamma resulting in a favourable metabolic profile. Azilsartan is well tolerated; the most common side effects are headache and diarrhea. No cases of hyperkalemia have been reported in 6-week clinical trials. Worsening of renal function and hypotension should be monitored, particul ...
introduction to drug discovery
introduction to drug discovery

... quantitative structure-activity relationship (QSAR), between the two. The mathematical expression can then be used to predict the biological response of other chemical structures. Receptor Most drugs produce their effects by acting on specific protein molecules, usually located in the cell membrane ...
Chapter 11 THC
Chapter 11 THC

... (Marinol) have been used to treat nausea and vomiting associated with chemotherapy in cancer patients. Other potential uses of Dronabinal are to reduce the muscle spasms and pain of multiple sclerosis and reduce the intraocular pressure of glaucoma. Both marijuana and non-psychoactive synthetic cann ...
in vivo
in vivo

... Each DAC™ construct is a fully patentable new chemical entity (NCE) that is composed of three components: A drug component: a peptide or small molecule that is responsible for the biological activity ...
Introduction of two new anaesthetic agents
Introduction of two new anaesthetic agents

... • a2-adrenoceptors: are found in both the central and peripheral nervous system. They are found both pre- and postsynaptically and serve to produce inhibitory functions. • -Presynaptic a2 receptors inhibit the release of noradrenaline and thus serve as an important receptor in the negative feedback ...
CHF Drugs
CHF Drugs

... - chronic hacking dry cough - hyperkalemia - angioneurotic edema (class specific to if you get it on one ACE inhibitor, you’ll get it with all. SE profile occurs in 20 % of all patients. Considerations: Class III & IV HF  hypotension if not monitored properly, which will decrease renal function and ...
Hydrogen Bonding: The Last Mystery in Drug Design?
Hydrogen Bonding: The Last Mystery in Drug Design?

... extensively studied in a series of thermolysin inhibitors (Fig. 6). The replacement of the -NH- group of the ligands by –O– reduces binding affinities by a factor of 1 000, which has been explained by the lack of the NH ··· O = C hydrogen bond and a mutual repulsion of the two electronegative oxygen ...
Zomig Rapimelt
Zomig Rapimelt

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NK1 receptor antagonist

Neurokinin 1 (NK1) antagonists are a novel class of medications that possesses unique antidepressant, anxiolytic, and antiemetic properties. The discovery of neurokinin 1 (NK1) receptor antagonists was a turning point in the prevention of nausea and vomiting associated with cancer chemotherapy.An example of a drug in this class is aprepitant. Chemotherapy-induced emesis appears to consist of acute and delayed phases. So far, the acute phase emesis responds to 5-HT3 antagonists while the delayed phase remains difficult to control. The discovery and development of NK1 receptor antagonists have elicited antiemetic effect in both acute and especially in delayed phases of emesis.The first registered clinical use of NK1 receptor antagonists was the treatment of emesis, associated with cancer chemotherapy.
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