| 词条 | Mazapertine |
| 释义 |
| ImageFile = Mazapertine.svg | ImageSize = 200px | IUPACName = Piperidin-1-yl[3-({4-[2-(propan-2-yloxy)phenyl]piperazin-1-yl}methyl)phenyl]methanone | OtherNames = RWJ-37796 |Section1={{Chembox Identifiers | CASNo = 134208-17-6 | CASNo_Ref = {{cascite|correct|}} | UNII = N0X1XW704P | PubChem = 60820 | ChemSpiderID = 54808 | ChEMBL = 10085 | SMILES = O=C(N1CCCCC1)c2cc(ccc2)CN4CCN(c3ccccc3OC(C)C)CC4 | InChI = 1/C26H35N3O2/c1-21(2)31-25-12-5-4-11-24(25)28-17-15-27(16-18-28)20-22-9-8-10-23(19-22)26(30)29-13-6-3-7-14-29/h4-5,8-12,19,21H,3,6-7,13-18,20H2,1-2H3 | InChIKey = ZKZFPRUSWCYSGT-UHFFFAOYAF | StdInChI = 1S/C26H35N3O2/c1-21(2)31-25-12-5-4-11-24(25)28-17-15-27(16-18-28)20-22-9-8-10-23(19-22)26(30)29-13-6-3-7-14-29/h4-5,8-12,19,21H,3,6-7,13-18,20H2,1-2H3 | StdInChIKey = ZKZFPRUSWCYSGT-UHFFFAOYSA-N |Section2={{Chembox Properties | C=26 | H=35 | N=3 | O=2 | Appearance = | Density = | MeltingPt = | BoilingPt = | Solubility = |Section3={{Chembox Hazards | MainHazards = | FlashPt = | AutoignitionPt = }}Mazapertine (RWJ-37796) is an antipsychotic agent that was developed by Johnson & Johnson but never marketed. It exerts its pharmacological effect through affinity for dopamine D2, serotonin 5-HT1A, and α1-adrenergic receptors.[1] Mazapertine is safe and well tolerated when administered orally.[2] Analogs of mazapertine with conformational restriction have been prepared and have greater affinity for the 5-HT1A receptor.[3]References1. ^{{Cite journal | last1 = Reitz | first1 = A. B. | last2 = Baxter | first2 = E. W. | last3 = Codd | first3 = E. E. | last4 = Davis | first4 = C. B. | last5 = Jordan | first5 = A. D. | last6 = Maryanoff | first6 = B. E. | last7 = Maryanoff | first7 = C. A. | last8 = McDonnell | first8 = M. E. | last9 = Powell | first9 = E. T. | last10 = Renzi | doi = 10.1021/jm970164z | first10 = M. J. | last11 = Schott | first11 = M. R. | last12 = Scott | first12 = M. K. | last13 = Shank | first13 = R. P. | last14 = Vaught | first14 = J. L. | title = Orally Active Benzamide Antipsychotic Agents with Affinity for Dopamine D2, Serotonin 5-HT1A, and Adrenergic α1Receptors | journal = Journal of Medicinal Chemistry | volume = 41 | issue = 12 | pages = 1997–2009 | year = 1998 | pmid = 9622541 | pmc = }} {{Antipsychotics}}{{Nervous-system-drug-stub}}2. ^{{Cite journal | last1 = Kleinbloesem | first1 = C. H. | last2 = Jaquet-Müller | first2 = F. O. | last3 = Al-Hamdan | first3 = Y. | last4 = Baldauf | first4 = C. | last5 = Gisclon | first5 = L. | last6 = Wesnes | first6 = K. | last7 = Curtin | first7 = C. R. | last8 = John Stubbs | first8 = R. | last9 = Walker | first9 = S. A. | doi = 10.1016/S0009-9236(96)90008-9 | last10 = Brunner-Ferber | first10 = F. O. | title = Incremental dosage of the new antipsychotic mazapertine induces tolerance to cardiovascular and cognitive effects in healthy men* | journal = Clinical Pharmacology & Therapeutics | volume = 59 | issue = 6 | pages = 675–685 | year = 1996 | pmid = 8681493 | pmc = }} 3. ^{{cite journal | doi = 10.1016/S0960-894X(97)00074-7 | title = Hindered rotation congeners of mazapertine: High affinity ligands for the 5-HT1A receptor | year = 1997 | last1 = Baxter | first1 = Ellen W. | last2 = Reitz | first2 = Allen B. | journal = Bioorganic & Medicinal Chemistry Letters | volume = 7 | issue = 7 | pages = 763}} 6 : Antipsychotics|Piperidines|Piperazines|Phenol ethers|Isopropyl compounds|Carboxamides |
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