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Adenosine Receptor P1 Receptor

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Adenosine Receptor P1 receptor Adenosine receptors (ARs) comprise a group of G protein-coupled receptors (GPCR) which mediate the physiological actions of adenosine. To date, four AR subtypes have been cloned and identified in different tissues. These receptors have distinct localization, signal transduction pathways and different means of regulation upon exposure to agonists. A key property of some of Adenosine receptors is their ability to serve as sensors of cellular oxidative stress, which is transmitted by transcription factors, such as NF-κB, to regulate the expression of ARs. The importance of Adenosine receptors in the regulation of normal and pathological processes such as sleep, the development of cancers and in protection against hearing loss will be examined. www.MedChemExpress.com 1 Adenosine Receptor Inhibitors, Agonists, Antagonists, Activators & Modulators (Rac)-Mirabegron D5 5'-N-Ethylcarboxamidoadenosine ((Rac)-YM178 D5) Cat. No.: HY-14773S (NECA) Cat. No.: HY-103173 (Rac)-Mirabegron D5 ((Rac)-YM178 D5) is a 5'-N-Ethylcarboxamidoadenosine (NECA) is a deuterium labeled (Rac)-Mirabegron. nonselective adenosine receptor agonist. (Rac)-Mirabegron is the racemate of Mirabegron. Mirabegron is a selective β3-adrenoceptor agonist. Purity: >98% Purity: 99.86% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 5 mg, 10 mg 8-Cyclopentyl-1,3-dimethylxanthine A2A receptor antagonist 1 Cat. No.: HY-W011955 (CPI-444 analog) Cat. No.: HY-102024 8-Cyclopentyl-1,3-dimethylxanthine (Compound 2a) A2A receptor antagonist 1 (CPI-444 analog) is an is a selective adenosine A1 receptor antagonist antagonist of both adenosine A2A receptor and with Kis of 10.9 nM and 1440 nM for A1 receptor A1 receptor with Ki values of 4 and 264 nM, and A2 receptor, respectively. respectively.</br>. Purity: >98% Purity: 99.81% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg A2AR-agonist-1 A2B receptor antagonist 1 Cat. No.: HY-18776 Cat. No.: HY-U00321 A2AR-agonist-1 is a potent A2AR and ENT1 agonist A2B receptor antagonist 1 is a potent A2B with Ki of 4.39 and 3.47 for A2AR and ENT1. IC50 adenosine receptor antagonist extracted from value: 4.39 and 3.47 (Ki) Target: A2AR and ENT1 patent WO 2009157938 A1 EXAMPLE 9B. A2AR-agonist-1 is a novel dual-action compound, targeting the Adenosine A2A Receptor and Adenosine Transporter for Neuroprotection. Purity: 99.96% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 1 mg, 5 mg AB-MECA AB928 Cat. No.: HY-19365 Cat. No.: HY-129393 AB-MECA is a high affinity A3 adenosine receptor AB928 is an orally bioavailable, selective dual agonist, has high affinity for recombinant A1 and adenosine receptor (A2aR/A2bR) antagonist. AB928 A3 receptors. relieves adenosine-mediated immune suppression. AB928 has immunomodulatory and antitumor activities. Purity: 99.10% Purity: 99.30% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 10 mM × 1 mL, 1 mg, 5 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Acefylline Adenosine 5'-monophosphate monohydrate (Theophyllineacetic acid; Theophylline-7-acetic acid) Cat. No.: HY-B1505 (5'-AMP monohydrate) Cat. No.: HY-A0181A Acefylline (Theophyllineacetic acid), a xanthine Adenosine 5'-monophosphate monohydrate is an derivative, is an adenosine receptor antagonist. adenosine A1 receptor agonist. Adenosine Acefylline is a peptidylarginine deiminase (PAD) 5'-monophosphate monohydrate has significant activator. Acefylline is also a bronchodilator, antiviral activity against HSV-1 and HSV-2. which inhibits rat lung cAMP phosphodiesterase isoenzymes. Purity: 99.89% Purity: 99.07% Clinical Data: Launched Clinical Data: Phase 4 Size: 10 mM × 1 mL, 100 mg Size: 10 mM × 1 mL, 500 mg, 1 g 2 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Adenosine A1 receptor activator T62 Adenosine amine congener Cat. No.: HY-106199 (ADAC) Cat. No.: HY-128064 Adenosine A1 receptor activator T62 is an Adenosine amine congener (ADAC) is a selective A1 allosteric enhancer of adenosine A1 receptor. adenosine receptor agonist, can ameliorate noise- Adenosine A1 receptor activator T62 produces and Cisplatin-induced cochlear injury. Adenosine antinociception in animal models of acute pain and amine congener also has neuroprotective effects. also reduces hypersensitivity in models of inflammatory and nerve-injury pain. Purity: ≥98.0% Purity: 99.23% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg Size: 10 mM × 1 mL, 5 mg Adenosine antagonist-1 Adenosine-2'-monophosphate Cat. No.: HY-100274 (2'-AMP; Adenosine 2'-phosphate; AMP 2'-phosphate) Cat. No.: HY-124151 Adenosine antagonist-1 is an adenosine A3 receptor Adenosine-2'-monophosphate (2'-AMP) is converted (AA3R) antagonist. by extracellular 2’,3'-CAMP. Adenosine-2'-monophosphate is further metabolized to extracellular adenosine (a mechanism called the extracellular 2’,3’-cAMP-adenosine pathway). Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg Aminophylline APNEA Cat. No.: HY-B0140 (N6-[2-(4-Aminophenyl)ethyl]adenosine) Cat. No.: HY-18687 Aminophylline is a competitive and non-selective APNEA (N6-[2-(4-Aminophenyl)ethyl]adenosine) is a phosphodiesterase (PDE) inhibitor. Aminophylline potent, non-selective A3 adenosine receptor is a competitive adenosine receptor antagonist. agonist. Aminophylline has apulmonary vasodilator action as well as a bronchodilator action and has the potential for asthma research. Purity: 99.91% Purity: 95.01% Clinical Data: Launched Clinical Data: Phase 4 Size: 10 mM × 1 mL, 100 mg, 500 mg Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg AZD4635 BAY 60-6583 (HTL1071) Cat. No.: HY-101980 Cat. No.: HY-103171 AZD4635 (HTL1071) is a potent, selective and BAY 60-6583 is a potent and high-affinity agonist orally active adenosine A2A receptor (A2AR) of adenosine A2B receptor (EC50 = 3 nM) antagonist. AZD4635 binds to human A2AR with a over A1, A2A, and A3 receptors. BAY 60-6583 binds Ki of 1.7 nM and shows >30-fold selectivity to mouse, rabbit, and dog A2BAR with Ki values of over other adenosine receptors. 750 nM, 340 nM and 330 nM, respectively. Purity: 99.68% Purity: 99.58% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg BAY-545 Capadenoson Cat. No.: HY-111767 (BAY 68-4986) Cat. No.: HY-14917 BAY-545 is a potent and selective A2B adenosine Capadenoson is a selective agonist of adenosine-A1 receptor antagonist, with an IC50 of 59 nM. receptor. Purity: 97.06% Purity: 99.28% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg www.MedChemExpress.com 3 CGS 15943 CGS 21680 Cat. No.: HY-100678 Cat. No.: HY-13201 CGS 15943 is an orally bioavailable non-xanthine CGS 21680 is a selective adenosine A2A receptor Adenosine Receptor antagonist. Its Ki for human agonist, with a Ki of 27 nM. A1, A2A, A2B, and A3 Adenosine Receptors are 3.5, 4.2, 16, and 50 nM in transfected CHO cells, respectively. Purity: 99.63% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 1 mg Size: 1 mg, 5 mg CGS 21680 Hydrochloride Cirazoline hydrochloride Cat. No.: HY-13201A (LD 3098 hydrochloride) Cat. No.: HY-101300 CGS 21680 Hydrochloride is a selective adenosine Cirazoline hydrochloride (LD 3098 hydrochloride) A2A receptor agonist with a Ki of 27 nM. is a potent competitive full α1A-adrenergic receptor (α1A-AR) agonist (Ki=120 nM) and only a partial agonist at α1B-AR (Ki= 960 nM) and α1D-AR (Ki=660 nM). Purity: 99.70% Purity: ≥98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 5 mg, 10 mg, 50 mg CPI-444 Derenofylline (V81444; ciforadenant) Cat. No.: HY-101978 (SLV 320) Cat. No.: HY-14858 CPI-444 (V81444) is a potent, orally active and Derenofylline (SLV 320) is a potent, selective and selective adenosine A2A receptor (A2AR) orally active adenosine A1 receptor antagonist, antagonist, which induces antitumor responses. with Ki values of 1 nM, 200 nM and 398 nM for human A1, A3 and A2A receptors respectively. Purity: 99.94% Purity: 98.26% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg Diphylline Doxofylline (Diprophylline) Cat. No.: HY-B0128 Cat. No.: HY-B0004 Diphylline (Diprophylline) is a potent A1/A2 Doxofylline is an antagonist of adenosine A1 adenosine receptor antagonist and cyclic receptor which also inhibits phosphodiesterase IV. nucleotide phosphodiesterase inhibitor. Diphylline, a xanthine derivative, is a bronchodilator and vasodilator drug and has the potential for chronic bronchitis and emphysema. Purity: 99.07% Purity: 99.32% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 100 mg, 500 mg Size: 10 mM × 1 mL, 100 mg DPCPX FSCPX (PD 116948) Cat. No.: HY-100937 Cat. No.: HY-116042 DPCPX (PD 116948), a xanthine derivative, is a FSCPX is a potent and selective irreversible highly potent and selective Adenosine A1 receptor antagonist of A1 adenosine receptor (A1AR), 3 antagonist, with a Ki of 0.46 nM in H-CHA with low nanomolar potency for binding to the binding to A1 receptors in rat whole brain A1AR.
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    MedDocs Publishers ISSN: 2638-1370 Annals of Clinical Nutrition Open Access | Mini Review Study of Adulterants and Diluents in Some Seized Captagon-Type Stimulants Ali Zaid A Alshehri1,2*; Mohammed saeed Al Qahtani1,3; Mohammed Aedh Al Qahtani1,4; Abdulhadi M Faeq1,5; Jawad Aljohani1,6; Ammar AL-Farga7 1Department of Medical Laboratory Technology, College of Applied Medical Sciences, University of Jeddah, Saudi Arabia 2Poison Control and Medical Forensic Chemistry Center, Ministry of Health, Riyadh, Saudi Arabia 3Khammis Mushayte Maternity & Children Hospital, Ministry of Health, Saudi Arabia 4Ahad Rufidah General, Hospital, Aseer, Ministry of Health, Saudi Arabia 5Comprehensive Specialized Clinics of Security Forces in Jeddah, Ministry of Interior, Saudi Arabia 6Compliance Department, Yanbu Health Sector, Ministry of Health, Saudi Arabia 7Department of Biochemistry, Faculty of Science, University of Jeddah, Saudi Arabia *Corresponding Author(s): Ali Zaid A Alshehri Department of Medical Laboratory Technology, College of Applied Medical Sciences, University of Jeddah, Saudi Arabia Email: [email protected] Received: Apr 27, 2020 Accepted: Jun 05, 2020 Published Online: Jun 10, 2020 Journal: Annals of Clinical Nutrition Publisher: MedDocs Publishers LLC Online edition: http://meddocsonline.org/ Copyright: © Alshehri AZA (2020). This Article is distributed under the terms of Creative Commons Attribution 4.0 International License Introduction ATS are synthetic compounds belonging to the class of stimu- and heroin users combined [3,4]. Fenethylline, 7-(2-amethyl lants that excite the Central Nervous System (CNS) to produce phenyl-amino ethyl)-theophylline, is a theophylline derivative of adrenaline-like effects such as amphetamine, methamphet- amphetamine. It is a psychoactive drug which is similar to am- amine, fenethylline, methylphenidate and dextroamphetamine phetamine in many ways [5].
  • Pharmacy and Poisons (Third and Fourth Schedule Amendment) Order 2017

    Pharmacy and Poisons (Third and Fourth Schedule Amendment) Order 2017

    Q UO N T FA R U T A F E BERMUDA PHARMACY AND POISONS (THIRD AND FOURTH SCHEDULE AMENDMENT) ORDER 2017 BR 111 / 2017 The Minister responsible for health, in exercise of the power conferred by section 48A(1) of the Pharmacy and Poisons Act 1979, makes the following Order: Citation 1 This Order may be cited as the Pharmacy and Poisons (Third and Fourth Schedule Amendment) Order 2017. Repeals and replaces the Third and Fourth Schedule of the Pharmacy and Poisons Act 1979 2 The Third and Fourth Schedules to the Pharmacy and Poisons Act 1979 are repealed and replaced with— “THIRD SCHEDULE (Sections 25(6); 27(1))) DRUGS OBTAINABLE ONLY ON PRESCRIPTION EXCEPT WHERE SPECIFIED IN THE FOURTH SCHEDULE (PART I AND PART II) Note: The following annotations used in this Schedule have the following meanings: md (maximum dose) i.e. the maximum quantity of the substance contained in the amount of a medicinal product which is recommended to be taken or administered at any one time. 1 PHARMACY AND POISONS (THIRD AND FOURTH SCHEDULE AMENDMENT) ORDER 2017 mdd (maximum daily dose) i.e. the maximum quantity of the substance that is contained in the amount of a medicinal product which is recommended to be taken or administered in any period of 24 hours. mg milligram ms (maximum strength) i.e. either or, if so specified, both of the following: (a) the maximum quantity of the substance by weight or volume that is contained in the dosage unit of a medicinal product; or (b) the maximum percentage of the substance contained in a medicinal product calculated in terms of w/w, w/v, v/w, or v/v, as appropriate.