Purpose: Sarpogrelate hydrochloride, a selective 5-hydroxytryptamine 2A antagonist, is a widely used antiplatelet agent for the treatment of peripheral arterial disease (PAD). DP-R202 is a new sarpogrelate hydrochloride product with an improved dosage regimen compared with the agent in current use. The aim of this study was to compare the efficacy and safety profile of DP-R202 and Anplag* Tab in patients with PAD. Methods: This study was a 12-week, multicenter, randomized, double-blinded, active-controlled, parallel group comparative Phase III clinical trial. One hundred fifty-one volunteer patients with PAD were randomized to receive DP-R202 300 mg once daily or Anplag Table 100 mg TID for 12 weeks. The primary end point was a change in patient assessment of lower leg pain intensity with the use of a visual analog scale (VAS) after 12 weeks of treatment. Results after 4, 8, and 12 weeks of treatment were compared with baseline and between treatment groups, and all patients were assessed for ...
This study investigated the effect of sarpogrelate hydrochloride on the disposition of metoprolol tartrate in healthy male volunteers.
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I have a drug that reduces the level of a certain gene X when compared to control. Now, when I used the antagonist of the drug along with the drug itself, I see a huge increase in the mRNA levels of this gene, even higher than control itself. I know for sure that this antagonist does not have any inverse agonist activity. What other reasons could there be for this effect ...
Choosing to participate in a study is an important personal decision. Talk with your doctor and family members or friends about deciding to join a study. To learn more about this study, you or your doctor may contact the study research staff using the contacts provided below. For general information, Learn About Clinical Studies. ...
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Serotonin 5-HT2 receptors are stimulated by monoamine neurotransmitters including serotonin, dopamine and norepinephrine. 5-HT2 receptor stimulation causes a buildup of intracellular inositol triphosphate and thereby an increase of cytosolic Ca2+. 5-HT2C receptor agonists are attractive drug targets that have potential use in the treatment of a number of conditions including obesity, psychiatric disorders, sexual dysfunction and urinary incontinence. The 5-HT2C receptors are one of three subtypes that belong to the serotonin 5-HT2 receptor subfamily along with 5-HT2A and 5-HT2B receptors. The development of 5-HT2C agonists has been a major obstacle, because of severe side effects due to a lack of selectivity over 5-HT2A and 5-HT2B receptors. Activation of 5-HT2A receptors can induce hallucinations, and the activation of 5-HT2B receptors has been implicated in cardiac valvular insufficiency and possibly in pulmonary hypertension. In the late 1960s, non-selective serotonin receptor antagonists ...
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Risperidone 6mg. Pimavanserin, a selective serotonin (5-HT)2A-inverse agonist, enhances the efficacy and safety of risperidone, 2mg/day, but does not enhance efficacy of haloperidol.
The IUPHAR/BPS Guide to Pharmacology. amoxapine ligand page. Quantitative data and detailed annnotation of the targets of licensed and experimental drugs.
Sarpogrelate (brand name Anplag; former developmental code names MCI-9042, LS-187,118) is a drug which acts as an antagonist at the 5HT2A and 5-HT2B receptors. It blocks serotonin-induced platelet aggregation, and has applications in the treatment of many diseases including diabetes mellitus, Buergers disease, Raynauds disease, coronary artery disease, angina pectoris, and atherosclerosis. Naftidrofuryl Pertz H, Elz S. In-vitro pharmacology of sarpogrelate and the enantiomers of its major metabolite: 5-HT2A receptor specificity, stereoselectivity and modulation of ritanserin-induced depression of 5-HT contractions in rat tail artery. Journal of Pharmacy and Pharmacology. 1995 Apr;47(4):310-6. PMID 7791029 Nishio H, Inoue A, Nakata Y. Binding affinity of sarpogrelate, a new antiplatelet agent, and its metabolite for serotonin receptor subtypes. Archives Internationales de Pharmacodynamie et de Thérapie. 1996 Mar-Apr;331(2):189-202. PMID 8937629 Muntasir HA, Hossain M, Bhuiyan MA, Komiyama T, ...
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BERRO, LAIS F.... Effects of the serotonin 2C receptor agonist WAY163909 on the abuse-related effects and mesolimbic dopamine neurochemistry induced by abused stimulants in rhesus monkeys. Psychopharmacology 234 n.17 p. 2607-2617 SEP 2017. Journal article.
Overview. Benzodiazepine (BZD) drugs increase the inhibitory effects of gamma-aminobutyric acid (GABA) interneurons on cholinergic neurons. However, BZD drugs
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YM-348 je lek sa indazolnim osnovom koji deluje kao potentan i selektivan agonist 5-HT2C receptor, sa EC50 vrednošću od 1 nM i 15x selektivnošću u odnosu na 5-HT2A. On je umereno selektivan 3x u odnosu na blisko srodni 5-HT2B receptor.[1][2] On ispoljava termogeno i anoreksično dejsto u životinjskim studijama, što ga čini potencijalno korisnim u lečenju gojaznosti.[3][4][5][6] ...
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5-HT1 receptori su potfamilija 5-HT receptora koji vezuju endogeni neurotransmiter serotonin (5-hidrokstriptamin, 5-HT).[1] 5-HT1 potfamilija sadrži pet G protein-spregnutih receptora koji vezuju Gi/Go i posreduju inhibitornu neurotransmisiju.[2] Ova grupa obuhvata 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, i 5-HT1F. Ne postoji 5-HT1C receptor, jer je njegova klasifikacija promenjena u 5-HT2C receptor. ...
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When DArcy Wentworth Thompsons On Growth and Form was published 100 years ago, it raised the question of how biological forms arise during development and across evolution. In light of the advances in molecular and cellular biology since then, a succinct modern view of the question states: how do genes encode geometry? Our new special issue is packed with articles that use mathematical and physical approaches to gain insights into cell and tissue patterning, morphogenesis and dynamics, and that provide a physical framework to capture these processes operating across scales.. Read the Editorial by guest editors Thomas Lecuit and L. Mahadevan, as they provide a perspective on the influence of DArcy Thompsons work and an overview of the articles in this issue.. ...
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collecting cells HT1080 - posted in Tissue and Cell Culture: I am trying to collect cells HT1080 (fibrosarcoma) from 24-well plate, but they are very stubborn, I washed first with PBS, and then tried to take them together with 200ul of PBS by scraping them with tip and pipetting up and down, but many cells satyed in wells. Do you know any method for taking them? The purpose is to collect them do lysis and Western Blot. Thank you!!!