1-naphthylpiperazine
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1-naphthylpiperazine
1-(1-Naphthyl)piperazine (1-NP) is a drug which is a phenylpiperazine derivative. It acts as a non- selective, mixed serotonergic agent, exerting partial agonism at the 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, and 5-HT1F receptors, while antagonizing the 5-HT2A, 5-HT2B, and 5-HT2C receptors. It has also been shown to possess high affinity for the 5-HT3, 5-HT5A, 5-HT6, and 5-HT7 receptors, and may bind to 5-HT4 and the SERT as well. In animals it produces effects including hyperphagia, hyperactivity, and anxiolysis, of which are all likely mediated predominantly or fully by blockade of the 5-HT2C receptor. Derivatives of naphthylpiperazine include CSP-2503, F-11,461, S-14506, and S-14671. See also * 1-(2-Naphthyl)piperazine (2-NP) * Substituted piperazine * Diphenylpiperazine * Phenylpiperazine * Quipazine Quipazine, also known as 1-(2-quinolinyl)piperazine (2-QP), is a serotonin, serotonergic drug of the arylpiperazine family and an structural analog, analogue ...
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Drug
A drug is any chemical substance other than a nutrient or an essential dietary ingredient, which, when administered to a living organism, produces a biological effect. Consumption of drugs can be via insufflation (medicine), inhalation, drug injection, injection, smoking, ingestion, absorption (skin), absorption via a dermal patch, patch on the skin, suppository, or sublingual administration, dissolution under the tongue. In pharmacology, a drug is a chemical substance, typically of known structure, which, when administered to a living organism, produces a biological effect. A pharmaceutical drug, also called a medication or medicine, is a chemical substance used to pharmacotherapy, treat, cure, preventive healthcare, prevent, or medical diagnosis, diagnose a disease or to promote well-being. Traditionally drugs were obtained through extraction from medicinal plants, but more recently also by organic synthesis. Pharmaceutical drugs may be used for a limited duration, or on a re ...
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5-HT5A Receptor
5-Hydroxytryptamine (serotonin) receptor 5A, also known as HTR5A, is a protein that in humans is encoded by the ''HTR5A'' gene. Agonists and Receptor antagonist, antagonists for 5-HT receptors, as well as serotonin uptake inhibitors, present promnesic (memory-promoting) and/or anti-amnesic effects under different conditions, and 5-HT receptors are also associated with neural changes. Function The gene described in this record is a member of 5-HT receptor, 5-hydroxytryptamine receptor family and encodes a multi-pass membrane protein that functions as a receptor for 5-hydroxytryptamine and couples to G proteins, negatively influencing cAMP levels via Gi and Go. This protein has been shown to function in part through the regulation of intracellular Ca2+ mobilization. The 5-HT5A receptor has been shown to be functional in a native expression system. Rodents have been shown to possess two functional 5-HT5 receptor subtypes, 5-HT5A and 5-HT5B, however while humans possess a gene cod ...
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S-14671
S-14671 is a naphthylpiperazine derivative which acts as a 5-HT1A receptor agonist (pKi = 9.3) with high efficacy and exceptional ''in vivo'' potency, and also as a 5-HT2A and 5-HT2C receptor antagonist (both are pKi = 7.8). It displays only low and non-significant affinity for 5-HT1B and 5-HT3 sites. In producing 5-HT1A-mediated effects such as hypothermia and spontaneous tail flicks in rodents, S-14671 is active at doses as low as 5 μg subcutaneously, and is about 10-fold more potent than 8-OH-DPAT and 100-fold more potent than flesinoxan and buspirone. Other 5-HT1A-mediated effects of S-14671 include induction of flat-body posture, corticosterone secretion, inhibition of morphine-induced antinociception, and attenuation of the electrical activity of the dorsal raphe nucleus. S-14671 has been found to possess powerful efficacy in the rodent forced swim test and in the pigeon conflict test, indicating marked antidepressant and anxiolytic effects, respectively, of ...
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S-14506
S-14,506 is a naphthylpiperazine, a 5-HT1A receptor agonist, and a dopamine receptor antagonist. See also * Naphthylpiperazine Naphthylpiperazine (NP) may refer to: * 1-(1-Naphthyl)piperazine (1-NP) * 1-(2-Naphthyl)piperazine (2-NP) Arylpiperazines Naphthalenes {{Short pages monitor [Baidu]  


CSP-2503
CSP-2503 is a potent and selective 5-HT1A receptor agonist, 5-HT2A receptor antagonist, and 5-HT3 receptor antagonist of the naphthylpiperazine class. First synthesized in 2003, it was designed based on computational models and QSAR studies. In rat studies, CSP-2503 has demonstrated anxiolytic effects, and thus has been suggested as a treatment for anxiety in humans with a multimodal mechanism of action In pharmacology, the term mechanism of action (MOA) refers to the specific biochemical Drug interaction, interaction through which a Medication, drug substance produces its pharmacological effect. A mechanism of action usually includes mention o .... See also * Naphthylpiperazine * S-14,671 * S-14,506 References {{Piperazines Diketopiperazines Experimental drugs Lactams 1-(1-Naphthyl)piperazines Pyrrolopyrazines ...
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Chemical Derivative
In chemistry, a derivative is a compound that is derived from a similar compound by a chemical reaction. In the past, derivative also meant a compound that ''can be imagined to'' arise from another compound, if one atom or group of atoms is replaced with another atom or group of atoms, but modern chemical language now uses the term structural analog for this meaning, thus eliminating ambiguity. The term "structural analogue" is common in organic chemistry. In biochemistry, the word is used for compounds that at least theoretically can be formed from the precursor compound. Chemical derivatives may be used to facilitate analysis. For example, melting point (MP) analysis can assist in identification of many organic compounds. A crystalline derivative may be prepared, such as a semicarbazone or 2,4-dinitrophenylhydrazone (derived from aldehydes or ketones), as a simple way of verifying the identity of the original compound, assuming that a table of derivative MP values is availa ...
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Anxiolysis
An anxiolytic (; also antipanic or anti-anxiety agent) is a medication or other intervention that reduces anxiety. This effect is in contrast to anxiogenic agents which increase anxiety. Anxiolytic medications are used for the treatment of anxiety disorders and their related psychological and physical symptoms. Nature of anxiety Anxiety is a naturally-occurring emotion and response. When anxiety levels exceed the tolerability of a person, anxiety disorders may occur. People with anxiety disorders can exhibit fear responses, such as defensive behaviors, high levels of alertness, and negative emotions. Those with anxiety disorders may have concurrent psychological disorders, such as depression. Anxiety disorders are classified using six possible clinical assessments: Different types of anxiety disorders will share some general symptoms while having their own distinctive symptoms. This explains why people with different types of anxiety disorders will respond differently to diffe ...
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Pakistan Journal Of Pharmaceutical Sciences
The ''Pakistan Journal of Pharmaceutical Sciences'' is a bimonthly peer-reviewed open access medical journal covering pharmaceutical sciences. It was established in 1988 and is published by the Faculty of Pharmacy, University of Karachi. The editor-in-chief is Iqbal Azhar (University of Karachi). According to the ''Journal Citation Reports'', the journal has a 2015 impact factor The impact factor (IF) or journal impact factor (JIF) of an academic journal is a type of journal ranking. Journals with higher impact factor values are considered more prestigious or important within their field. The Impact Factor of a journa ... of 0.581. References External links * * * Pharmacology journals English-language journals Academic journals established in 1988 Bimonthly journals University of Karachi Academic journals of Pakistan {{Pharma-journal-stub ...
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Hyperactivity
Attention deficit hyperactivity disorder (ADHD) is a neurodevelopmental disorder characterised by symptoms of inattention, hyperactivity, impulsivity, and emotional dysregulation that are excessive and pervasive, impairing in multiple contexts, and developmentally inappropriate. ADHD symptoms arise from executive dysfunction. Impairments resulting from deficits in self-regulation such as time management, inhibition, task initiation, and sustained attention can include poor professional performance, relationship difficulties, and numerous health risks, collectively predisposing to a diminished quality of life and a reduction in life expectancy. As a consequence, the disorder costs society hundreds of billions of US dollars each year, worldwide. It is associated with other mental disorders as well as non-psychiatric disorders, which can cause additional impairment. While ADHD involves a lack of sustained attention to tasks, inhibitory deficits also can lead to diffic ...
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Hyperphagia
Polyphagia, or hyperphagia, is an abnormally strong, incessant sensation of hunger or desire to eat often leading to overeating. In contrast to an increase in appetite following exercise, polyphagia does not subside after eating and often leads to rapid intake of excessive quantities of food. Polyphagia is not a disorder by itself; rather, it is a symptom indicating an underlying medical condition. It is frequently a result of abnormal blood glucose levels (both hyperglycemia and hypoglycemia), and, along with polydipsia and polyuria, it is one of the "3 Ps" commonly associated with uncontrolled diabetes mellitus. Etymology The word ''polyphagia'' () uses combining forms of '' poly-'' + '' -phagia'', from the Greek words πολύς (polys), "very much" or "many", and φᾰ́γω (phago), "eating" or "devouring". Underlying conditions and possible causes Polyphagia is one of the most common symptoms of diabetes mellitus. It is associated with hyperthyroidism and endocrine di ...
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Serotonin Transporter
The serotonin transporter (SERT or 5-HTT) also known as the sodium-dependent serotonin transporter and solute carrier family 6 member 4 is a protein that in humans is encoded by the SLC6A4 gene. SERT is a type of monoamine transporter protein that transports the neurotransmitter serotonin from the synaptic cleft back to the presynaptic neuron, in a process known as serotonin reuptake. This transport of serotonin by the SERT protein terminates the action of serotonin and recycles it in a sodium-dependent manner. Many antidepressant medications of the SSRI and tricyclic antidepressant classes work by binding to SERT and thus reducing serotonin reuptake. It is a member of the sodium:neurotransmitter symporter family. A repeat length polymorphism in the promoter of this gene has been shown to affect the rate of serotonin uptake and may play a role in sudden infant death syndrome, aggressive behavior in Alzheimer disease patients, post-traumatic stress disorder and depression ...
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