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GABA - the Houpt Lab
GABA - the Houpt Lab

... 2. Stored in vesicles in the presynaptic terminal & released with a specific effect on target postsynaptic cell via receptors 3. Exogenous administration (e.g. injection) causes the same effect 4. A specific mechanism exists to remove it from the synapse 5. Each neuron makes only one or a few neurot ...
Corporate Presentation
Corporate Presentation

... 2012; Phase II (pediatrics) initiated early 2012 Competitive Positioning: Expected to be first-to-market longacting hGH; Superb clinical, safety and immunogenicity profile, non-viscous drug product, granted orphan designation in the U.S. CMC Status – High-yielding, high-quality GMP process and drug ...
Practical I
Practical I

... "Reversible" cholinesterase inhibitors are generally short-acting. They bind AChE reversibly. They include physostigmine that enters the CNS, and neostigmine and edrophonium that do not. Physostigmine enters the CNS and can cause restlessness, apprehension, and hypertension in addition to the effect ...
I.2 New Prospects for Drug Discovery (IV)
I.2 New Prospects for Drug Discovery (IV)

... As stated above it would be extremely desirable, for the discovery and development of new drugs, to have a well-defined structure for the inactive and active conformation of the different GPCR of pharmacological interest. This could allow the elucidation of the molecular details of the activation me ...
Chapter 16 Cholinesterase Inhibitors
Chapter 16 Cholinesterase Inhibitors

... Variety of bacteria and protozoa can be responsible Infections are usually self-limited Many cases require no treatment Antibiotics should be used only when clearly indicated ...
TRICYCLIC ANTIDEPRESSANTS
TRICYCLIC ANTIDEPRESSANTS

... T, Fraser DT. Site of action and active form of local anesthetics. Neurossci Res, 1971, 4, 65-99 ...
Sympathetic Drugs
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... from GIT, 1st-pass hepatic elimination  more rapidly eliminated. • Also more likely to enter CNS and cause central effects (e.g., nightmares). • Cardioselectivity diminishes with higher doses. ...
Time to Sleep Anesthesia Pharmacology Review
Time to Sleep Anesthesia Pharmacology Review

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Inhibitory effect of deltorphin-II on development of

... malaria in humans: P. falciparum, P. vivax, P. ovale, P. malariae and P. knowlesi [1]. It is a disease that can be treated in just 48 hours, yet, it can cause fatal complications if the diagnosis and treatment are delayed. Malaria is the fifth-most common cause of death from infectious diseases worl ...
Parkinson`s disease
Parkinson`s disease

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... continue to be an important target for drug development. Current global revenues for kinase inhibitors were nearly $29.1 billion in 2011 and are projected to reach nearly $40.3 billion in 201513. ...
Ligand Residence Time at G-protein–Coupled Receptors—Why We
Ligand Residence Time at G-protein–Coupled Receptors—Why We

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Exploring the Possible Mode of Anxiolytic Action
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Opioids
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Antihistamines
Antihistamines

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Psychiatric Drugs Bind to Classical Targets Within Early Exocytotic
Psychiatric Drugs Bind to Classical Targets Within Early Exocytotic

... Figure 1. Insights from intracellular nicotine actions on the ␣4␤2 nicotinic acetylcholine receptors (nAChR). (A) Chaperoning, matchmaking, reduction of endoplasmic reticulum (ER) stress, and the unfolded protein response (UPR) (5,16,88). Nicotine enters the neuron, permeates into the ER, and serves ...
Angiotensin receptor blocker (arb) antihypertensive dose
Angiotensin receptor blocker (arb) antihypertensive dose

... Development of Diabetic Nephropathy in Patients with Type 2 Diabetes. Hans-Henrik Parving, M.D., D.M.Sc., Hendrik. Diuretics, angiotensin-converting enzyme inhibitors (ACEIs), and angiotensin receptor blockers (ARBs) represent 3 classes of drugs widely used in the treatment of. Each profile is a com ...
Newer Antihypertensive Drugs
Newer Antihypertensive Drugs

... Renalase, a novel kidney-related peptide that might impact CV health. Renalase is the first known circulating amine oxidase in plasma that metabolizes catecholamines. ...
Solubility # 6
Solubility # 6

... nature of lipid, because it has a primary alcohol) and a long hydrocarbon chain, such as that of fatty acids, which make up part of a lipid membrane. ⇒ The concentration of the drug in both layers is determined by appropriate analytical technique. [drug] lipid ⇒ P= ...
PowerPoint 演示文稿
PowerPoint 演示文稿

... drug does the body. That is original action between the drug and the cells of the body. The action of the drug does the body. That is original action between the drug and the cells of the body. ...
Endocrinology Drug List
Endocrinology Drug List

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Drugs for respiratory system
Drugs for respiratory system

... Cough is usually a valuable protective reflex mechanism for clearing foreign material and secretions from the airway. In some conditions, such as inflammation or neoplasia, the cough reflex may become inappropriately stimulated and in such cases, antitussive drugs may be used. ...
Effector Pathway-Dependent Relative Efficacy at Serotonin Type 2A
Effector Pathway-Dependent Relative Efficacy at Serotonin Type 2A

... (Costa et al., 1992; Samama et al., 1993; Leff, 1995). The active form of the receptor is capable of interacting with effector in the absence of agonist and thus is partly responsible for basal effector activation. Agonists act by preferentially binding to and enriching the active (R*) form, thereby ...
3D QSAR AND MOLECULAR DOCKING STUDIES OF STRUCTURALLY DIVERSE ESTROGEN
3D QSAR AND MOLECULAR DOCKING STUDIES OF STRUCTURALLY DIVERSE ESTROGEN

... ovaries and testis with involvement of placenta, adipose tissue, and adrenal glands1. Among the several structurally related forms 17βestradiol is found as predominant. Estrogen plays crucial role in female reproductive system and also exerts important effects on nonreproductive targets such as bone ...
Early treatment of psychosis
Early treatment of psychosis

... Copyright holders of content included in this material should contact [email protected] with any questions, corrections, or clarification regarding the use of content. For more information about how to cite these materials visit http://open.umich.edu/education/about/terms-of-use. Any medical i ...
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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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