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Title: Directly observable behavioral effects of lorcaserin in rats
Title: Directly observable behavioral effects of lorcaserin in rats

... other behavioral effects in rats. For example, the prototypical 5-HT2C receptor agonist mCPP induces yawning and penile erections (Protais et al., 1995; Kennett and Curzon, 1988). In addition to 5-HT2C receptors, lorcaserin also has affinity for other 5-HT receptor subtypes, including 5-HT2A, 5-HT2B ...
Fragment-based Drug Discovery of the Synthetic Small Molecule
Fragment-based Drug Discovery of the Synthetic Small Molecule

... ƒ Some of these compounds possessed activity against hERG (patch clamp) and further SAR showed it was possible to obtain compounds with good efficacy and little or no activity in the hERG assay ƒ AT13387 was chosen as a clinical candidate after further profiling during a candidate selection phase ...
A Novel Tissue Protective Peptide: Cyclic Helix B Peptide
A Novel Tissue Protective Peptide: Cyclic Helix B Peptide

... tissue-protective effects for a wide range of organs, but the very high dosage required to achieve that goal would cause unfavorable side effects, including hypertension and thrombosis [1-3]. Helix B surface peptide (HBSP), which was derived from the aqueous surface of the helix B domain of EPO, was ...
Topic 7
Topic 7

... of neuroscientist Oliver Sachs (played by Robin Williams). ...
Homogeneous GTP Binding Assay For G
Homogeneous GTP Binding Assay For G

... GTP binding assay. Agonist binding to GPCRs stimulates the guanine nucleotide exchange, GDP bound to Gα subunit of heterotrimeric Gproteins, dissociates and is replaced by GTP. Karo Bio’s AlphaKey™ technology is based on BioKey® peptide probes that e.g. specifically bind to the Gαi subunit in a conf ...
Cannabis
Cannabis

... • These compounds are called cannabinoids • The psychotropic effects of cannabis product marijuana and hashish are mostly attributed to Δ9-THC ...
Edarbi to losartan conversion
Edarbi to losartan conversion

... Medscape, LLC requires everyone who is in a position to control the content of an education activity to . Notice: We are a community based organization dedicated to the implementation of fair and consistent guidelines in all California counties as a safe harbor from. Learn about Bumex (Bumetanide) m ...
Worms
Worms

... • Say the dose rate of A in sheep is 0.2 mg/kg. • Let’s say the human ‘no observable effect level’ (NOEL) based on animal studies for A has been determined as 1.25 mg/kg body weight. • The safety factor applied is generally 200. • So, a the adult daily intake (ADI) is 6 g/kg, 200 fold less than the ...
PSY650-Antipsychotics-Sedative-Hypnotics
PSY650-Antipsychotics-Sedative-Hypnotics

... Not for depression-associated anxiety If on stimulant, wait for stimulant effects to wear off – “Wide awake drunk” ...
Drugs affecting the Respiratory System
Drugs affecting the Respiratory System

...  Narrow therapeutic window—therapeutic range is 5-15 mcg/mLh  Multiple drug interactions ...
Selective Serotonin Reuptake Inhibitors (SSRIs) with Dual
Selective Serotonin Reuptake Inhibitors (SSRIs) with Dual

... dramatically from 1 case/10000 in the early 90’s to 1 case/110 in 2011. The diagnosis is characterized by three main domains: dysfunction in social interaction, communication impairment and repetitive behaviors. Selective Serotonin Reuptake Inhibitors (SSRIs) are currently the drug class of choice f ...
Drug receptors and Pharmacodynamics
Drug receptors and Pharmacodynamics

... conformational change in the receptor. Thus the effects of full agonists may be more efficiently coupled to receptor occupancy than those of partial agonists. However, coupling efficiency is also determined by the biochemical events that transduce receptor occupancy into cellular response. High effi ...
A positive allosteric modulator (PAM)
A positive allosteric modulator (PAM)

...  This approach confers a greater selectivity and better glutamate modulatory control at disease mediating receptors. Thus, this mechanism may offer a clinical advantage to maximize therapeutic activity while limiting undesirable side-effects or toxicity.  The possibility to combine PAMs with ortho ...
CHAPTER 3.1 (part 2) and 3.2 READING GUIDE
CHAPTER 3.1 (part 2) and 3.2 READING GUIDE

... CHAPTER 3.1 (part 2) and 3.2 READING GUIDE: ...
Delerium
Delerium

... MOA: increase cholinergic transmission by inhibiting cholinesterase at the synaptic cleft ...
SECONDARY METABOLITES ISOLATED FROM PEROVSKIA
SECONDARY METABOLITES ISOLATED FROM PEROVSKIA

... II. Terrestrial plants of the genus Perovskia The genus Perovskia belongs to the Family Labiatae, Order Lamiales, Class Magnoliopsida, and is made up of seven different species (Perveen et al., 2009). Native to Central Asia, Afghanistan, Iran, and Pakistan, the plants comprising the Perovskia genus ...
Blockade of D2 receptor increases prolactin release and causes
Blockade of D2 receptor increases prolactin release and causes

...  Tardive Dyskinesia – develops late in antipsychotic therapy, usually at high doses x 6 months, rhythmic motions of head, face and shoulders, may be irreversible  Do not use DA or Levo-Dopa, use diphenhydramine (Benadryl), benztropine (Cogentin) or trihexephenidyl (Artane) ...
A fatty acid in the MCT ketogenic diet for epilepsy treatment blocks
A fatty acid in the MCT ketogenic diet for epilepsy treatment blocks

... the MCT diet. Nevertheless, it is believed by many epileptologists that ketogenic diets, including the MCT diet, are often effective in patients who do not respond to antiseizure drugs (Sills et al., 1986b). These physicians would be surprised if the diet was no more efficacious than an antiseizure d ...
Sedatives
Sedatives

... o Eszopiclone/Zolpidem/Zaleplon: hypnotics that modulate GABAA receptor via interaction with BZ binding site (but these are NOT benzos) ...
Interaction of Plant Extracts with Central Nervous System Receptors
Interaction of Plant Extracts with Central Nervous System Receptors

... for interaction with 10 plant extracts, which has contributed to the understanding of the action of herbal medicines and has provided bioassays for analysis of active plant ingredients [10]. Plant extracts from Hypericum perforatum, St. John’s wort, have been frequently studied because of their reco ...
6-rhinitis and cough2015-02-09 20:541.0 MB
6-rhinitis and cough2015-02-09 20:541.0 MB

... In bronchiectasis, pneumonia & TB  they are of partial benefit Hardly any benefit in cystic fibrosis & severe infections  Give rhDNAase ...
Treatment of Cough
Treatment of Cough

... Treatment of Cough 1. Antitussive a. Opioid i. Codeine (methylmorphine) b. Non – opioid i. Dextromethorphan 2. Expectorant a. Guaifenesin 3. Mucolytics a. N – actylcysteine b. Bromhexine c. Ambroxol (active metabolite of Bromhexine) ...
High-dose antipsychotic medication
High-dose antipsychotic medication

... at D2receptors, but their selectivity and potency vary considerably. By 'selectivity' is meant the 'cleanliness' of their pharmacology - what receptors other than D2 receptors the drug might block. 'Potency' is a complex property, reflecting the bioavailability of the drug at strategic sites, and th ...
Benzodiazepines
Benzodiazepines

Lecture 4
Lecture 4

... and can have serious side-effects over time. • Opioid painkillers such as morphine are highly effective at reducing pain, but longterm use can lead to dependence and tolerance. As the body becomes used to the drug it becomes less effective so higher doses are needed for the same effect, side effects ...
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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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