에타졸레이트

Etazolate
에타졸레이트
Etazolate.svg
임상자료
경로:
행정		구강
ATC 코드
  • 없는
법적현황
법적현황
  • 일반적으로: 통제되지 않음
식별자
  • 에틸 1-에틸-4-[2-(프로판-2-ylidene)히드라지닐]-1H-피라졸로[3,4-b]피리딘-5-카르복실산염
CAS 번호
펍켐 CID
IUPHAR/BPS
켐스파이더
유니
체비
켐벨
CompTox 대시보드 (EPA)
화학 및 물리적 데이터
공식C14H19N5O2
어금질량289.339 g·198−1
3D 모델(JSmol)
  • CCN1C2=NC=C(C(=C2C=N1)N=C(C)C(=O)OCC

에타졸레이트(SQ-20,009, EHT-0202)는 화라졸로피리딘 파생물질로 약리학적 특성이 독특한 항불안제다.[1][2][3] 바비투레이트 결합 사이트에서 GABAA 수용체의 양성 알로스테리액 변조기,[4][5][6][7] A와12 A 하위 유형의 아데노신 길항제,[8] 그리고 PDE4 이소폼에 선택되는 인산염 억제제 역할을 한다.[9][10][11] 현재 알츠하이머병 치료를 위한 임상시험 중이다.[12]

합성

카르타졸레이트 및 에타졸레이트 합성: E.R. SQUIBB & SONS, Inc., New York, N.Y., US. DE 2123318

참고 항목

참조

  1. ^ Hall, Judith A.; Morton, Ian (1999). Concise dictionary of pharmacological agents: properties and synonyms. Kluwer Academic. ISBN 0-7514-0499-3.
  2. ^ Williams M (May 1983). "Anxioselective anxiolytics". Journal of Medicinal Chemistry. 26 (5): 619–28. doi:10.1021/jm00359a001. PMID 6132997.
  3. ^ Williams M, Risley EA (February 1979). "Enhancement of the binding of 3H-diazepam to rat brain membranes in vitro by SQ 20009, A novel anxiolytic, gamma-aminobutyric acid (GABA) and muscimol". Life Sciences. 24 (9): 833–41. doi:10.1016/0024-3205(79)90367-9. PMID 449623.
  4. ^ Zezula J, Slany A, Sieghart W (April 1996). "Interaction of allosteric ligands with GABAA receptors containing one, two, or three different subunits". European Journal of Pharmacology. 301 (1–3): 207–14. doi:10.1016/0014-2999(96)00066-0. PMID 8773466.
  5. ^ Remington, Gary; Baskys, Andrius (1996). Brain mechanisms and psychotropic drugs. Boca Raton: CRC Press. ISBN 0-8493-8386-2.
  6. ^ M. Mishina; Kurachi, Yoshihisa (2000). Pharmacology of ionic channel function: activators and inhibitors. Berlin: Springer. ISBN 3-540-66127-1.
  7. ^ Progress in Drug Research / Volume 31 (Progress in Drug Research). Boston: Birkhauser. 1987. p. 526. ISBN 3-7643-1837-6.
  8. ^ Williams M, Jarvis MF (February 1988). "Adenosine antagonists as potential therapeutic agents". Pharmacology Biochemistry and Behavior. 29 (2): 433–41. doi:10.1016/0091-3057(88)90182-7. PMID 3283781. S2CID 35635747.
  9. ^ Chasin M, Harris DN, Phillips MB, Hess SM (September 1972). "1-Ethyl-4-(isopropylidenehydrazino)-1H-pyrazolo-(3,4-b)-pyridine-5-carboxylic acid, ethyl ester, hydrochloride (SQ 20009)--a potent new inhibitor of cyclic 3',5'-nucleotide phosphodiesterases". Biochemical Pharmacology. 21 (18): 2443–50. doi:10.1016/0006-2952(72)90414-5. PMID 4345859.
  10. ^ Wang P, Myers JG, Wu P, Cheewatrakoolpong B, Egan RW, Billah MM (May 1997). "Expression, purification, and characterization of human cAMP-specific phosphodiesterase (PDE4) subtypes A, B, C, and D". Biochemical and Biophysical Research Communications. 234 (2): 320–4. doi:10.1006/bbrc.1997.6636. PMID 9177268.
  11. ^ Gresele, Paolo; Gresele, P. (2002). Platelets in thrombotic and non-thrombotic disorders: pathophysiology, pharmacology and therapeutics. Cambridge, UK: Cambridge University Press. ISBN 0-521-80261-X.
  12. ^ "Pipeline ExonHit". Archived from the original on 2011-01-11. Retrieved August 2010. {{cite web}}: 날짜 값 확인: access-date= (도움말)