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Screening for Hormone-Like Therapeutic Compounds.pdf
Screening for Hormone-Like Therapeutic Compounds.pdf

... with the ability to modulate these targets could lead to the development of valuable therapeutics against serious pathological conditions. Typical methods for identifying these compounds have included engineered in vivo reporter systems, as well as in vitro receptor binding assays. More recently, sm ...
I. The direct-acting drugs
I. The direct-acting drugs

Evidence for the Existence of Nonmonotonic Dose
Evidence for the Existence of Nonmonotonic Dose

... for receptor occupancy theory to accurately describe the concentration response relationships for many drug, natural and synthetic compounds • Many natural or synthetic compounds (i.e. EDCs) are likely nonselective or have variably selectivity for different receptors • Not pre-screened for a recepto ...
Antidepressant, Anti-anxiety Drugs
Antidepressant, Anti-anxiety Drugs

... Almost all NE pathways in the brain originate from the cell bodies of neuronal cells in the locus coereleus in the midbrain, which send their axons diffusely to the cortex, cerebellum and limbic areas (hippocampus, amygdala, hypothalamus, thalamus).  Mood: -- higher functions performed by the cort ...
Lamb Mechanisms Drug Action
Lamb Mechanisms Drug Action

... Hormones, Steroids, Vitamins and Neurotransmitters alter cell functions by interacting with cellular receptors. ...
The Atypical Antipsychotics
The Atypical Antipsychotics

... They are considered atypical in the way they affect dopamine and serotonin neurotransmission in the four key dopamine pathways in the brain. Mechanism of action Dopamine receptor blocking activity in the brain:. D1 and D5 receptors activate adenylyl cyclase, often exciting neurons, whereas D2, D3 an ...
药理概论1
药理概论1

...  An adaptive state that develops in response to repeated drug administration.  Psychologic dependence is manifested by compulsive drugseeking behavior.  Physiologic dependence is present when withdrawal of drug produces symptoms and signs.  Drug addiction is defined as the compulsive, out-of-con ...
Memantine and Neuroprotection
Memantine and Neuroprotection

... restlessness/ agitation (@ higher doses: 40– 60 mg/ day). Memantine work better for severe conditions. ◦ Neuropathic pain ◦ Alzheimer’s disease: FDA approval for moderateto-severe disease. ...
Important side effects to be considered when choosing antipsychotic
Important side effects to be considered when choosing antipsychotic

...  Dopamine receptor blocking activity in the brain:. D1 and D5 receptors activate adenylyl cyclase, often exciting neurons, whereas D2, D3 and D4 receptors inhibit adenylyl cyclase, or mediate membrane K+ channel opening leading to neuronal hyperpolarization. The neuroleptic drugs bind to these rece ...
Sympatholytics
Sympatholytics

... tends to cause blood to pool in the lower extremities. However, several reflexes, including sympathetically mediated venoconstriction minimize this pooling and maintain cerebral perfusion. If these reflex actions do not occur, then orthostatic hypotension could result. ...
Autacoids
Autacoids

... Antimuscarinic effects, e.g. dry mouth, urinary retention, & constipation ...
Mechanisms of drug action
Mechanisms of drug action

... breathing difficulty The drug used,salbutamol is a B2 receptor agonist that bind B2 receptors and act on them to cause bronchodilatation ...
Document
Document

... immune active cells (such as T cells, neutrophils, and eosinophils), “which suggests an important role for H4 receptors in the regulation of immune function”. ...
مهم
مهم

... 2. Promotion of norepinephrine release  acting on terminals of sympathetic nerves to cause release of NE 3. Blockade of norepinephrine reuptake  blocking NE reuptake cause NE to accumulate within the synaptic gap, and thereby increase receptor activation. 4. Inhibition of norepinephrine inactivati ...
T5_a: High resolution copy of the slides of the talk
T5_a: High resolution copy of the slides of the talk

... Abuse: ‐ typical disco‐drug ‐ when sleeping is not possible/wanted : truck drivers, artists Effects: ‐ hyperactivity ‐ physical and mental productivity increases ‐ demand for sleeping decreases ‐ iv „rush” Overdose: ‐ sy stimulation ‐ disorientation ‐ long term: destruction of dopaminergic pathways  ...
receptors
receptors

... Caffeine’s actions resemble those of amphetamines – fatigue disappears, mood improves, and sociability is enhanced. It is very likely that new substances will be synthesized in the future that have similar desirable effects. Would these developments alter our tendency to put judgmental labels on com ...
Kinetics of metoclopramide effects on human 5
Kinetics of metoclopramide effects on human 5

... current suppression by 200 nM metoclopramide, Fig. I). Therefore, persuasive evidence that metoclopramide inhibits radioligand binding of specific 5-HT3 receptor antagonists and contrasting reports of 5-HT3 antagonists acting via non-competitive mechanisms (for review, See [2]) need not be a contrad ...
Autonomic Nervous System
Autonomic Nervous System

... mood inappropriation, paranoia (persecution mania) and hallucinations (voices) and Negative symptoms: withdrawal from society, flattened emotional responses, defect in selective attention (can’t distinguish between important and insignificant) Affects up to 1% of population, high suicide rate (10%) ...
Physiological Antagonism between 5
Physiological Antagonism between 5

... Glutamate Receptors in Prefrontal Cortex1 5-Hydroxytryptamine2A (5-HT2A) receptor antagonists block the psychotomimetic effects of hallucinogens in humans (Vollenweider et al., 1998) and are thought to contribute to the therapeutic effects of atypical ntidepressant/antipsychotic drugs (Kroeze and Ro ...
CNS Neurotransmitters
CNS Neurotransmitters

... • It is the GluR2 subunit that makes most AMPA receptors Ca++ impermeant • The GluR2 subunit contains one amino acid substitution : arginine (R) versus glutamine (Q) in all other GluRs ...
Lecture 14
Lecture 14

... mood inappropriation, paranoia (persecution mania) and hallucinations (voices) and Negative symptoms: withdrawal from society, flattened emotional responses, defect in selective attention (can’t distinguish between important and insignificant) Affects up to 1% of population, high suicide rate (10%) ...
Document
Document

181lec5
181lec5

... G protein coupled to 2nd messenger system  effector is enzyme that promotes formation of intracellular “second messenger” ...
Depression and anxiety Lou haiyan(娄海燕)
Depression and anxiety Lou haiyan(娄海燕)

...  Relieves anxiety without producing sedation, impairment of motor skills, or memory loss.  Does not induce withdrawal symptoms upon discontinuation.  Does not act immediately.  Can take up to 1 week to become effective.  Used for chronic anxiety states. ...
Sample question
Sample question

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5-HT2C receptor agonist

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