Title: Directly observable behavioral effects of lorcaserin in rats
... addition to 5-HT2C receptors, lorcaserin also has affinity for other 5-HT receptor subtypes, including 5-HT2A, 5-HT2B, and 5-HT1A (Thomsen et al., 2008). Although lorcaserin has been shown to have efficacy at 5-HT2A receptors in vitro (Thomsen et al., 2008), it is unclear whether lorcaserin has agon ...
... addition to 5-HT2C receptors, lorcaserin also has affinity for other 5-HT receptor subtypes, including 5-HT2A, 5-HT2B, and 5-HT1A (Thomsen et al., 2008). Although lorcaserin has been shown to have efficacy at 5-HT2A receptors in vitro (Thomsen et al., 2008), it is unclear whether lorcaserin has agon ...
Antiemetic Guidelines for Chemotherapy and Radiation Therapy
... chemotherapy e.g. cisplatin has a rapid onset of emetogenicity (1.5 hours), so it is important that if pre-chemotherapy agents are given orally, they have sufficient time to be absorbed. Intravenous anti-emetics should only be given if the patient is unable to take oral anti-emetics and should be 30 ...
... chemotherapy e.g. cisplatin has a rapid onset of emetogenicity (1.5 hours), so it is important that if pre-chemotherapy agents are given orally, they have sufficient time to be absorbed. Intravenous anti-emetics should only be given if the patient is unable to take oral anti-emetics and should be 30 ...
Psychopharmacs - antidepressants
... Dual acting antidepressants (IV generation): efficacy comparable to TCA, higher than SSRI, especially in severe depression venlafaxine - available in sustained release formulation-Effexor XR (prolonged duration of action, lower peak plasma levels and fluctuations, better tolerability - higher co ...
... Dual acting antidepressants (IV generation): efficacy comparable to TCA, higher than SSRI, especially in severe depression venlafaxine - available in sustained release formulation-Effexor XR (prolonged duration of action, lower peak plasma levels and fluctuations, better tolerability - higher co ...
A1992HC31200002
... the sttes was also described. Taken together, the data suggested that the unique anesthetic and psychotomimebc properties of PCP-like drugs are mediated at specific PCP receptors. The observation that a benzomorphan’o opiate, Kallyl normetazocine (SKF-10047) bound to the PCP receptor. together with ...
... the sttes was also described. Taken together, the data suggested that the unique anesthetic and psychotomimebc properties of PCP-like drugs are mediated at specific PCP receptors. The observation that a benzomorphan’o opiate, Kallyl normetazocine (SKF-10047) bound to the PCP receptor. together with ...
Opioids
... Therefore, toxicity may result in renal insufficiency due to decreased clearance of this active metabolite (confusion, agitation) Morphine-3-glucuronide is another minor metabolite that may be proconvulsant (CNS excitatory properties; again, take care with renal insufficiency) ...
... Therefore, toxicity may result in renal insufficiency due to decreased clearance of this active metabolite (confusion, agitation) Morphine-3-glucuronide is another minor metabolite that may be proconvulsant (CNS excitatory properties; again, take care with renal insufficiency) ...
nausea and vomiting - KSU Faculty Member websites
... The half-lives of granisetron, tropisetron and the active metabolite of dolasetrom are 2 to 3 times longer than that of ondansetron. These observations initially suggested that more frequent ondansetron administration would be required. However, it has now been shown that receptor blockade dose not ...
... The half-lives of granisetron, tropisetron and the active metabolite of dolasetrom are 2 to 3 times longer than that of ondansetron. These observations initially suggested that more frequent ondansetron administration would be required. However, it has now been shown that receptor blockade dose not ...
THESIS OUTLINE
... In Chapter 7, the effects of chronic treatment with the opioid antagonist NTX upon opioid receptor levels were determined using quantitative autoradiography. Chronic NTX treatment has been shown to induce supersensitivity to morphine’s analgesic effects and is known to increase opioid receptor numbe ...
... In Chapter 7, the effects of chronic treatment with the opioid antagonist NTX upon opioid receptor levels were determined using quantitative autoradiography. Chronic NTX treatment has been shown to induce supersensitivity to morphine’s analgesic effects and is known to increase opioid receptor numbe ...
Pharmacology Definitions
... response from the cell. The antagonist shows no selectivity for the activated state of the receptor and hence the receptor is not activated. Antagonists show affinity for the receptor binding site, having a complementary structure, however have zero efficacy and thus no response is ever achieved by ...
... response from the cell. The antagonist shows no selectivity for the activated state of the receptor and hence the receptor is not activated. Antagonists show affinity for the receptor binding site, having a complementary structure, however have zero efficacy and thus no response is ever achieved by ...
The Organic Chemistry of Drug Design and Drug Action
... FIGURE 3.15 (A) Dose-response curve for an antagonist (X); (B) effect of a competitive antagonist (X) on the response of a neurotransmitter (acetylcholine; ACh); (C) effect of varying concentration of a competitive antagonist X in the presence of a fixed, maximally effective concentration of agonist ...
... FIGURE 3.15 (A) Dose-response curve for an antagonist (X); (B) effect of a competitive antagonist (X) on the response of a neurotransmitter (acetylcholine; ACh); (C) effect of varying concentration of a competitive antagonist X in the presence of a fixed, maximally effective concentration of agonist ...
... After a 1 h equilibration period, a first stimulus was delivered in lower tracheal and bronchial segments. This produced a rapid atropine-sensitive contraction, followed by a longer lasting atropine-resistant NANC contraction. Stimuli were delivered every 20–30 min or when the tension had returned t ...
the Pressure Right® PONV (Post Operative Nausea
... effectively deal with both early and delayed postoperative nausea and vomiting (PONV) symptoms. Its consistent anti-nausea effectiveness is continuous for up to 3 days. As a result, patients can have a hassle-free experience leading to a better quality of life recovery from PONV issues associated wi ...
... effectively deal with both early and delayed postoperative nausea and vomiting (PONV) symptoms. Its consistent anti-nausea effectiveness is continuous for up to 3 days. As a result, patients can have a hassle-free experience leading to a better quality of life recovery from PONV issues associated wi ...
Antipsychotics Antimanics Antidepressants
... MAO-A inhibitor with short duration of action; full ...
... MAO-A inhibitor with short duration of action; full ...
Towards a Molecular Description of the GABA
... Major mammalian inhibitory neurotransmitter receptor Pentameric integral membrane protein containing an ion channel selective for chloride ions. ...
... Major mammalian inhibitory neurotransmitter receptor Pentameric integral membrane protein containing an ion channel selective for chloride ions. ...
File
... blockers are available from different chemical families. • Diphenhydramine and Chlorpheniramine may be considered prototypes. • Because they have been developed for use in chronic conditions, H1 blockers are all active by the oral route. • Most are metabolized extensively in the liver. ...
... blockers are available from different chemical families. • Diphenhydramine and Chlorpheniramine may be considered prototypes. • Because they have been developed for use in chronic conditions, H1 blockers are all active by the oral route. • Most are metabolized extensively in the liver. ...
Document
... A small # of drugs produce their physiological effect without interacting with receptors. Examples: Drugs that bind to enzymes interfere with the normal activity of the enzyme in one of 2 ways CompetitiveNon-competitiveDrugs can also bind to membrane transport proteins (competitively and non-compet ...
... A small # of drugs produce their physiological effect without interacting with receptors. Examples: Drugs that bind to enzymes interfere with the normal activity of the enzyme in one of 2 ways CompetitiveNon-competitiveDrugs can also bind to membrane transport proteins (competitively and non-compet ...
Pharmacology Tutoring for Sedative Hypnotics and Antiemetics
... Which of the following is in the class that has been described as the most effective antiemetics to date? ...
... Which of the following is in the class that has been described as the most effective antiemetics to date? ...
Introduction to Pharmacology
... – A drug molecule which, when it interacts with a given receptor, produces a stimulus for change beyond the level of that receptor, but the stimulus is less than the maximum characteristic of that receptor ...
... – A drug molecule which, when it interacts with a given receptor, produces a stimulus for change beyond the level of that receptor, but the stimulus is less than the maximum characteristic of that receptor ...
Pharm_essays
... GC are steroid hormones. Endogenous GC are produced from cholesterol in the adrenal cortex and have general metabolic and systemic effects on carbohydrate and protein metabolism. Exogenous GC given therapeutically have powerful anti-inflammatory and immunosuppressive effects. The mechanism of GC act ...
... GC are steroid hormones. Endogenous GC are produced from cholesterol in the adrenal cortex and have general metabolic and systemic effects on carbohydrate and protein metabolism. Exogenous GC given therapeutically have powerful anti-inflammatory and immunosuppressive effects. The mechanism of GC act ...
Hallucinogens - People Server at UNCW
... and/or colorful visions Complete loss of time sense Bizarre distortions of body shape or size Altered perception of body consistency Sensations of floating or hovering in space Feelings of leaving one’s body Visions of spiritual or supernatural beings Emotions ranging from euphoria to ...
... and/or colorful visions Complete loss of time sense Bizarre distortions of body shape or size Altered perception of body consistency Sensations of floating or hovering in space Feelings of leaving one’s body Visions of spiritual or supernatural beings Emotions ranging from euphoria to ...
5th Lecture 1433
... An inverse agonist has higher affinity for R than for R* and thus will shift the equilibrium from the active (R*) to resting state (R) state A neutral antagonist has equal affinity for R and R* so does not by itself affect the conformational equilibrium but reduces by competition the binding of ...
... An inverse agonist has higher affinity for R than for R* and thus will shift the equilibrium from the active (R*) to resting state (R) state A neutral antagonist has equal affinity for R and R* so does not by itself affect the conformational equilibrium but reduces by competition the binding of ...
Serotonin or 5-hydroxytryptamine
... pulsations – Migraine attack associated with (based on histological studies): • sterile neurogenic perivascular edema • inflammation (clinically effective antimigraine medication reduce perivascular inflammation) ...
... pulsations – Migraine attack associated with (based on histological studies): • sterile neurogenic perivascular edema • inflammation (clinically effective antimigraine medication reduce perivascular inflammation) ...
What lessons can we learn from 20 years of chemokine receptor drug discovery?
... Glu283 essential for almost all compound interactions (except TAK-779) Partially overlaps with endogenous ligand binding site 2 ...
... Glu283 essential for almost all compound interactions (except TAK-779) Partially overlaps with endogenous ligand binding site 2 ...
Mainly 15-45 age range, but increasing in kids!
... Chloropromazine was a cheap, failed anti-histamine, which was unbelievably effective: ...
... Chloropromazine was a cheap, failed anti-histamine, which was unbelievably effective: ...
Pharmacology of Serotonin Reuptake Inhibitors (SRIs):
... MAO and COMT destroy DA DA Reuptake Pump Presynaptic DA autoreceptors: negative feedback on the release of DA 5-HT (serotonin) 2A receptors affect DA ...
... MAO and COMT destroy DA DA Reuptake Pump Presynaptic DA autoreceptors: negative feedback on the release of DA 5-HT (serotonin) 2A receptors affect DA ...
2 receptor
... especially at larger doses b2：vasodilatation of skeletal muscles and coronary vessels ...
... especially at larger doses b2：vasodilatation of skeletal muscles and coronary vessels ...
5-HT3 antagonist
The 5-HT3 antagonists, informally known as ""setrons"", are a class of drugs that act as receptor antagonists at the 5-HT3 receptor, a subtype of serotonin receptor found in terminals of the vagus nerve and in certain areas of the brain.With the notable exception of alosetron and cilansetron, which are used in the treatment of irritable bowel syndrome, all 5-HT3 antagonists are antiemetics, used in the prevention and treatment of nausea and vomiting. They are particularly effective in controlling the nausea and vomiting produced by cancer chemotherapy and are considered the gold standard for this purpose.The 5-HT3 antagonists may be identified by the suffix –setron, and are classified under code A04AA of the WHO's Anatomical Therapeutic Chemical Classification System.