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Introduction-1
Introduction-1

... Excitation(stimulation,兴奋): the body function increase or potentiated by the drug. Adrenaline accelerate the heart rate and output. Acetylcholine contracts the gastrointestinal smooth muscle. These effects are called stimulation. With the dose increase of the drug it may induce augmentation(亢进). For ...
PDF Format, 2,55 Mb - Laboratory of stress and feeding
PDF Format, 2,55 Mb - Laboratory of stress and feeding

... to mood and motivation. Indeed, numerous data accumulated in recent years suggest that the LS integrates sensory stimuli and, according to their relevance and valence, modulates the activity of the brain regions responsible for the direct driving of motivated behavior (such as hypothalamic regions o ...
The impact of pharmacogenetics on the development and use of
The impact of pharmacogenetics on the development and use of

... variety of other receptor actions. Aripiprazole has been recently introduced; as well as having 5-HT2A antagonist effects, it has a unique partial agonist action at the D2 receptor which is thought to be responsible for its lack of acute EPS or hyperprolactinaemia. Like EPS, hyperprolactinaemia, lea ...
Chapter 18
Chapter 18

... respondents aged 15 years and older indicated that they had used an opioid pain reliever, a stimulant, or a sedative or tranquilizer in the past year while 0.3% reported that they used any of these drugs to get high in the past year.  Among Canadians 15 years and older, the prevalence of past-year ...
Brexpiprazole II: Antipsychotic-Like and Procognitive Effects of a
Brexpiprazole II: Antipsychotic-Like and Procognitive Effects of a

... but others with higher D2 intrinsic activity have seen their development discontinued (e.g., bifeprunox; Newman-Tancredi et al., 2007) because of their insufficient clinical efficacy (Casey et al., 2008). A key issue for D2 partial agonism is to determine an optimal level of intrinsic activity (or r ...
A new, simple and robust radioligand binding method
A new, simple and robust radioligand binding method

... liquid and unbound ligand while retaining cells, including bound ligand, attached to the bottom surface. Immediately, 300 μl of binding buffer (including about 2 nM [3H]-RX821002) was added rather forcefully to the cells. Thereby, most of the HEK293 cells became re-suspended, due to that cell attach ...
Chem 491 presentation
Chem 491 presentation

... Harmaline and harmine (dihydroharmine and tetrahydroharmine) found in B. caapi and P. harmala are reversible inhibitors of MAO-A found in the CNS and MAO-B found in the gastrointestinal tract Evidence: clinical trial by McKenna, Towers, and Abbott (1984) Effects:Beta-carbolines from P. harmala alone ...
SERIES ‘‘GENETICS OF ASTHMA AND COPD IN THE POSTGENOME ERA’’
SERIES ‘‘GENETICS OF ASTHMA AND COPD IN THE POSTGENOME ERA’’

... genotypes with nonwild-type (i.e. five) repeat numbers were shown to have reduced levels of transcriptional activity, which might be expected to translate to lower levels of production of 5-lipoxygenase in vivo [5, 19]. The ALOX5 promoter polymorphism does not show an association with asthma suscept ...
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... Class 2: Ionotropic receptors/ion channels - nicotine, alcohol ...
Snyder, Solomon H. - The Tanner Lectures on Human Values
Snyder, Solomon H. - The Tanner Lectures on Human Values

... for various medical purposes, almost all of which depended on its ability to block the actions of the neurotransmitter acetylcholine at various glands and muscles throughout the body. The interaction of acetylcholine with drugs provides an excellent example of both basic and applied science. Atropin ...
Lefkowitz is working on a new kind of heart failure drug “combining
Lefkowitz is working on a new kind of heart failure drug “combining

... clinical trials but the approach is entirely general and could potentially be used on many different seven-transmembrane-spanning receptors.” Another possible application, Lefkowitz remarks, is in the treatment of pain. “The pain relieving effects of opiates appear to be mediated through G protein s ...
Adverse reactions
Adverse reactions

... the mechanism of action of antipsychotic drugs: 1) Mesolimbic-mesocortical pathway: the one most closely related to behavior and psychosis 2) Nigrostriatal pathway: it is involved in the coordination of voluntary movement. Blockade of the D2 receptors in the nigrostriatal pathway is responsible for ...
Recreational Drugs
Recreational Drugs

...  Has anabolic effects (stimulates protein synthesis) and has been used by bodybuilders to aid in fat reduction and muscle building.  Acts on at least 2 sites: o GABA receptor o A specific GHB binding site  Rapidly absorbed, peak concentrations occur within 20-60 minutes.  Most effects fade after ...
New therapeutic targets for ACE inhibitors and angiotensin receptor
New therapeutic targets for ACE inhibitors and angiotensin receptor

... appeared to be less favorable than chlortalidone in Afro-American (RR = 1.40) and woman (RR = 1.22) subgroups. The above data show different therapeutic effects of the ACE-I and ARB. Based on these inspiring data, a meta-analysis concerning coronary artery disease and strokes was performed. It was b ...
noradrenergic neuroeffector transmission as a target of drug action.
noradrenergic neuroeffector transmission as a target of drug action.

... response to NA without affecting the neuronal negative feedback mechanism mediated by 2-adrenoceptors. ...
Antipsychotics
Antipsychotics

... Dopamine Synapse ...
Drugs for Neurodegenerative Diseases
Drugs for Neurodegenerative Diseases

... Other drugs that increase dopamine levels ...
Post-operative Nausea and Vomiting - Vanderbilt University Medical
Post-operative Nausea and Vomiting - Vanderbilt University Medical

... Action: Acetaminophen is part of the non-steroidal anti-inflammatory medications. These medications inhibit cyclooxygenase which is the catalyst for the formation of prostaglandins. After cell injury, prostaglandins cause fever, inflammation and pain responses. (Lehne, 2010. p.840) ...
Gonadal Medications
Gonadal Medications

... Types of Oral Contraceptives: Combination Preparations: contain both estrogen and progestin (most common; 99-100% effective) Biphasic and Triphasic Preparations: low amounts of progestin combined with estrogen; amount of progestin varies during the cycle SubQ Implants: progestin implants containing ...
Targeting the dopamine D receptor in schizophrenia
Targeting the dopamine D receptor in schizophrenia

... higher than those found in the plasma water or spinal fluid in patients; in fact, the concentrations used would be lethal to humans. Additional work in vivo found that chlorpromazine and haloperidol increased the turnover of adrenaline and dopamine, as shown by the increased production of normetanep ...
Acromegaly: A New Therapy
Acromegaly: A New Therapy

... used in those patients not cured by surgery. Radiation can be given either as a series of treatments over several weeks or as a single treatment (stereotactic radiosurgery). The major disadvantage of radiation therapy is the slow onset of action. It often takes many years to reach maximal levels of ...
Indirect cholinergic agonists
Indirect cholinergic agonists

... - Atropine and Scopolamine are belladona alkaloids (competitive inhibitors) -Drugs differ in their CNS effects, scopolamine permeates the blood-brain barrier -At therapeutic doses atropine has negligible effects upon the CNS, scopolamine even at low doses has prominent CNS effects. ...
Adjunct to anesthesia One of a number of drugs or techniques used
Adjunct to anesthesia One of a number of drugs or techniques used

... 4- Decrease airway secretion and 9- Promote smooth induction and salivation. recovery from anesthesia. 5- Obtund autonomic reflex responses. Anticholinergic drugs An anticholinergic agent is a substance that blocks the neurotransmitter acetylcholine in the central and the peripheral nervous system. ...
Selexipag for the treatment of pulmonary arterial hypertension
Selexipag for the treatment of pulmonary arterial hypertension

... to a long-acting metabolite that binds with high selectivity to IP receptors, resulting in vasodilation, inhibition of platelet aggregation, and antiinflammatory effects. Results of a long-term, placebo-controlled, clinical outcomes–driven trial showed that selexipag significantly reduced the occurr ...
Project: Abbott Course Title: REDUCTIL Module title/ID: Competition
Project: Abbott Course Title: REDUCTIL Module title/ID: Competition

... Rimonabant was developed based on the knowledge that cannabis consumption is known to stimulate appetite. When people smoke cannabis, the increase in appetite is due to exogenous cannabinoids. Endogenous cannabinoids, such as anandamide, are thought to have a role in increasing appetite whether or n ...
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Cannabinoid receptor antagonist



The discovery of the endogenous cannabinoid system led to the development of CB1 receptor antagonists. The first cannabinoid receptor antagonist, rimonabant, was described in 1994. Rimonabant blocks the CB1 receptor selectively and it has been shown to decrease food intake and regulate body-weight gain. The prevalence of obesity worldwide is increasing dramatically and has a great impact on public health. The lack of efficient and well-tolerated drugs to cure obesity has led to an increased interest in research and development of cannabinoid antagonists. Cannabidiol, a naturally occurring cannabinoid, is a non-competitive CB1/2 antagonist.
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