ADX-47273

ADX-47273
ADX-47273
ADX-47273.svg
식별자
  • (S)-(4-fluorophenyl)-(3-[3-(4-fluoro-페닐)-[1,2,4]-옥사디아졸-5-yl]피페리딘-1-yl)메타논
CAS 번호
  • 851881-60-2 checkY
    851881-59-9(R 이소머),
    837413-22-6 (동료)
펍켐 CID
IUPHAR/BPS
켐스파이더
유니
켐벨
CompTox 대시보드 (EPA)
화학 및 물리적 데이터
공식C20H17F2N3O2
어금질량369.372 g·190−1
3D 모델(JSmol)
  • FC1=CC=C(C(N2CCC[C@@H](C2)C3=NC(C4=CC=C(F)=C4)=O)C=C1
  • InChI=1S/C20H17F2N3O2/c21-16-7-3-13(4-8-16)18-23-19(27-24-18)15-2-1-11-25(12-15)20(26)14-5-9-17(22)10-6-14/h3-10,15H,1-2,11-12H2/t15-/m0/s1 checkY
  • 키:VXQCCZHCFBHTTD-HNNXBMFYSA-N
(iii)

ADX-47273아덱스 테라피틱스가 개발한 연구용 의약품으로, 메타보틱스 글루타민산 수용체 서브타입 mGluR5 선택적으로 양성 알로스테릭 변조기(PAM) 역할을 한다.[1][2]동물학에서 비등방성항정신병 효과가 있으며,[3] 개선된 파생상품을 개발하기 위해 납 화합물로 사용되어 왔다.[4]

참고 항목

참조

  1. ^ de Paulis T, Hemstapat K, Chen Y, Zhang Y, Saleh S, Alagille D, Baldwin RM, Tamagnan GD, Conn PJ (June 2006). "Substituent effects of N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides on positive allosteric modulation of the metabotropic glutamate-5 receptor in rat cortical astrocytes". Journal of Medicinal Chemistry. 49 (11): 3332–44. doi:10.1021/jm051252j. PMID 16722652.
  2. ^ Stauffer, Shaun R. (17 August 2011). "Progress toward Positive Allosteric Modulators of the Metabotropic Glutamate Receptor Subtype 5 (mGlu5)". ACS Chemical Neuroscience. 2 (8): 450–470. doi:10.1021/cn2000519. PMC 3369763. PMID 22860171.
  3. ^ Liu F, Grauer S, Kelley C, Navarra R, Graf R, Zhang G, Atkinson PJ, Popiolek M, Wantuch C, Khawaja X, Smith D, Olsen M, Kouranova E, Lai M, Pruthi F, Pulicicchio C, Day M, Gilbert A, Pausch MH, Brandon NJ, Beyer CE, Comery TA, Logue S, Rosenzweig-Lipson S, Marquis KL (December 2008). "ADX47273 [S-(4-fluoro-phenyl)-{3-[3-(4-fluoro-phenyl)-[1,2,4]-oxadiazol-5-yl]-piperidin-1-yl}-methanone]: a novel metabotropic glutamate receptor 5-selective positive allosteric modulator with preclinical antipsychotic-like and procognitive activities". The Journal of Pharmacology and Experimental Therapeutics. 327 (3): 827–39. doi:10.1124/jpet.108.136580. PMID 18753411.
  4. ^ Engers DW, Rodriguez AL, Williams R, Hammond AS, Venable D, Oluwatola O, Sulikowski GA, Conn PJ, Lindsley CW (April 2009). "Synthesis, SAR and unanticipated pharmacological profiles of analogues of the mGluR5 ago-potentiator ADX-47273". ChemMedChem. 4 (4): 505–11. doi:10.1002/cmdc.200800357. PMC 2865690. PMID 19197923.