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Lorcaserin : The Serotonergic Weight Loss Medication
Lorcaserin : The Serotonergic Weight Loss Medication

... progressive fat loss. Belviq does not produce side effects of anxiety, depression, insomnia, palpations, racy heart, or constipation seen with the older appetite suppressors. In addition, Belviq has no effect on metabolism or “fat burning” it simply reduces appetite and food intake. In addition, Bel ...
No Tolerance to Peripheral Morphine Analgesia in
No Tolerance to Peripheral Morphine Analgesia in

... drawn into coded syringes by a nurse and given to the anesthesiologist and surgeon, respectively, who did not know their contents and performed the injections. General anesthesia was then terminated. The codes were broken at the end of the study. Assessment of pain. Postoperative pain was assessed u ...
GI Drugs
GI Drugs

... Drugs that affect GI motility (used for irritable bowel syndrome, GERD, prevention of vomiting) Physiology of GI motility  Afferent: Bolus of food, mechanically or chemically, activates enterochromaffin cells to release 5-HT  Interneurons: 5-HT binds to 5-HT3 receptors on afferent neurons  Effer ...
Neuromuscular Blockers Joanne Leung
Neuromuscular Blockers Joanne Leung

... • The only depolarizing neuromuscular blocker in clinical use • Very rapid onset of action (<1 min) • Short duration of action (5-10 min) • Acts as an ________ agonist at the nicotinic cholinergic receptor (similar action to ACh, but longer acting) ...
Redalyc.Neurobiological alterations in alcohol addiction: a review
Redalyc.Neurobiological alterations in alcohol addiction: a review

... GABA or γ-amino-butyric acid is the principal inhibitory neurotransmitter in the brain, and the GABAergic system plays an important role in the behavioural and pharmacological effects of ethanol. GABAA receptor protein complex is composed of five subunits, assembled to form a channel across the neur ...
Muharema Mustic
Muharema Mustic

... preference in high preference mice when given for 1 week? 2. Do these drugs prevent increase in preference that was due to vehicle injections that occurred over the 3 week period? ...
Pharmacology of anaesthetics
Pharmacology of anaesthetics

... • Mechanism of action – via acetylcholine receptor • Used to facilitate tracheal intubation, mechanical ventilation and surgery ...
opioid receptor gene variants: lack of association with
opioid receptor gene variants: lack of association with

... and these variants result in three amino acid substitutions (Ala6Val, Asn40Asp and Ser147Cys). The Ala6Val and Ser147Cys variants were rare and were observed in 2/134 chromosomes (0.015%) and in 3/1062 chromosomes (0.0028%), but were not characterized further. However, the Asn40Asp and IVS2+691 poly ...
Cholinergic and Anti
Cholinergic and Anti

... Page 2 of 9 i. The person is still making acetylcholine, you’re not giving them a drug that looks like acetylcholine to bind to a receptor ii. Rather, you’re putting in a drug that looks like acetylcholine to inhibit the breakdown of acetylcholine iii. This is an indirect mimetic agent as opposed to ...
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... Photo source: http://www.debatingeurope.eu/ and http://www.zocalopublicsquare.org/ ...
Morphine HO-  Group is needed for activity HO
Morphine HO- Group is needed for activity HO

... there were few pharmacological tools for the study of δ receptors. As a consequence, our understanding of their function is much more limited than those of the other opioid receptors.Recent work indicates that exogenous ligands which activate the delta receptors mimic the phenomenon known as 'ischem ...
40th Anniversary of Opioid Agonist Pharmacotherapy for
40th Anniversary of Opioid Agonist Pharmacotherapy for

... Dole, V.P., Nyswander, M.E. and Kreek, M.J.: Narcotic blockade: a medical technique for stopping heroin use by addicts. Trans. Assoc. Am. Phys., 79:122136, 1966. 2) Translational applied clinical research performed at Manhattan General Hospital (to become Bernstein Institute of Beth Israel Medical C ...
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... phenethyl and it was found to be longer acting (6 hrs) than salbutamol •During the recent Modification of the aryl ether group in Salmeterol, it was a great success that this improved the compound with significantly increased durations of action had been developed. ...
Neurobiological alterations in alcohol addiction: a review
Neurobiological alterations in alcohol addiction: a review

... GABA or γ-amino-butyric acid is the principal inhibitory neurotransmitter in the brain, and the GABAergic system plays an important role in the behavioural and pharmacological effects of ethanol. GABAA receptor protein complex is composed of five subunits, assembled to form a channel across the neur ...
Serotonergic Modulation of Rat Pineal Gland Activity: In Vivo
Serotonergic Modulation of Rat Pineal Gland Activity: In Vivo

... Experiment 2. The aim of this experiment was to assess the effects of 5-HT receptor activation by m-CPP on the pineal melatonin production during the night, when the gland is physiologically activated by NE. To this purpose, 54 rats (weighing 200 –250 g) were used in this experiment. At 9:00 PM, in ...
Hallucinogens - People Server at UNCW
Hallucinogens - People Server at UNCW

... • Although neurotoxic doses in non-humans (520 mg/kg twice or more/day for several days) are generally higher than would be typical of human use, people often take several tablets at a time or throughout an night’s binge and a tablet may contain up to 300 mg: 4-5 mg/kg in an average person. ...
Hydrogen Bonding: The Last Mystery in Drug Design?
Hydrogen Bonding: The Last Mystery in Drug Design?

... interacts with Gly216 is reduced to –CH2–, affinity decreases only by a factor of 4 [32]. Sometimes, it seems that exact shape similarity is more important for affinity than the formation of hydrogen bonds. 2,4-Difluorotoluene, sterically mimicking thymine, is a striking example. Although this analo ...
JA Jeevendra Martyn
JA Jeevendra Martyn

... J. A. Jeevendra Martyn The physiology of neuromuscular transmission could be analyzed and understood at the most simple level by using the classic model of nerve signaling to muscle through the acetylcholine receptor. The mammalian neuromuscular junction is the prototypical and most extensively stud ...
OVERVIEW
OVERVIEW

... target but have different efficacies (degree of response) , why? This observation suggests that other factors, in addition to affinity and receptor occupancy, determine the strength of response. Accordingly, an additional modifier termed intrinsic activity was proposed. This use of the word "efficac ...
The Magic Mint - Stephanie Nichole Halbleib
The Magic Mint - Stephanie Nichole Halbleib

... • Activated endogenous by peptides (like endorphins), or exogenously by alkaloid opiates (such as morphine) • Signal transduction is theorized as follows: – Activation is coupled to the G protein which increases phosphodiesterase activity – Breaks down cAMP, producing an inhibitory effect in neurons ...
The thesis
The thesis

... The sensation of pain is fundamental in the maintenance of the biological integrity of the body, but chronic pain status cause severe somatic and psychic impairment, which give rise to considerable social and economic burden not only on the individual but also on the society. The International Assoc ...
  CLINTON E. CANAL, PH.D. CURRICULUM VITAE
  CLINTON E. CANAL, PH.D. CURRICULUM VITAE

... determinants for ligand binding at serotonin 5-HT2A and 5-HT2C GPCRs: Affinity results analyzed by molecular modeling and ligand docking studies. International Journal of Quantum Chemistry, 112, 38073814. PMID: 23913978; PMCID: PMC3729958. 15. Morgan, D., Canal, C.E., Kondabolu, K., Sakhuja, R., Rob ...
Appetitive Instrumental Learning Requires Coincident Activation of
Appetitive Instrumental Learning Requires Coincident Activation of

... On days 1–5 of testing, each rat received the appropriate microinf usion immediately before it was placed in an operant chamber. For experiment 1, rats received either a low (n ⫽ 8), medium (n ⫽ 9), or high (n ⫽ 9) dose of SCH-23390 or saline (n ⫽ 8). For experiment 2, rats received either AP-5 (n ⫽ ...
Effect of Ergot Alkaloids on 3H-Flunitrazepam Binding to Mouse
Effect of Ergot Alkaloids on 3H-Flunitrazepam Binding to Mouse

... the steroid binding site that seems to mediate rapid, nongenomic effects of neuroactive steroid hormones in the brain2,3. The recognition sites for other classes of compounds on GABAA receptors were also hypotesized2. Ergot drugs have been used clinically in many settings: as diagnostics, cognition ...
Drugs used in Parkinson`s disease
Drugs used in Parkinson`s disease

... • Hepatic function monitoring is needed.Most seriously, fulminating hepatic necrosis is associated with tolcapone use. • Entacapone does not exhibit this toxicity and has largely replaced tolcapone. • Effect of entacapone on dopa concentration in the central nervous system COMT =catechol-Omethyltran ...
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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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