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Chapter 4 Lecture Notes Page
Chapter 4 Lecture Notes Page

... Glycine (found in spinal cord and lower brain stem) Peptides Endogenous opiads “like opium” found in midbrain (tectum, tegmentum, periaquductal gray) Produces analgesia Inhibits fleeing and hiding Produces “reward” or reinforcement Lipids Cannabinoids THC (analgesia and sedation, stimulates appetit ...
General Issues
General Issues

... (draw with a solid line) 3. How would a non-competitive antagonist modify the curve (draw with a dotted line) ...
answers - UCSD Cognitive Science
answers - UCSD Cognitive Science

... o Blood albumin: if the molecule is bound to a depot (like albumin) they cannot reach their sites of action o Fat cells: another example, most slowly, and less likely to interfere with the initial effects of the drug  Blood brain barrier: only lets fat soluble molecules pass; the faster a drug can ...
Antagonists
Antagonists

... in one cell type but not another • Other genes are regulated by a hormone only during specific times (i.e. cell division, differentiation, etc) • We need to understand these details to understand physiology, pathophysiology and pharmacology ...
Introduction to neuropharmacology
Introduction to neuropharmacology

... No formal system for the classification of receptors exists. A receptor is usually defined as a protein that binds a relatively specific molecule called the ligand. The binding of the ligand to its receptor has a functional effect. The two main types of receptors could be defined as ionotropic and m ...
mind altering… synthetic (designer) and naturally occuring
mind altering… synthetic (designer) and naturally occuring

... Administration (FDA) for treatment of chemotherapy-induced nausea and vomiting that has not responded to conventional antiemetics. Though it was approved by the FDA in 1985, the drug only began marketing in the United States in 2006. It is also approved for use in treatment of anorexia and weight lo ...
Proceedings of the British Pharmacological Society
Proceedings of the British Pharmacological Society

... increases food intake in satiated or non-deprived animals by a central mechanism of action (1). In order to test the hypothesis that endogenous GABA, acting at central GABAB receptors, plays a physiological role in the control of feeding behaviour, we argued that blocking these receptors with a cent ...
Population responses
Population responses

... Mixed antagonist: binds to separate site but modulates the ability of agonist to bind Physiological antagonist: a drug (or endogenous mediator) that antagonizes the effect of another drug (or endogenous mediator) by producing an opposing physiological response, typically by a different type of recep ...
Receptors & Transmitters
Receptors & Transmitters

...  disease (epilepsy, ALS, Parkinson’s)  drug abuse (cocaine, amphetamine)  treatment (depression, OCD) ...
A Project by Rose Software Ltd
A Project by Rose Software Ltd

... although even himself had no understanding of its pharmacodynamical characteristics at that time. He developed peptidergic agonists-antagonists against numerous vasopressin receptor sub-types, however, no one had an understanding of the receptor dynamics of brain vasopressin-receptor („V3, currently ...
The Organic Chemistry of Drug Design and Drug Action
The Organic Chemistry of Drug Design and Drug Action

...  90% of -blockers, antiepileptics, and oral anticoagulants on drug market are racemates  50% of antihistamines, anticholinergics, and local anesthetics on drug market are racemates ...
(2-aminoethyl) imidazole
(2-aminoethyl) imidazole

... • The activity of E-isomer is great higher than that of Z-isomer. ...
Receptor pharmacology
Receptor pharmacology

... Ligand: any molecule that binds to a receptor. Examples: Nicotine, curare, and mecamylamine are ligands for the muscle nicotinic receptor. Agonist: a ligand that activates the receptor (opens a ligand-gated channel or stimulates a G protein). Example: Nicotine is an agonist at the nicotinic receptor ...
1B Ulcer Medicines
1B Ulcer Medicines

... in the stomach wall, but an enzyme (15-hydroxyprostaglandin dehydrogenase) stops the prostaglandins from working. Licorice blocks this enzyme, and so the prostaglandins stick around longer, make ulcers heal. HOWEVER chemistry always has a price, licorice causes cortisol to bind to a protein causing ...
Addiction - ISpatula
Addiction - ISpatula

... they must learn to appreciate the effects) -Marijuana tends to inhibit aggression and accentuate caution as opposed to alcohol ...
d) Bronchodilator Response
d) Bronchodilator Response

... Agonists. A drug that has both affinity for a receptor and elicits a response is called an agonist. A drug that produces a less than maximal effect is termed a partial agonist. Antagonists. A drug that has affinity for a receptor but is not able to induce an effect is known as an antagonist. Antagon ...
Drugs Affecting Uterine Contraction
Drugs Affecting Uterine Contraction

... • fetal distress, prematurity, abnormal presentation) ...
Neurotransmitter Receptors - VCC Library
Neurotransmitter Receptors - VCC Library

... urinating, constipation, potential for diabetes (high glucose concentration from glycogenolysis), and low blood pressure due to dilation of vessels. 2. A 1-antagonist would help decrease the heart rate and force of contraction. Also, an M2-agonist would slow the heart rate to normal. By combining t ...
THE UNIVERSITY OF AUCKLAND
THE UNIVERSITY OF AUCKLAND

... b) Based on the data, what type of drug (i.e. type of agonist or antagonist) does Drug B appear most likely to be? Explain your answer and provide an example of this type of drug. (3 marks) Full marks could be achieved with either CRA or NCA, depending on how data was interpreted – either was fine, ...
Neurophysiol
Neurophysiol

... postsynaptic potential ...
Darifenacin Hydrobromide
Darifenacin Hydrobromide

... ----A potent and competitive M3 selective receptor antagonist a white to almost white, crystalline powder. Brand name : Emselex Synonyms: (S)-2-{1-[2-(2,3-Dihydrobenzofuran-5yl)Ethyl]-3-Pyrrolidinyl}-2,2-Diphenylacetamide Hydrobromide ...
PREMEDICATION DRUGS
PREMEDICATION DRUGS

...  Imidazo – benzodiazepine derivative  It is this imidazole ring which imparts water solubility ...
- ISpatula
- ISpatula

... -the interaction of second messenger usually occurs around the C-termini and the ligand interacts with the receptor at the area between the N-termini and the extracellular loops we can classify them to different classes depending on their structure: (usually the N-terminus makes the difference) Clas ...
Summary overview: Gi and Gs G-protein coupled receptors - Di-Et-Tri
Summary overview: Gi and Gs G-protein coupled receptors - Di-Et-Tri

... There are also inhibitory G-proteins . The stimulatory Gsα, when it binds GTP, activates Adenylate cyclase. . An inhibitory Giα, when it binds GTP, inhibits Adenylate cyclase. Different effectors & their receptors induce Giα to exchange GDP for GTP than those that activate Gsα. In some cells, the co ...
The Discovery of the Endocannabinoid System
The Discovery of the Endocannabinoid System

... intracellular signaling molecules. The chemical structure of delta 9-THC, the classic and prototypical cannabinoid of the cannabis plant, has been modified to create synthetic analog drugs like HU-210, which is many times more potent an agonist (chemical activator) of the CB1 receptor. Such potent d ...
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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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