
07 Rhinitis & cough
... • Many of the 1st generation drugs have effects that are not mediated by H1- receptors. • Such as antimuscarinic activity, alpha adrenoceptors blocking, serotonin receptors antagonism & local anesthetic receptor sites. • Some of these actions are of therapeutic value & some are undesirable. ...
... • Many of the 1st generation drugs have effects that are not mediated by H1- receptors. • Such as antimuscarinic activity, alpha adrenoceptors blocking, serotonin receptors antagonism & local anesthetic receptor sites. • Some of these actions are of therapeutic value & some are undesirable. ...
Respiratory Pharmacology Week 4
... or β-adrenergic receptors. • Blood vessels: α1 couples to Gq, which results in increased intracellular Ca2+ which results in smooth muscle contraction. α2, on the other hand, couples to Gi, which causes a decrease of cAMP activity, resulting in e.g. smooth muscle contraction. • Heart/Lung: β recepto ...
... or β-adrenergic receptors. • Blood vessels: α1 couples to Gq, which results in increased intracellular Ca2+ which results in smooth muscle contraction. α2, on the other hand, couples to Gi, which causes a decrease of cAMP activity, resulting in e.g. smooth muscle contraction. • Heart/Lung: β recepto ...
TOPIC OUTLINE
... in the graph of H2 block indicate periods where Ach or gastrin released, such as during meal times. ...
... in the graph of H2 block indicate periods where Ach or gastrin released, such as during meal times. ...
2002
... The procedure for the alfentanil-trained monkeys is similar, but not identical. These animals are also trained and tested in a discrete, multiple-cycle procedure. The main difference between the alfentanil procedure and the EKC procedure is that the alfentanil monkeys are required to make 20 rather ...
... The procedure for the alfentanil-trained monkeys is similar, but not identical. These animals are also trained and tested in a discrete, multiple-cycle procedure. The main difference between the alfentanil procedure and the EKC procedure is that the alfentanil monkeys are required to make 20 rather ...
Bromo-DragonFly
... Bromo-DragonFly is a synthetic hallucinogen [1], also known as Bromo-DragonFLY, 3C-BromoDragonfly, DOB-Dragonfly and Br-DF. It is named after its molecular structure, which has an attached bromine atom and resembles a dragonfly. Bromo-DragonFly is a research chemical [2]. Very little reliable data i ...
... Bromo-DragonFly is a synthetic hallucinogen [1], also known as Bromo-DragonFLY, 3C-BromoDragonfly, DOB-Dragonfly and Br-DF. It is named after its molecular structure, which has an attached bromine atom and resembles a dragonfly. Bromo-DragonFly is a research chemical [2]. Very little reliable data i ...
Effects
... antagonist opposes the pharmacological action of the agonist. Competitive antagonism can be overcome by increasing the concentration of the agonist at the receptor site. (Example: Acetylcholine and atropine antagonism at muscarinic receptors). ...
... antagonist opposes the pharmacological action of the agonist. Competitive antagonism can be overcome by increasing the concentration of the agonist at the receptor site. (Example: Acetylcholine and atropine antagonism at muscarinic receptors). ...
Anxiety - Psychiatry Training
... Anxiety is…. • … a subjective experience of unpleasant anticipation, accompanied by characteristic behavioural and physiological responses (e.g. avoidance, vigilance and arousal) • Evolutionary value: to protect individuals from danger. • Present in most/?all higher animals – ? universal mechanism ...
... Anxiety is…. • … a subjective experience of unpleasant anticipation, accompanied by characteristic behavioural and physiological responses (e.g. avoidance, vigilance and arousal) • Evolutionary value: to protect individuals from danger. • Present in most/?all higher animals – ? universal mechanism ...
Opiates
... receptors, display in vivo binding preference for bendorphin, enkephalins, dynorphin and nociceptin/orphanin FQ, respectively. These are not completely selective for each type of receptor since the opioid peptides show a degree of sequence homology, although modified synthetic agonists are more selec ...
... receptors, display in vivo binding preference for bendorphin, enkephalins, dynorphin and nociceptin/orphanin FQ, respectively. These are not completely selective for each type of receptor since the opioid peptides show a degree of sequence homology, although modified synthetic agonists are more selec ...
Alpha Receptors, Beta Receptors, Kappa Receptors
... • Not only stimulates nicotinic receptors, it also triggers the release of endorphins and dopamine in the mesolimbic system of the brain • Pleasure, addiction and reward are the result • Also inhibitory transmitters are released, such as GABA, to reduce anxiety, lessening of irritation and aggressio ...
... • Not only stimulates nicotinic receptors, it also triggers the release of endorphins and dopamine in the mesolimbic system of the brain • Pleasure, addiction and reward are the result • Also inhibitory transmitters are released, such as GABA, to reduce anxiety, lessening of irritation and aggressio ...
Barbiturate
... - But it enzyme inducer so can be used for jaundice because it ↑ glucoronyl activity that responsible for conjugation of bilirubin. ...
... - But it enzyme inducer so can be used for jaundice because it ↑ glucoronyl activity that responsible for conjugation of bilirubin. ...
Farmacocinética
... Figure 4. Discoveries of G-protein-coupled receptor (GPCR) behavior through biochemical research conducted during the past 25 years. See the main text for specific de and examples. Abbreviations: RAMPs, receptor activity-modifying proteins; RCP, receptor component protein. ...
... Figure 4. Discoveries of G-protein-coupled receptor (GPCR) behavior through biochemical research conducted during the past 25 years. See the main text for specific de and examples. Abbreviations: RAMPs, receptor activity-modifying proteins; RCP, receptor component protein. ...
Schizophrenia II - Psychiatry Training
... • Atypical antipsychotic drugs – clozapine: antipsychotic without associated EPS or increases in serum prolactin; active at low levels of D2 occupancy (<60%) – “atypical” term later expanded to include its unique activity in treating treatmentresistant patients ...
... • Atypical antipsychotic drugs – clozapine: antipsychotic without associated EPS or increases in serum prolactin; active at low levels of D2 occupancy (<60%) – “atypical” term later expanded to include its unique activity in treating treatmentresistant patients ...
Pharmacology/Therapeutics II Block I Lectures
... KEY CONCEPTS AND LEARNING OBJECTIVES At the end of this lecture the learner will be able to: ...
... KEY CONCEPTS AND LEARNING OBJECTIVES At the end of this lecture the learner will be able to: ...
Pharmacology Block 3 Notes Autonomic Pharmacology I
... receptor’s activity (thus serving as an agonist); however when this receptor is activated, the activity of the neuron is decreased (generating an inhibitory effect) The receptor is thus an INHIBITORY RECEPTOR This is how molecules like GABA operate The goal of neurons (and neurotransmitters) is ...
... receptor’s activity (thus serving as an agonist); however when this receptor is activated, the activity of the neuron is decreased (generating an inhibitory effect) The receptor is thus an INHIBITORY RECEPTOR This is how molecules like GABA operate The goal of neurons (and neurotransmitters) is ...
- Opus
... BU08028 exhibits an extra-long duration of antinociceptive and antiallodynic actions, up to 30 h. To our knowledge, this is the sole analgesic with such a long duration of action in nonhuman primates. The high logP value of BU08028 could contribute to its unique pharmacokinetic profile (30, 38). Mor ...
... BU08028 exhibits an extra-long duration of antinociceptive and antiallodynic actions, up to 30 h. To our knowledge, this is the sole analgesic with such a long duration of action in nonhuman primates. The high logP value of BU08028 could contribute to its unique pharmacokinetic profile (30, 38). Mor ...
Elicited Behavior and Classical Conditioning
... Drugs or ligands that bind and are capable of changing the shape of the receptor protein and subsequently alter cell function are called agonists. The ligands that attach most readily are said to have high affinity for the receptor. Antagonists, in contrast, are capable of binding and may have high ...
... Drugs or ligands that bind and are capable of changing the shape of the receptor protein and subsequently alter cell function are called agonists. The ligands that attach most readily are said to have high affinity for the receptor. Antagonists, in contrast, are capable of binding and may have high ...
Heart Failure
... •Vasoconstriction by (-) enantiomer is countered by (+) enatiomer and 2 agonist activity- ultimate result is a decrease in PVR and mild decrease in systemic blood pressure ...
... •Vasoconstriction by (-) enantiomer is countered by (+) enatiomer and 2 agonist activity- ultimate result is a decrease in PVR and mild decrease in systemic blood pressure ...
Slide 1
... The role of Mg in blunting the intubation response is evolving: It has direct VD properties on coronary arteries and inhibiting CA release, thus attenuating the hemodynamic effects during endotracheal intubation. Beside its role in blunting the pressor response to intubation , it also produce ...
... The role of Mg in blunting the intubation response is evolving: It has direct VD properties on coronary arteries and inhibiting CA release, thus attenuating the hemodynamic effects during endotracheal intubation. Beside its role in blunting the pressor response to intubation , it also produce ...
Pharmacology of the Autonomic Nervous System
... D. Synthesis and Metabolism of Catecholamines Tyrosine in the bloodstream is taken up into nerves and converted into catecholamine. The five main enzymes whose functions are critical to the formation of catecholamines are discussed below (Figure 6). Tyrosine hydroxylase (tyrosine to dopa) is the rat ...
... D. Synthesis and Metabolism of Catecholamines Tyrosine in the bloodstream is taken up into nerves and converted into catecholamine. The five main enzymes whose functions are critical to the formation of catecholamines are discussed below (Figure 6). Tyrosine hydroxylase (tyrosine to dopa) is the rat ...
Respiratory drugs - Suny-perfusion
... B. Anticholinergic bronchodilators 1. muscarinic receptors • The lung is innervated not only by sympathetic nerve fibers (the blood vessels and glands of the lungs), but also by parasympathetic nerve fibers (the mucous glands and smooth muscle). ...
... B. Anticholinergic bronchodilators 1. muscarinic receptors • The lung is innervated not only by sympathetic nerve fibers (the blood vessels and glands of the lungs), but also by parasympathetic nerve fibers (the mucous glands and smooth muscle). ...
Revisiting AMPA Receptors as an Antiepileptic Drug Target
... ligands that selectively activated them. An additional potent excitatory amino acid was α-amino-3-hydroxyl-5-methyl-4isoxazole-propionic acid (AMPA), which was synthesized by Krogsgaard-Larsen as an analog of ibotenic acid and found to excite neurons through non-NMDA receptors that seemed to be dist ...
... ligands that selectively activated them. An additional potent excitatory amino acid was α-amino-3-hydroxyl-5-methyl-4isoxazole-propionic acid (AMPA), which was synthesized by Krogsgaard-Larsen as an analog of ibotenic acid and found to excite neurons through non-NMDA receptors that seemed to be dist ...
Revisiting AMPA receptors as an antiepileptic drug target
... ligands that selectively activated them. An additional potent excitatory amino acid was α-amino-3-hydroxyl-5-methyl-4isoxazole-propionic acid (AMPA), which was synthesized by Krogsgaard-Larsen as an analog of ibotenic acid and found to excite neurons through non-NMDA receptors that seemed to be dist ...
... ligands that selectively activated them. An additional potent excitatory amino acid was α-amino-3-hydroxyl-5-methyl-4isoxazole-propionic acid (AMPA), which was synthesized by Krogsgaard-Larsen as an analog of ibotenic acid and found to excite neurons through non-NMDA receptors that seemed to be dist ...
Cannabinoids in bipolar affective disorder: a review and
... 2003; Surguladze et al., 2003). CB1 receptors belong to a family of G-protein coupled receptors that includes receptors for aminergic neurotransmitters (noradrenaline, dopamine, serotonin and acetylcholine) and act through second messenger systems. CB2 receptors are similar to CB1 receptors but are ...
... 2003; Surguladze et al., 2003). CB1 receptors belong to a family of G-protein coupled receptors that includes receptors for aminergic neurotransmitters (noradrenaline, dopamine, serotonin and acetylcholine) and act through second messenger systems. CB2 receptors are similar to CB1 receptors but are ...
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.