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Enhancing Cannabinoid Neurotransmission
Enhancing Cannabinoid Neurotransmission

... animals showed decreased shock-induced reinstatement of fear. Control experiments demonstrated that the effects of AM404 could not be attributed to alterations in the expression of conditioned fear, locomotion, shock reactivity, or baseline startle, as these parameters seemed unchanged by AM404. Fur ...
Effects of Δ9-tetrahydrocannabinol on reward and anxiety in rats
Effects of Δ9-tetrahydrocannabinol on reward and anxiety in rats

... long × 10 cm wide) and two enclosed arms (50 × 10 × 40 cm) extended from a common central platform (10 × 10 cm), based on a design validated by Lister (1987). The maze was constructed of blond varnish-painted wood, elevated to a height of 74 cm above floor level. The enclosed arms were surrounded by ...
Dear Parents of A Smith, Your child currently has a final 9
Dear Parents of A Smith, Your child currently has a final 9

... b. MOA for prevention of migraine no fully understood- may stabilize seroternergic neurotransmission by anatagonizing down regulation of 5-HT2 receptors c. Examples i. Selective serotonin reuptake inhibitors (SSRI) (Prozac and others) 1. More efficacious with migraines associated with depression- in ...
hypertension
hypertension

... data on prognostic benefits, if any, of clonidine. At present, it is occasionally used in combination with a diuretic.  Clonidine has also facilitated alcohol withdrawal and smoking cessation. ADR:  Orthostatic hypotension  Sedation  Rebound effect ...
IDENTIFICATION OF DUAL AGONISTIC NOVEL LIGANDS FOR INSULIN RECEPTOR AND... THROUGH MOLECULAR DOCKING
IDENTIFICATION OF DUAL AGONISTIC NOVEL LIGANDS FOR INSULIN RECEPTOR AND... THROUGH MOLECULAR DOCKING

... triacetate, gymnemic diacetate, gymnemic triacetate and gallic acid are satisfying the Lipinski properties. One of the most daunting steps for a drug candidate is having favorable ADMET characteristics. Prentis et al., (1988)20 suggested that optimizing these properties during early drug discovery i ...
skeletal muscle relaxants
skeletal muscle relaxants

... B) Centrally acting (spasmolytic drugs) Diazepam ( act through GABA A) receptors) Baclofen (GABA B) receptors Dantroline ( act directly by interfering release of ...
Functional Characterization of GABAA Receptors in Neonatal
Functional Characterization of GABAA Receptors in Neonatal

... molecular architecture of native GABAA receptors is extremely heterogeneous (Bonnert et al. 1999; Hevers and Lüddens 1998). Pharmacological studies of recombinant receptors have shown that individual subunits and their subtypes confer different sensitivities to GABAA receptor modulators (Hevers and ...
5-Hydroxytryptamine2C Receptor Contribution to m
5-Hydroxytryptamine2C Receptor Contribution to m

... Animal Surgery and Preparation. All procedures were approved by the Vanderbilt University Medical Center Institutional Animal Care and Use Committees and were conducted according to the NIH Guide for the Care and Use of Laboratory Animals. Adult male Sprague-Dawley rats (n ⫽ 6 per group) were housed ...
Heart Failure
Heart Failure

... •Reduces both right and left ventricular afterload by reducing pulmonary and systemic vascular resistance •Results in increased cardiac output and decreased ventricular wall stress during systole •Also has moderate direct positive inotropic activity independent of its afterload reducing effects •Red ...
[ PDF ] - journal of evolution of medical and dental sciences
[ PDF ] - journal of evolution of medical and dental sciences

... Iloperidone, a new dopamine type 2/serotonin type 2A antagonist provides better efficacy with less extra-pyramidal symptoms than D2 receptor antagonist antipsychotics. Iloperidone additionally has high affinity for alpha1 receptors and moderate affinity for alpha-2C receptors.2,3 Despite this knowle ...
Thromboxane Receptors Antagonists and/or Synthase Inhibitors
Thromboxane Receptors Antagonists and/or Synthase Inhibitors

... Western countries. Several clinical conditions are characterized by increased incidence of cardiovascular events and enhanced thromboxane (TX)-dependent platelet activation. Enhanced TX generation may be explained by mechanisms relatively insensitive to aspirin. More potent drugs possibly overcoming ...
Nefazodone in the rat: mimicry and antagonism of [À]-DOM
Nefazodone in the rat: mimicry and antagonism of [À]-DOM

... altered, relative to dose, by pretreatment with the monoamine reuptake inhibitor, nefazodone. Similar to ( ± ) fluoxetine, fluvoxamine, and venlafaxine (Winter et al., 1999a), the enhancement of [ ]-DOM-induced stimulus control occurs in the presence of significant partial substitution by nefazodone ...
Hallucinogens - WordPress.com
Hallucinogens - WordPress.com

... • DRN activity does not correlate well with behavioral effects of LSD • A group of 5-HT1 agonists (e.g. buspirone) are anxiolytics, not hallucinogens • 5-HT-like and catecholamine-like hallucinogen potency correlates with 5-HT2a affinity • Downregulation/desensitization/blockade of 5-HT2a receptors ...
PowerPoint Presentation - Lecture 9
PowerPoint Presentation - Lecture 9

... aldosterone & Na excreted, but H2O & K retained - Used to treat HTN primarily, - but not a 1st line drug. Also used in heart failure. - SE = hyperkalemia & 1st dose hypotension (more common with comb. Diuretic & ACE inhibitor. ...
Neurotransmitters
Neurotransmitters

... • DRN activity does not correlate well with behavioral effects of LSD • A group of 5-HT1 agonists (e.g. buspirone) are anxiolytics, not hallucinogens • 5-HT-like and catecholamine-like hallucinogen potency correlates with 5-HT2a affinity • Downregulation/desensitization/blockade of 5-HT2a receptors ...
Research advances in basic mechanisms of seizures and
Research advances in basic mechanisms of seizures and

... Epilepsy is a common neurological disease but the mechanism of seizure generation has been only partially unraveled. Furthermore, almost 30% of epileptic patients are resistant to pharmacological treatment. Therefore, elucidation of the basic mechanism of seizures and search for new antiepileptics i ...
Marijuana
Marijuana

... Addiction can occur to THC, but only at dose and use levels far above what is now used recreationally. ...
RT101 Basic Therapeutics
RT101 Basic Therapeutics

... drug must be increased (over time) to obtain the desired effect -or- a decreasing intensity of responsiveness to a drug over time Tachyphylaxis: Rapidly developing tolerance to a drug -or- a rapid decrease in responsiveness to a drug. Additive effects: The effect of two chemicals acting simultaneous ...
Oncostatin`s LIFR sentence
Oncostatin`s LIFR sentence

... group of Australian researchers has found a ligand, oncostatin M, that can elicit bone formation when it binds to a receptor called LIFR or bone resorption when it binds to another receptor called OSMR.1 The challenge will be to develop small molecules that are selective enough to agonize the intera ...
Alterations in Cardiovascular Function:
Alterations in Cardiovascular Function:

... REDUCE HEART RATE as well as blood pressure! ...
Adverse reactions
Adverse reactions

... the mechanism of action of antipsychotic drugs: 1) Mesolimbic-mesocortical pathway: the one most closely related to behavior and psychosis 2) Nigrostriatal pathway: it is involved in the coordination of voluntary movement. Blockade of the D2 receptors in the nigrostriatal pathway is responsible for ...
Estrogen receptor modulators and down regulators
Estrogen receptor modulators and down regulators

... • Tamoxifen should not be administered with anastrozole. Concurrent use decreased anastrozole plasma levels by 27%.The combination had no efficacy benefit when compared to tamoxifen administration alone. Tamoxifen pharmacokinetics were not affected. • Tamoxifen enhance anticoagulant effect of coumar ...
Parazoanthoxanthin A blocks Torpedo nicotinic acetylcholine
Parazoanthoxanthin A blocks Torpedo nicotinic acetylcholine

... ParaA and tacrine are structurally similar, and both substances are anticholinesterase agents. It is also possible that they could similarly modify nAChR responses. This view is supported by the observation that tacrine shortens the open time of nAChR, meaning that it is an open channel blocker [20] ...
as a PDF
as a PDF

... been found after long-term treatment with various antidepressants 3°. These findings have led to the suggestion that an excess of 5-HT at some receptors, probably the 5-HT 2 type, could be involved in depressive illness. The 5-HT1A agonist 8-OH-DPAT has been found to selectively reduce brain 5-HT sy ...
toxicology 3 - Calgary Emergency Medicine
toxicology 3 - Calgary Emergency Medicine

... – Used to be given as cocktail and that’s when people ran into problems – Can precipitate Sz / cholinergic symptoms. ...
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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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