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2015 department of medicine research day
2015 department of medicine research day

... Design: This is an open-label, safety, pharmacokinetic (PK), dose-escalation, multicenter study. Rationale: KD019 was originally developed for a solid tumor indication, and is currently being investigated as a cancer treatment. In non-clinical studies, KD019 selectively inhibited key kinases and val ...
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2 receptor

... but it is also unpleasant, and therefore also an emotional experience. Many people report pain in the absence of tissue damage or any likely pathophysiological cause; usually this happens for psychological reasons. There is no way to distinguish their experience from that due to tissue damage, if we ...
5th Lecture 1433
5th Lecture 1433

... Drug-Receptor Bonds and Selectivity  Drugs which bind through weak bonds to their receptors are generally more selective than drugs which bind through very strong bonds  This is because weak bonds require a very precise fit of the drug to its receptor if an interaction is to occur  Only a few re ...
Direct cholinergic agonists
Direct cholinergic agonists

... two main targets of drug action: the postsynaptic receptor and the acetylcholinesterase enzyme, which breaks down acetylcholine. direct-acting cholinergic agonists have a direct action on the receptor for acetylcholine. Some drugs are specific for the muscarinic receptor; others are specific for the ...
THE UNIVERSITY OF AUCKLAND
THE UNIVERSITY OF AUCKLAND

... Full marks could be achieved with either CRA or NCA, depending on how data was interpreted – either was fine, but these two are the most likely. Shifts in the curve needed to be identified and explained. CIA did not achieve full marks because using a method like the one used in this course would not ...
Pharmacology 6 – SNS Antagonists
Pharmacology 6 – SNS Antagonists

... 1. Name common examples of non-selective and selective SNS antagonists and what are they clinically used for. 2. How do SNS antagonists produce their anti-hypertensive effects and what are their side effects. 3. Compare the effects produced by selective and non-selective antagonists, name examples o ...
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A1992HC31200002

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Brief Receptor Theory
Brief Receptor Theory

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ANTIPSYCHOTICS Objectives: After this lecture has been presented
ANTIPSYCHOTICS Objectives: After this lecture has been presented

... 1. clozapine (“Clozaril” – approved by the FDA in 1989, it seems to help those with negative antipsychotic symptoms. This drug poses a risk for agranulocytosis, a potentially life-threatening blood disorder. In addition, a recent retrospective study revealed cardiovascular complications such as myoc ...
How? Morphine is a pain medication of the opiate type which is
How? Morphine is a pain medication of the opiate type which is

... well as 41.2% hydrophobic residues. The dynorphins are found widely distributed in the CNS. Their storage vesicles are larger and more dense and a stronger and prolonged stimulus is needed to cause the large vesicles to release their contents into the synaptic cleft. The dynorphins are found to be e ...
Pharmacodynamics
Pharmacodynamics

Patrick chapter 19 part 2
Patrick chapter 19 part 2

... Steroid acts as a spacer for the quaternary centres (1.09nm) Acyl groups are added to introduce the Ach skeleton Faster onset then tubocurarine but slower than suxamethonium Longer duration of action than suxamethonium (45 min) No effect on blood pressure and fewer side effects © 1 ...
What lessons can we learn from 20 years of chemokine receptor drug discovery?
What lessons can we learn from 20 years of chemokine receptor drug discovery?

... Two hydrophobic pockets - extracellular face of TMI-III TMI III & TMIII TMIII-VII VII Glu283 essential for almost all compound interactions (except TAK-779) Partially overlaps with endogenous ligand binding site 2 ...
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Research and Development of Olopatadine hydrochloride, an

... In terms of chemical structure, olopatadine would be distinguished from the other antiallergic drugs marketed so far. The compound possesses a dimethylamine moiety at the terminal of the side chain and a directly substituted acetic acid moiety on its tricyclic core structure. The introduction of a p ...
THESIS OUTLINE
THESIS OUTLINE

... receptors in cocaine reinforcement. The studies in Chapter 3 were designed to establish the involvement of µ-opioid receptors in cocaine reinforcement, which was determined with acquisition of cocaine self-administration by µ-opioid receptor knockout mice as a measure. It appears from previous studi ...
ADRENERGIC RECEPTORS AS THERAPEUTIC TARGETS
ADRENERGIC RECEPTORS AS THERAPEUTIC TARGETS

... The pharmacodynamic principles that aid in the understanding of adrenergic receptors and the actions of drugs on these receptors. ...
Neurotransmitter Receptors - VCC Library
Neurotransmitter Receptors - VCC Library

Cimetidine - Clemson University
Cimetidine - Clemson University

... • This results in reduction of gastric volume and acidity. It also decreases the amount of gastric acid released in response to other stimuli. ...
Mechanisms of drug action
Mechanisms of drug action

... A lethal dose (LD) is an indication of the lethality of a given substance. Because resistance varies from one individual to another, the 'lethal dose' represents a dose (usually recorded as dose per kilogram of subject body weight) at which a given percentage of subjects will die. Animal-based LD me ...
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... Partial- sub maximal physiological response In the presence of a full agonist a partial agonist behaves like an antagonist. Inverse agonistdecreases the rate of signal transduction ...
Glucocorticoids
Glucocorticoids

... Treatment: anti-steroids (synthesis + receptor), surgery. ...
Drug Action - people.vcu.edu
Drug Action - people.vcu.edu

... marijuana, digitalis, quinine, …………. ...
Pharmacology Objectives 2
Pharmacology Objectives 2

... 3. Give evidence for the existence of drug receptors. i. Drug potency indicates sites of interactions, e.g. LSD. ii. Similar molecules produce similar effects, e.g. norepinephrine & epinephrine. iii. Difference in action of stereoisomers, e.g. dextrophan(-) and levophranol(+). iv. Competitive antago ...
NON-INFECTIOUS DISEASES
NON-INFECTIOUS DISEASES

... Leukotriene antagonists (e.g. montelukast, zafirlukast) Glucocorticosteroids Many available for oral or aeorosol use (AEROSOL: beclamethasone, budesonide. fluticasone, triamcinolone, mometasone, ciclesonide – ORAL: prednisone, methylprednisolone, cortisone) ...
Towards a Molecular Description of the GABA
Towards a Molecular Description of the GABA

... • Structure of drug binding sites and differences in different receptor isoforms are NOT KNOWN, as is the overall receptor structure. • Do know about a homologous protein complex, the nicotinic acetylcholine receptor (does not recognize benzodiazepine). • However, has been studied extensively. Struc ...
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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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