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Kinetics of metoclopramide effects on human 5
Kinetics of metoclopramide effects on human 5

... compared with the fast onset and offset kinetics of 5-HT-induced currents (for example, the wash out of pre-equilibrated metoclopramide is 150 times slower than the onset of 5HT-induced currents, see Fig. 2, right panel) and (2) the low efficacy of metoclopramide in inhibiting radioligand binding (e ...
Schizophrenia and the supersensitive synapse
Schizophrenia and the supersensitive synapse

... subsequently categorize into subsets of neuropsychiatric disorders. The model may be termed the ‘supersensitive synapse’. Outline of the integrated model The chain of events starts with a nonspecific injury. This can be a gene mutation leading to hypofunction or hyperfunction of a protein. It can be ...
Datasheet - Santa Cruz Biotechnology
Datasheet - Santa Cruz Biotechnology

... interacting with specific intracellular receptors to regulate gene expression. This superfamily of receptors includes both steroid and nonsteroid receptors. Like many nonsteroid hormone receptors, PXR (Pregnane X Receptor) binds as a heterodimer with RXR to a DNA sequence typical of a nonsteroid hor ...
File
File

... Opioid Analgesics • Analgesics: Are the Drugs which selectively relieves pain by acting in the CNS or on peripheral pain mechanisms, without significantly altering the consciousness – Opioids and NSAIDS • Narcotics Those drugs which possess both an analgesic (pain relieving) and sedative properties. ...
曹永孝
曹永孝

... III. Ganglion-Blocking Drugs These agents block the action of ACh and similar agonists at the N receptors of autonomic ganglia. They lack selectivity and have broad side effects so that they have been abandoned for clinical use. ...
Chapter 8 Cholinoceptor
Chapter 8 Cholinoceptor

... III. Ganglion-Blocking Drugs These agents block the action of ACh and similar agonists at the N receptors of autonomic ganglia. They lack selectivity and have broad side effects so that they have been abandoned for clinical use. ...
lec#6 ANS - DENTISTRY 2012
lec#6 ANS - DENTISTRY 2012

... Its peripheral actions are mainly due to ↑ NE release Has little direct effects on adrenergic receptors particularly β2 Unlike NE, it is not metabolized by MAO or COMT so it has longer DOA and it is effective orally ...
Download the presentation slides (PDF)
Download the presentation slides (PDF)

... and the American College of Physicians have all issued cautiously affirmative statements • Legal for medicinal use in 20 states • Legal for recreational use in 2 states ...
- University of Mississippi
- University of Mississippi

... Although moderate to severe pain is a very common medical complaint among patients, it is still a very complicated condition to manage. In most communities today, pain is managed by giving opioids, like morphine, to patients. Although opioids have strong analgesic effects, they can also produce many ...
Adrenergic and anti-adrenergic drugs
Adrenergic and anti-adrenergic drugs

... ´ Effects include: increased BP, increased heart rate, relaxation of bronchial smooth muscle, vasoconstriction in peripheral blood vessels ...
Hypnotics and Sedatives
Hypnotics and Sedatives

... • Selectively blocks dopamine D2 receptors, avoiding nigrostriatal pathway • α-blockade • Also blocks H1 ...
Fatty acid amide hydrolase - The Scripps Research Institute
Fatty acid amide hydrolase - The Scripps Research Institute

... Over the past decade, great strides have been made in our understanding of the endogenous cannabinoid (endocannabinoid) system and its molecular constituents. In the early 1990s, two G-protein-coupled receptors (GPCRs), CB1 [1] and CB2 [2], were characterized that recognize D9-tetrahydrocannabinol ( ...
Designer Drugs
Designer Drugs

... “designer drug” was first coined by law enforcement in the 1980s second International Opium Convention in 1925 which specifically banned alternative esters of morphine 1960s - 1970s, new synthetic hallucinogens (modifications of LSD & PCP) 1980s - 1990s, design of MDMA (ecstasy) & methcathinone 2000 ...
Predicting new molecular targets for known drugs
Predicting new molecular targets for known drugs

... probably therapeutically essential6. Recent kinase drugs, such as Gleevec and Sutent, although perhaps designed for specificity, modulate several targets, and these ‘off-target’ activities may also be essential for efficacy7,8. Conversely, anti-Parkinsonian drugs such as Permax and Dostinex activate ...
kuliah farmakologi antidepresan
kuliah farmakologi antidepresan

... as alprazolam, and termination did not cause rebound anxiety symptoms because of clonazepam's long elimination half-life. ◦ Clonazepam displays low lipid solubility, it is less likely to cause anterograde amnesia compared to the other high-potency BZDs. For example, clonazepam is half as lipid solub ...
Toxicant – Receptor Interactions: Fundamental - UNC
Toxicant – Receptor Interactions: Fundamental - UNC

... From the viewpoint of biochemistry and neuroscience, “receptor” refers to a distinct class of molecules that have unique and characteristic functions and modes of action that involve endogenous ligands. Enzymes are, in one sense, receptors with respect to their substrates (and inhibitors, too). As w ...
Antipsychotics
Antipsychotics

... Injectable, conventional agents are typically used such as haloperidol 5-10 mg IM or zuclopenthixol acetate 50150mg It may be given every hour until  Acute symptoms are controlled  Side effects occur  Patient falls asleep ...
File
File

... • The nausea and vomiting produced by chemotherapeutic agents demands especially effective management. • Nearly 70% to 80% of patients who undergo chemotherapy experience nausea and/or vomiting. • Several factors influence the incidence and severity of chemotherapy-induced nausea and vomiting (CINV) ...
Medication Strategies for Behavior Patients Lynne Seibert DVM, MS
Medication Strategies for Behavior Patients Lynne Seibert DVM, MS

... Monoamine neurotransmitters (catecholamines and indoleamines) are related by their chemical structures, are concentrated in the midbrain, hypothalamus, and limbic system, and are stored in granular vesicles within axons and nerve terminals. The principle means of inactivation is by reuptake at the s ...
Anti-platelet agents
Anti-platelet agents

... • The peak inhibitory effect on platelet aggregation is apparent approximately one hour post-administration • Aspirin produces the irreversible inhibition of the enzyme cyclooxygenase and therefore causes irreversible inhibition of platelets for the rest of their lifespan (7 days) ...
Datasheet Blank Template - Santa Cruz Biotechnology
Datasheet Blank Template - Santa Cruz Biotechnology

... interacting with specific intracellular receptors to regulate gene expression. This superfamily of receptors includes both steroid and nonsteroid receptors. Like many nonsteroid hormone receptors, PXR (Pregnane X Receptor) binds as a heterodimer with RXR to a DNA sequence typical of a nonsteroid hor ...
Anti-psychotics
Anti-psychotics

... Subject selection limitation (most patients had no EPS/TD and those that had TD were assigned to second generation APDs only) ...
PWTherepeuticCannabis Fanciullo Slides
PWTherepeuticCannabis Fanciullo Slides

... inconsistently associated with cannabis use. A study of 65,855 members of a U.S. health management organization (HMO) that classified members as experimenters (six or fewer lifetime usages), former users, or current users found no increased risk of HNSCC, lung, colorectal, melanoma, or breast cancer ...
Evidence-Based Clinical Effects of Selective Estrogen Receptor
Evidence-Based Clinical Effects of Selective Estrogen Receptor

... has positive effects on the serum lipid profile. In reproductive tissues, however, raloxifene appears to behave as a very effective estrogen antagonist. Thus, the first significant step has been taken in bringing targeted, ER-active agents to specific groups of patients. This new therapy will help u ...
File
File

... • H1 blockers are competitive pharmacologic antagonists at H1receptor, these drugs have no effect on histamine release from storage sites. Because their structure closely resembles that of muscarinic blockers and alpha blockers, many of these agents are also pharmacologic antagonists at these recept ...
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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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