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the effects of zolmitriptan on nasal mucociliary clearance (nmcc)
the effects of zolmitriptan on nasal mucociliary clearance (nmcc)

... mechanism of stimulation of these ciliated cells activate transient receptor potential cation channel subfamily V member 4(TRPV4)like channel that elevate the intracellular Ca+ ,the channel opening require the activity of prostaglandin A2,so TRPV4 regarded as new target to consider in order to devel ...
SNPsWEB07
SNPsWEB07

... SNPS can have profound effects on drug responses ...
Cannabinoids for Gastrointestinal Diseases: Potential Therapeutic
Cannabinoids for Gastrointestinal Diseases: Potential Therapeutic

... are opposite to those produced by cannabinoid receptor agonists. These effects are not unequivocally attributable to displacement of endocannabinoids, as SR141716A behaves as an inverse agonist at the human cannabinoid CB 1 receptors [4-6]. ...
Delta-Opioid Ligands Reverse Alfentanil
Delta-Opioid Ligands Reverse Alfentanil

... of about 100-fold (Portoghese, 1991). TIPP(c) is the most selective delta antagonist; its selectivity for delta receptors is 10,000-fold over other receptors (Schiller et al., 1993). The poor receptor selectivity of delta drugs used in the past studies may have contributed to the disparate results c ...
Eliot Gardner, Ph.D. - Nysam
Eliot Gardner, Ph.D. - Nysam

... † AUC (0-15) P < 0.05 and # AUC (15-60) P < 0.001 for analgesics vs NaCl 0.9 % ...
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 ...
The Successful Treatment of Opioid Withdrawal
The Successful Treatment of Opioid Withdrawal

... 5-hydroxytryptophan (5-HTP) has not been studied in direct relation to relieving opioid withdrawal-induced muscle spasms, it has been shown to be an effective treatment of serotonin depletion and muscle spasms caused by withdrawal from 3,4-methylenedioxymethamphetamine (MDMA) (12-13). Reflecting on ...
Targeting the dopamine D receptor in schizophrenia
Targeting the dopamine D receptor in schizophrenia

... action of chlorpromazine in the 1960s and 1970s, many types of physiological and biochemical experiments were carried out. A variety of possible therapeutic targets were explored for the mode of action of chlorpromazine, including its action on mitochondrial enzymes, sodium–potassium-ATPase and rela ...
Anti-platelets
Anti-platelets

... • Cyclic peptide inhibitor of the fibrinogen binding site on GpIIb/IIIa receptor • Short duration of action: 6-12 hrs • Given with aspirin and heparin • Use: – Acute coronary syndrome – Angioplastic coronary interventions • Adverse effects: – Bleeding (10%) – Thrombocytopenia (0.5-1%) 3) Tirofiban • ...
Pharmacokinetic and pharmacodynamic profile of oral and
Pharmacokinetic and pharmacodynamic profile of oral and

... in two doses (0.25 and 0.5 mg/kg) in a placebocontrolled design. Behavioral responses; ACTH, cortisol, prolactin and MCPP blood level; temperature and pulse rate were measured over a 210-min period after administration of tablets. Non-linear doseresponse relationships between MCPP and ACTH, cortisol ...
A Dangerous Triad: Sertraline, Mirtazapine and Methadone
A Dangerous Triad: Sertraline, Mirtazapine and Methadone

... reaction firstly reported in the 1950’s in patients taking a monoamine oxidase (MAO) inhibitor called iproniazid in combination with pethidine. It was theorized that the reaction was due to overstimulation of 5-hydroxytryptamine (5-HT) receptors in the central nervous system due to the combined effe ...
What is the prognosis for new centrally-acting anti
What is the prognosis for new centrally-acting anti

... candidates that are currently at the pre-registration phase in the USA and review a wide range of novel compounds and drug targets that are in discovery or early clinical development. 2. A brief history of centrally-acting anti-obesity 2.1. The first generation of weight-loss drugs Anti-obesity drugs ...
Pharmacology of opioids
Pharmacology of opioids

... Opioids produce their actions at a cellular level by activating opioid receptors. These receptors are distributed throughout the central nervous system (CNS) with high concentrations in the nuclei of tractus solitarius, peri-aqueductal grey area (PAG), cerebral cortex, thalamus and substantia gelati ...
JWH018, a common constituent of Spice herbal blends, is a potent
JWH018, a common constituent of Spice herbal blends, is a potent

... The cannabinoid receptor 1 (CB1) cannabinoid receptor (nomenclature follows Alexander et al., 2008) has been identified as the receptor that mediates the behavioural effects of THC in animals (Monory et al., 2007) and likely does so in humans (Huestis et al., 2001). The CB1 receptor is predominately ...
Parazoanthoxanthin A blocks Torpedo nicotinic acetylcholine
Parazoanthoxanthin A blocks Torpedo nicotinic acetylcholine

... Nicotinic acetylcholine receptors (nAChRs) are ligand gated receptors that mediate signal transduction in chemical synapses in the central and peripheral nervous system [1,2]. Thus, they play a role in various nervous system-related disorders, such as Alzheimer’s disease, myasthenia gravis, schizoph ...
Slides - American Chemical Society
Slides - American Chemical Society

... Neuronal synaptic transmission involves: •neurotransmitter presynaptic release •receptor binding, binding site release, •and neurotransmitter degradation/reuptake Drug molecules “look like” natural substrates bind to receptor, transporter, or enzyme active sites ...
The UNSIN Report
The UNSIN Report

... inherent risk in increasing synaptic levels affinity, or low receptor expression. These of any neurotransmitter is the risk of it factors all contribute to decreased 5-HT1A binding to another receptor in the central activity in the OFC, therefore resulting in nervous system. For example, Prozac, agg ...
April 2017
April 2017

... Addiction is also defined many ways. The American Society of Addiction Medicine (ASAM) defines addiction as a primary, chronic, neurobiologic disease of brain motivation, reward, and memory with genetic, psychosocial, and environmental factors influencing its development and manifestations. The Amer ...
Stahl_3rd_ch04_Part2..
Stahl_3rd_ch04_Part2..

... neurotransmission is that the full array of downstream signal transduction is triggered by a full agonist (Figure 4-23). Thus, downstream proteins are maximally phosphorylated and genes are maximally affected. Loss of the agonist actions of a neurotransmitter at G protein-linked receptors, due to de ...
Click here for handout
Click here for handout

... antihelminthics for use in  farm animals and (1950s)  humans H Human use abandoned due  b d dd to “side effects” Introduced as potential  antidepressants (1970s) Abandoned as “too  amphetamine‐like” ...
2006_11_30-Lalani-Tox_3 - Calgary Emergency Medicine
2006_11_30-Lalani-Tox_3 - Calgary Emergency Medicine

... At high concentrations, open Cl- channel directly Will not require GABA presence to open channel NB! Propofol also works by opening the Cl channel ...
Nefazodone in the rat: mimicry and antagonism of [À]-DOM
Nefazodone in the rat: mimicry and antagonism of [À]-DOM

... venlafaxine, and citalopram, higher doses of nefazodone appear to reduce [ ]-DOM appropriate responding (Fig. 1). This biphasic effect of nefazodone was not predictable based on reports of nefazodone being a potent 5-HT2A antagonist (Taylor et al., 1995; Davis et al., 1997). More specifically, as th ...
Oral Small Molecule GLP-1 Receptor (GLP
Oral Small Molecule GLP-1 Receptor (GLP

Dopamine receptor agonist treatment of Parkinson`s disease
Dopamine receptor agonist treatment of Parkinson`s disease

... Parkinson’s disease is a progressive neurodegenerative disorder which affects approximately 1% of individuals over 60 years of age. There has been a growing interest in dopamine agonists as a form of treatment for this disease. The aims of this systematic review and metaanalysis were to establish th ...
Neuromuscular Blocking Agents
Neuromuscular Blocking Agents

... • Depolarizing Muscle relaxant – Prolonged depolarization causes relaxation due to the time limited lower gate on the sodium channel. – Gate cannot reopen until end plate repolarization – End plate cannot repolarize as long as muscle relaxant bind to ach receptor (Phase 1 block) – Prolonged end-plat ...
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5-HT2C receptor agonist

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