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Pazinaclone

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The first-pass metabolism of ( S )- and ( R )-pazinaclone on oral administration of the racemate was enantioselective, with respective bioavailabilities of 1.7 and 0.8% in rats, 10.4 and 1.9% in dogs, and 0 and 11.4% in monkeys. Therefore, the enantioselectivity was more pronounced after oral dosing. Citing Literature Issue Download PDF.

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good yields and diastereomeric excesses. This methodology was applied to the asymmetric synthesis of a new pazinaclone ana-logue which is of interest in the field of benzodiazepine-receptor agonists. Introduction Isoindolinones I (Figure€1), e.g., 2,3-dihydro-1H-isoindol-1-ones, also called phthalimidines are bicyclic lactams whose mo-.
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Define pazinaclone. Pazinaclone as a noun means A sedative and anxiolytic cyclopyrrolone drug.
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1 . Serum and urine concentrations of enantiomers of pazinaclone (DN-2327) and an active metabolite M II, were measured after single and twice daily oral doses of 4 and 8 mg racemic drug to healthy subjects.. 2 . The kinetics of rac-pazinaclone and rac-M II were dose-independent and no unchanged drug was recovered in urine.. 3 . The terminal elimination half-lives of the drug.
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Corvalol (Корвалол, Corvalolum, Korvalol) is a tranquilizer based on the herb valerian (Valeriana officinalis) root, as well peppermint oil Mentha piperita and hop extract Humulus lupulus and the barbiturate phenobarbital, popular in Eastern Europe and the former Soviet Union as a heart medication. It is available as a transparent liquid with a characteristic strong aroma, and as white.
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Analogs of Pazinaclone, (S)-PD172938 and Related Biologically Relevant Isoindolinones Antonia Di Mola 1, *, Giorgia Nicastro 1 , Lorenzo Serusi 1 , Rosanna Filosa 2 , Mario Waser 3.
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Pazinaclone (DN-2327) is a sedative and anxiolytic drug in the cyclopyrrolone family of drugs. Some other cyclopyrrolone drugs include zopiclone and eszopiclone.. Pazinaclone has a very.
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دکس‌مدتومیدین، با نام تجاری Dexdomitor (توسط اوریون کورپوریشن )، در اتحادیه اروپا برای استفاده در گربه‌ها و سگ‌ها در سال ۲۰۰۲ برای اثرات آرام بخشی و القای بیهوشی عمومی تأیید شد. [۱] سازمان غذا و.
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A practical one-pot isoindolinone synthesis enabled by RhIII catalysis was developed. The advantage of this protocol is that it does not require pre-preparation of amide substrates, because RhIII participates in two reactions independently. This mild, operationally multicomponent process transforms a wide variety of commercially available aldehydes into. KEGG Orthology (KO) [BR:hsa00001] 09130 Environmental Information Processing 09133 Signaling molecules and interaction 04080 Neuroactive ligand-receptor interaction. The psychomotor, memory, subjective, and reinforcing effects of DN-2327 (DN), a novel partial agonist at benzodiazepine receptors, were compared with those of alprazolam (AL) in 14 men with histories of sedative drug abuse. Placebo, DN (8, 16, and 32 mg), and AL (0.5, 1.0, and 2.0 mg) were administered orally in a randomized, double-blind, cross-over design. DN and AL.

This methodology was applied to the asymmetric synthesis of a new pazinaclone analogue which is of interest in the field of benzodiazepine-receptor agonists. Keywords:Aza-Michael reaction, phase-transfer catalyst, asymmetric organocatalysis, 3- substituted isoindolinones Introduction.

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The absorption of pazinaclone was more extensive when the drug was given to fed animals as suspension. Thus, the toxicity studies were performed using form I of pazinaclone with a particle size of about 20 microns primarily in rats, mice, and dogs. PMID: 8876929 [Indexed for MEDLINE] Publication Types: Comparative Study; MeSH terms. Animals. Dichloralphenazone is a 1:2 mixture of antipyrine with chloral hydrate.In combination with paracetamol and isometheptene, it is the active ingredient of medications for migraine and tension headaches, including Epidrin and Midrin.Performance impairments are common with this drug and caution is advised, for example when driving motor vehicles. This file is licensed under the Creative Commons Attribution-Share Alike 4.0 International license.: You are free: to share – to copy, distribute and transmit the work; to remix – to adapt the work; Under the following conditions: attribution – You must give appropriate credit, provide a link to the license, and indicate if changes were made. You may do so in any reasonable manner, but. In rats, mice, hamsters, and guinea pigs given a 5 mg/kg oral dose of pazinaclone (CAS 103255-66-9), unchanged drug concentration in plasma was highest in mice (AUC; 90 ng.h/ml), followed in decreasing order by guinea pigs (AUC; 41 ng.h/ml), hamsters (AUC; 18 ng.h/ml),. S-pazinaclone was 33-fold greater than that after oral dosing of the R-enantiomer at 4 mg/kg. The toxic activity is thus likely to reside predominantly in the R-enantiomers of pazinaclone and M-II. The exposure of the R-enantiomers in humans, after administration of the anticipated clinical dose of the racemic.

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Further, at any one of the centres of load let PL represent the magnitude and direction of the gross load, and Pa, Pb the two resistances by which the piece to which that load is applied is supported; then wifl those three lines be respectively the diagonal and sides of a parallelogram; or, what is the same thing, they will be equal to the three sides of a triangleS and they must be in the.

  • پریمیدون. پریمیدون ( آیوپاک آدی: 5-Ethyl-5-phenyl-1,3-diazinane-4,6-dione, اینگیلیسجه: Primidone, روسجا: Примидон) بیر شیمیایی بیلشیک دواء. بۇ دواءنین مول جرمیسی مول/قرم ۲۱۸٫۲۵۲ دیر. متابولیسمی قاراجییرده باش وئریر. The absorption of pazinaclone in dogs was improved by decreasing its particle size: AUCs of pazinaclone after dosing of the drug having particle size of 5.5, 20.8, and 79.3 microns were 1361, 822, and 297 ng.h/ml, respectively. Since large-scale preparation of bulk pazinaclone with a particle size of 5 microns or smaller was not feasible, the. S-pazinaclone was 33-fold greater than that after oral dosing of the R-enantiomer at 4 mg/kg. The toxic activity is thus likely to reside predominantly in the R-enantiomers of pazinaclone and M-II. The exposure of the R-enantiomers in humans, after administration of the anticipated clinical dose of the racemic. Pazinaclone. A 77000, DN 2327 MeSH terms Animals Anti-Anxiety Agents / pharmacology* Anti-Anxiety Agents / therapeutic use Clinical Trials as Topic Drugs, Investigational / pharmacology* Drugs, Investigational / therapeutic use Humans Isoindoles Naphthyridines / pharmacology* Naphthyridines / therapeutic use Spiro Compounds / pharmacology*.

  • Further, at any one of the centres of load let PL represent the magnitude and direction of the gross load, and Pa, Pb the two resistances by which the piece to which that load is applied is supported; then wifl those three lines be respectively the diagonal and sides of a parallelogram; or, what is the same thing, they will be equal to the three sides of a triangleS and they must be in the. pazinaclone Molecular Formula CHClNO Average mass 478.927 Da Monoisotopic mass 478.140778 Da ChemSpider ID 53893 More details: Names Properties Searches Spectra Vendors Articles More Names and Synonyms Database ID (s) Validated by Experts, Validated by Users, Non-Validated, Removed by Users. Oct 01, 1993 · Abstract 1. Serum and urine concentrations of enantiomers of pazinaclone (DN-2327) and an active metabolite MII, were measured after single and twice daily oral doses of 4 and 8 mg racemic drug to healthy subjects. 2. The kinetics of rac-pazinaclone and rac-MII were dose-independent and no unchanged drug was recovered in urine. 3..

Properties: LD50 orally in mice: 5513 mg/kg (Yamamoto). Toxicity data: LD50 orally in mice: 5513 mg/kg (Yamamoto) Derivative Type: N4-Acetylsulfamethoxazole. CAS Registry Number: 21312-10-7. Properties: Crystals from alcohol, mp 209-210°. Melting point: mp 209-210°. Therap-Cat: Antibacterial; antipneumocystic.

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Nov 14, 2020 · isoindolin-1-one is a common moiety present in many natural products like nuevamine, 1 magallanesine, 2 staurosporine etc. 3 more specifically, 3-substituted isoindolin-1-ones are found in pharmacologically important synthetic drugs such as pazinaclone, 4 renin inhibitors, 5 antiarrhythmic agents, 6 and hiv reverse transcriptase inhibitor 7 (fig..

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  • 1. Serum and urine concentrations of enantiomers of pazinaclone (DN-2327) and an active metabolite MII, were measured after single and twice daily oral doses of 4 and 8 mg racemic.

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La zopiclone est un hypnotique de la famille chimique des cyclopyrrolones, apparenté aux benzodiazépines 2. Elle est commercialisée notamment sous le nom d' Imovane. La zopiclone possède des propriétés hypnotiques, sédatives, anxiolytiques, myorelaxantes et amnésiantes. Elle fait partie des hypnotiques les plus couramment utilisés.

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Herein we report the first racemic and asymmetric synthesis of novel 3-methylated analogs of valuable biologically active isoindolinones, bearing a tetrasubstituted stereocenter. In.

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Pregnanolone, also known as 3α,5β-tetrahydroprogesterone (3α,5β-THP) or as 5β-pregnan-3α-ol-20-one, is a naturally occurring pregnane steroid and a derivative of progesterone. Related compounds include allopregnanolone (3α,5α-THP; brexanolone), epipregnanolone (3β,5β-THP), hydroxydione, isopregnanolone (3β,5α-THP), and renanolone . History [ edit]. Properties: LD50 orally in mice: 5513 mg/kg (Yamamoto). Toxicity data: LD50 orally in mice: 5513 mg/kg (Yamamoto) Derivative Type: N4-Acetylsulfamethoxazole. CAS Registry Number: 21312-10-7. Properties: Crystals from alcohol, mp 209-210°. Melting point: mp 209-210°. Therap-Cat: Antibacterial; antipneumocystic. Search results for Pazinaclone at Glentham Life Sciences. Find catalogue prices, chemical data, technical specifications and MSDS documents. Pazinaclone (DN-2327) is a sedative and anxiolytic drug in the cyclopyrrolone family of drugs. Some other cyclopyrrolone drugs include zopiclone and eszopiclone.. Pazinaclone ( 9.1.36) (DN-2327) is an investigational sedative and anxiolytic drug, a nonbenzodiazepine compound that has a high affinity for benzodiazepine receptors. It acts as a partial agonist at γ-aminobutyric acid (GABA) benzodiazepine receptors..

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Molecular Formula: C25H23ClN4O4. Molecular Weight: 478.93. Percent Composition: C 62.70%, H 4.84%, Cl 7.40%, N 11.70%, O 13.36%. Literature References: Non-benzodiazepine exhibiting mixed agonist/antagonist effects with benzodiazepine receptors; activity resides primarily in the (S)-enantiomer.. Pazinaclone (DN-2327) is a sedative and anxiolytic drug in the cyclopyrrolone family of drugs. Some other cyclopyrrolone drugs include zopiclone and eszopiclone.. Pazinaclone has a very similar pharmacological profile to the benzodiazepines including sedative and anxiolytic properties, but with less amnestic effects, and at low doses it is a relatively selective anxiolytic, with sedative.

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  • PAZINACLONE, (R)- 2RL7K6WX26 Other Structure General Names 4: Identifiers 3: Related Substances 1: PAZINACLONE, (R)- 2RL7K6WX26 Other Details Stereochemistry: ABSOLUTE.

  • Derivatives. The derivatives of thioxanthene used clinically as antipsychotics include: Chlorprothixene (Cloxan, Taractan, Truxal); Clopenthixol (Sordinol); Flupenthixol (Depixol, Fluanxol); Thiothixene (Navane); Zuclopenthixol (Cisordinol, Clopixol, Acuphase); The therapeutic efficacy of these drugs is related to their ability to antagonize the D 2 receptors in the brain,.

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  • Jun 07, 2006 · Alprazolam is a benzodiazepine derivative that is currently used in the treatment of generalized anxiety, panic attacks with or without agoraphobia, and depression. Alprazolam has a fast onset of symptom relief (within the first week); it is unlikely to produce dependency or abuse. No tolerance to its therapeutic effect has been reported..

  • Chemistry. gamma-Butyrolactone is a lactone. It is hydrolyzed under basic conditions, for example in a sodium hydroxide solution into sodium gamma-hydroxybutyrate, the sodium salt of gamma-hydroxybutyric acid. Under acidic conditions it forms an equilibrium mixture of both compounds. gamma-Butyrolactone can be synthesized from gamma-hydroxybutyric acid by removal of water or by distillation.

RESEARCH & DEVELOPMENT Pazinaclone: clinically effective anxiolytic pazinaclone* [DN-2327), a benzodiazepine receptor agonist, produced significant improvements in several. Prof. for Organic Stereochemistry(Head of the Institute) TN Tower and Somnium - 3rd Floor - T 309. +43 732 2468 5411. +43 732 2468 5402. mario.waser@jku.at. ResearcherID ( F-5521-2010) ORCID ( 0000-0002-8421-8642) ScopusID ( 8518457600) EurJOC Author Profile.

Pazinaklon je organsko jedinjenje, koje sadrži 25 atoma ugljenika i ima molekulsku masu od 478,928 Da.. Osobine.

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This file is licensed under the Creative Commons Attribution-Share Alike 4.0 International license.: You are free: to share - to copy, distribute and transmit the work; to remix - to adapt the work; Under the following conditions: attribution - You must give appropriate credit, provide a link to the license, and indicate if changes were made. You may do so in any reasonable manner, but. Indeed, pazinaclone produces its sedative and anxiolytic effects by acting as a partial agonist at GABA A (γ-aminobutyric acid type A) benzodiazepine receptors . In order to circumvent any hydrolysis of the ketal group during the preparation of the starting benzamide (see Supporting Information File 1 ), the synthesis of intermediate 24 was. Prozac 및 Sarafem 상표명으로 판매되는 플루옥세틴 은 선택적 세로토닌 재흡수 억제제 ( [2] SSRI) 클래스의 항우울제 이다. 그것 은 주요 우울증, 강박장애, 폭식증, 공황장애, [2] 월경전 발작장애 의 치료 에 사용된다. 또한 8세 [6] 이상 청소년과 아동의 주요 우울증.

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Indeed, pazinaclone produces its sedative and anxiolytic effects by acting as a partial agonist at GABA A (γ-aminobutyric acid type A) benzodiazepine receptors . In order to circumvent any hydrolysis of the ketal group during the preparation of the starting benzamide (see Supporting Information File 1 ), the synthesis of intermediate 24 was. In rats, mice, hamsters, and guinea pigs given a 5 mg/kg oral dose of pazinaclone (CAS 103255-66-9), unchanged drug concentration in plasma was highest in mice (AUC; 90 ng.h/ml), followed in decreasing order by guinea pigs (AUC; 41 ng.h/ml), hamsters (AUC; 18 ng.h/ml),. สารานุกรมเภสัชกรรม. ฟลูนิแทรซิแพม (Flunitrazepam) หรือชื่อทางการค้าว่า โรฮิปนอล (Rohypnol) เป็น ยานอนหลับ มีฤทธิ์ทำให้นอนหลับและสูญเสีย.

Infobox references. Bromisoval (INN), commonly known as bromovalerylurea, is a hypnotic and sedative of the bromoureide group discovered by Knoll in 1907 and patented in 1909. [1] It is marketed over the counter in Asia under various trade names (such as Brovarin [2] ), usually in combination with nonsteroidal anti-inflammatory drugs.

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Glutethimide is a CYP2D6 enzyme inducer. When taken with codeine, it enables the body to convert higher amounts of the codeine (higher than the average 5 - 10%) in to morphine. The street name for a combination of Doriden and Codeine #4 is a "load" or "doors and fours" or "Pancakes" in Pancakes and Syrup (Glutethimide and codeine based cough. Differences in the stereoselective pharmacokinetics of pazinaclone (DN-2327), a new anxiolytic, and its active metabolite after intravenous and oral single doses to dogs. Hussein Z, Mulford DJ, Bopp BA, Granneman GR. Drug Metab Dispos, 21(5):805-810, 01 Sep 1993 Cited by: 2 articles | PMID: 7902240. Pazopanib is a cancer medicine that is used to treat patients with kidney cancer (advanced renal cell carcinoma). It is also used to treat advanced soft tissue sarcoma (STS) in patients who have received other cancer treatments. Pazopanib interferes with the growth of cancer cells, which are eventually destroyed by the body.. Define pazinaclone. Pazinaclone as a noun means A sedative and anxiolytic cyclopyrrolone drug ... Key:HUNXMJYCHXQEGX-UHFFFAOYSA-N Y. (verify) زالپلون که با نام تجاری سوناتا مشهور است، یک داروی آرامبخش - خواب‌آور است که برای درمان بی‌خوابی استفاده می‌شود. زالپلون یک خواب‌آور غیر بنزودیازپینی از گروه. Pazinaclone (DN-2327) is a sedative and anxiolytic drug in the cyclopyrrolone family of drugs. Some other cyclopyrrolone drugs include zopiclone and eszopiclone.. Contents. Synthesis; See also; References; Pazinaclone has a very similar pharmacological profile to the benzodiazepines including sedative and anxiolytic properties, but with less amnestic effects, [1] and at low.

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课题组合影. 朱钢国博士,教授,省“万人计划”科技创新领军人才,Tel:0579-82282640;E-mail: [email protected],主要经历如下:. 1996年9月-2000年7月:浙江师范大学化学系,理学学士。. 2000年9月-2005年7月:中科院上海有机化学研究所,理学博士,导师张兆国教授.

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Below is a list of pazinaclone words - that is, words related to pazinaclone. The top 4 are: sedative, anxiolytic, cyclopyrrolone and zopiclone.You can get the definition(s) of a word in the. Inn - Free download as PDF File (.pdf), Text File (.txt) or read online for free. WHO inn list. صوديوم ثيوپنتال Sodium thiopental ، ويشتهر باسم پنتوثال الصوديوم وهو علامة تجارية لمعامل آبوت. ثيوبنتال، ثيوبنتون أو ترابانال ,هو من مجموعة الباربيتيورات قصيرة الأجل سريعة الثأثير، ويعطى في الاستجوابا. Sommaire du brevet 2628178. Énoncé de désistement de responsabilité concernant l'information provenant de tiers. Disponibilité de l'Abrégé et des Revendications. (12) Demande de brevet : (11) CA 2628178. (54) Titre français : PROCEDE DE LYOPHILISATION ET PRODUITS OBTENUS SELON LEDIT PROCEDE. (54) Titre anglais : LYOPHILIZATION PROCESS.

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Jun 07, 2006 · Alprazolam and DN‐2327 (Pazinaclone) in humans: Psychomotor, memory, subjective, and reinforcing effects. Exp Clin Psychopharmacol 1995; 3 :39–48. [ Google Scholar ]. Pazinaclone ( DN-2327) is a sedative and anxiolytic drug in the cyclopyrrolone family of drugs. Some other cyclopyrrolone drugs include zopiclone and eszopiclone .. Flubrotizolam. Flubrotizolam ( 2-bromo-4- (2-fluorophenyl)-9-methyl-6H-thieno [3,2-f] [1,2,4]triazolo [4,3-a] [1,4]diazepine) is a thienotriazolodiazepine derivative with potent sedative and anxiolytic effects, which has been sold as a designer drug. [1] [2] [3]. Pagoclone is an anxiolytic agent from the cyclopyrrolone family, related to better-known drugs such as the sleeping medication zopiclone.It was synthesized by a French team working for Rhone-Poulenc & Rorer S.A. Pagoclone belongs to the class of nonbenzodiazepines, which have similar effects to the older benzodiazepine group, but with quite different chemical structures. pazinaclone. Molecular Formula C 25 H 23 ClN 4 O 4; Average mass 478.927 Da; Monoisotopic mass 478.140778 Da; ChemSpider ID 53893; More details: Systematic name.. As a general overview, some examples of the possible benefits of drug combinations include: (1) Enhanced euphoria, e.g. see speedball which is massively euphoric but also very dangerous, (2) reduced psychological discomfort (e.g. anxiolytics with psychedelics), (3) uniquely interesting effects, e.g. LSD + MDMA (see below), and (4) reduced.

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Molecular Formula: C25H23ClN4O4. Molecular Weight: 478.93. Percent Composition: C 62.70%, H 4.84%, Cl 7.40%, N 11.70%, O 13.36%. Literature References: Non-benzodiazepine exhibiting mixed agonist/antagonist effects with benzodiazepine receptors; activity resides primarily in the (S)-enantiomer.. The effects of single oral doses of DN-2327 (DN, 2 mg or 3 mg), a newly developed partial benzodiazepine receptor agonist, and alprazolam (APZ, 0.8 mg), a full receptor agonist, on psychomotor function and short-term memory were assessed using three psychometric tests: letter cancellation, visual vigilance and Sternberg's memory scanning task.. Pazinaclone, also known as A-77000; DN-2327, is a sedative and anxiolytic drug in the cyclopyrrolone family of drugs. Some other cyclopyrrolone drugs include zopiclone and eszopiclone. Pazinaclone has a very similar pharmacological profile to the benzodiazepines including sedative and anxiolytic properties, but with less amnestic effects, and at low doses it is a relatively selective.

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(R)-Pazinaclone: Description (R)-Pazinaclone belongs to the class of organic compounds known as beta amino acids and derivatives. These are amino acids having a (-NH2) group attached to the beta carbon atom. Based on a literature review very few articles have been published on (R)-Pazinaclone. Pazinaclone, Pazinaclone supplier, Pazinaclone distributor, CAS 103255-66-9, Pazinaclone manufacturer, Pazinaclone wholesale. Unités du SI et CNTP, sauf indication contraire. Les benzodiazépines Écouter ( BZD) sont une classe de composés organiques formés d'un cycle benzénique fusionné à un cycle diazépine. On classe aussi parmi les benzodiazépines les thiénodiazépines, qui à la différence d'avoir un cycle benzène possèdent un cycle thiophène. KEGG Orthology (KO) [BR:hsa00001] 09130 Environmental Information Processing 09133 Signaling molecules and interaction 04080 Neuroactive ligand-receptor interaction.

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103255-66-9 - DPGKFACWOCLTCA-UHFFFAOYSA-N - Pazinaclone [USAN:INN] - Similar structures search, synonyms, formulas, resource links, and other chemical information.