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Drug-induced hypo- and hyperprolactinemia: mechanisms, clinical
Drug-induced hypo- and hyperprolactinemia: mechanisms, clinical

... circumventricular organs. In hypothalamus, the secretion of prolactin is independent from the one in the hypophysis, although the exact function of prolactin produced at this level or elsewhere has not been identified. It must be noted that, for delivery at the CNS level, the circulant prolactin mus ...
Understanding the metabolism of codeine is important for the
Understanding the metabolism of codeine is important for the

... will still produce morphine from codeine, but much less than the EMs or UMs (less than 1% conversion). Thus, the concentrations of morphine and its metabolites in their plasma will be so low as to be not measurable. Having said that, these metabolites are still formed, and they do appear in the urin ...
The Rational Use of Drugs - Part 4
The Rational Use of Drugs - Part 4

... When the assumption of linearity does not hold, the EC50 no longer approximates the KD. For example, the EC50 will be much smaller than the KD when “spare receptors” are present. A tissue is said to express “spare receptors” when only a small fraction of the receptor population must be occupied by d ...
Marijuana Dosing Issues: Notes From the Literature
Marijuana Dosing Issues: Notes From the Literature

... by phenotypes, and even the time of harvest affects which cannabinoids are present and in what percentages. An individual may be much more sensitive than another, heavy smokers may experience different chemical effects than light smokers, and ingestion may alter bioavailability. “The bulk of the res ...
I The 1982 John
I The 1982 John

... different as ...
`Spice` Wars - Cayman Chemical
`Spice` Wars - Cayman Chemical

... mixture of synthetic cannabinoids (Table 1). Importantly, two novel compounds, JWH 200 and JWH 250, were positively identified, suggesting that the variety of synthetic cannabinoids that are currently in use may be underappreciated. Cayman Chemical intends to continue developing products and methods ...
A case of heroin overdose reversed by sublingually administered
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... poppy, Papaver somniferum. Although developed originally as an analgesic, its potential utility for the management of opioid dependence has been discussed since early research in the 1970s [13]. Buprenorphine exerts the majority of its effects at the mu opioid receptor where it acts as a partial ago ...
Dopamine and glucose, obesity, and reward deficiency syndrome
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Overview of pleiotropic effects of platelet P2Y12receptor inhibitors
Overview of pleiotropic effects of platelet P2Y12receptor inhibitors

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Glycine receptors in the central nervous system
Glycine receptors in the central nervous system

... Alcohol is a legal, easily accessible and socially accepted drug. This status contributes to the widely spread consumption of ethanol, entailing that individuals vulnerable to addiction are likely to encounter this particular drug. As a drug ethanol is commonly consumed for its acute effects. In hum ...
Biological substrates of reward and aversion: A nucleus accumbens
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... and Rompré, 1989). There are three primary lines of evidence implicating the NAc in reward, involving pharmacological, molecular, and electrophysiological approaches. 3.1. Pharmacological evidence It is well established that drugs of abuse (Di Chiara and Imperato, 1988) and natural rewards (Fibiger ...
A Multifaceted GABAA Receptor Modulator
A Multifaceted GABAA Receptor Modulator

... general anesthetic etomidate. The negligible activities displayed by methaqualone at numerous neurotransmitter receptors and transporters in an elaborate screening for additional putative central nervous system (CNS) targets suggest that it is a selective GABAAR modulator. The mode of action of meth ...
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Characterization of the Effects of the Partial Dopamine Agonist

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Opioids - Waterloo Region Integrated Drugs Strategy
Opioids - Waterloo Region Integrated Drugs Strategy

... Fentanyl is a potent opioid, used in anesthesia, for pain, chronic pain, pain in end of life care Typically administered as a patch placed on the skin Fentanyl is produced by pharmaceutical manufacturers Small chemical changes to fentanyl can result in drugs with very similar actions These “bootleg” ...
Barbiturate
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The so-called „designer steroids“ Nor
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... The anabolic androgenic steroids belong to the list of prohibited substances given by the WADA´s List Committee. In fact, not all the biological and toxicological risks especially when administered for doping purposes are unknown. Thus, we completely characterized the substances Norbolethone, Desoxy ...
Glucagon Receptor Agonists and Antagonists
Glucagon Receptor Agonists and Antagonists

... mRNA levels in the retina increase with plus lens wear.6 Conversely, the absence of immediate early gene production during form deprivation or negative lens wear implies minimal release of peptides from glucagon amacrine cells and suggests that the lack of glucagon is responsible for the development ...
Medical Cannabis for Aging - Americans for Safe Access
Medical Cannabis for Aging - Americans for Safe Access

... ulcers at therapeutically effective doses. Cannabinoid receptors in the brain Moreover, it does not depress respiration, produce dependence, induce body weight loss, or cause mutations, as many commonly prescribed drugs do. Studies on its mechanism of action are currently underway, with cytokine syn ...
6 points each
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... some patients. Theoretically, what kinds of change(s) in receptor binding would be desirable in a new drug (call it “neo-olanzapine”) that would have the same therapeutic effect and potency as olanzapine, but less dry mouth. How could the development of such a compound be pursued most effectively? S ...
Safety and Side Effects of Cannabidiol, a Cannabis sativa Constituent
Safety and Side Effects of Cannabidiol, a Cannabis sativa Constituent

... [2][3]. Evidence suggests that the potency of CBD has decreased in recent years, while THC concentrations have increased, since the use of varieties such as sensimillia (‘skunk’), provided by ilegal cannabis growers, currently dominates the supply of cannabis in many countries [3]. CBD induces marke ...
Introduction to Inhibitors
Introduction to Inhibitors

... maximum after exposure to inhibitory molecule for a selected period of time. This term is used usually with ...
Intro to Inhibitors-MM edition-final
Intro to Inhibitors-MM edition-final

... maximum after exposure to inhibitory molecule for a selected period of time. This term is used usually with ...
Maricopa County Superior Court Family Court
Maricopa County Superior Court Family Court

...  Most compounds are not detected by standard drug screening tests ...
Document
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... Hismanal was FDA approved in 1988 as an antihistamine for allergy and hay fever symptom relief. The FDA first warned consumers and healthcare providers of new safety information regarding Hismanal February 9, 1998 due to the risk of death, cardiovascular adverse events, anaphylaxis, and serious drug ...
m5zn_776561dda50e649
m5zn_776561dda50e649

... ● Medicinal chemistry is a chemistry-based discipline, also involving aspects of biological, medical and pharmaceutical sciences. It is concerned with the invention, discovery, design, identification and preparation of biologically active compounds, the study of their metabolism, the interpretation ...
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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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