디클로펜신

Diclofensine
디클로펜신
Diclofensine.svg
임상자료
ATC 코드
  • 없음
법적현황
법적현황
  • 일반적으로: 합법적
식별자
  • 4-(3,4-lorophenyl)-7-methoxy-2-methyl-1,2,3,4-methydhydroisoquinolin)
CAS 번호
펍켐 CID
켐스파이더
유니
켐벨
화학 및 물리적 데이터
공식C17H17CL2NO
어금질량322.23 g·properties−1
3D 모델(JSmol)
  • CN1CC(C2=C(C1)C=C(C=C2)OC)C3=CC(=C(C=C3)Cl)Cl
  • InChi=1S/C17H17Cl2NO/c1-20-9-12-7-13(21-2)4-5-14(112)15(120)11-3-6-16(18)17(19)8-11-8/h3-8,15H,9-10H2,1-2H3-2H3 ☒N
  • 키:ZJDCGVDEEHWEIG-UHFFFAOYSA-N ☒N
☒NcheckY (이게 뭐야?) (iii)

디클로펜신(Ro 8-4650)은 1970년대[1] 호프만-라 로슈가 새로운 항우울제를 찾아 개발했다.활동에는 (S)등분체가 책임이 있는 것으로 나타났다.[2]3중[5] 모노아민 재흡수 억제제 역할을 [3][4]하는 각성제로 도파민과 노르에피네프린 재흡수를 주로 억제하며 DAT, NET, SERT(도파민, 노르에피네프린, 세로토닌 전달체)의 친화력(Ki)이 각각 16.8nM, 15.7nM, 51nM이다.[6][7]상대적으로 부작용이 적은 [8][9][10]인체 실험에서 효과적인 항우울제인 것으로 밝혀졌지만,[11] 결국 남용 가능성에 대한 우려 때문인지 임상 개발에서 떨어졌다.[12][13]

디클로펜신은 화학적으로 테트라하이드로이소퀴놀린(THIQ) 파생상품으로, 노미펜신(as nomifensine)과 같다.

참고 항목

참조

  1. ^ 미국 특허 3947456 A, Alfred Rheiner, "대체된 4-페닐 이소퀴놀린"은 1976-03-30으로 호프만-라 로슈 주식회사에 배당되었다.
  2. ^ Crossley, Roger (1995). Chirality and the Biological Activity of Drugs. 2000 Corporate Blvd., N.W., Boca Raton, Florida 33431: CRC Press, Inc. p. 138. ISBN 978-0-8493-9140-8.{{cite book}}: CS1 maint : 위치(링크)
  3. ^ Keller HH, Schaffner R, Carruba MO, Burkard WP, Pieri M, Bonetti EP, et al. (1982). "Diclofensine (Ro 8-4650)--a potent inhibitor of monoamine uptake: biochemical and behavioural effects in comparison with nomifensine". Advances in Biochemical Psychopharmacology. 31: 249–63. PMID 6979165.
  4. ^ Omer LM (July 1982). "Pilot trials with diclofensine, a new psychoactive drug in depressed patients". International Journal of Clinical Pharmacology, Therapy, and Toxicology. 20 (7): 320–6. PMID 7107085.
  5. ^ Di Renzo G, Amoroso S, Taglialatela M, Canzoniero LM, Maida P, Lombardi G, Annunziato L (1988). "Pure uptake blockers of dopamine can reduce prolactin secretion: studies with diclofensine". Life Sciences. 42 (21): 2161–9. doi:10.1016/0024-3205(88)90131-2. PMID 2968488.
  6. ^ Gasić S, Korn A, Eichler HG (May 1986). "Effect of diclofensine, a novel antidepressant, on peripheral adrenergic function". Clinical Pharmacology and Therapeutics. 39 (5): 582–5. doi:10.1038/clpt.1986.100. PMID 3698467. S2CID 34977195.
  7. ^ Andersen PH (August 1989). "The dopamine inhibitor GBR 12909: selectivity and molecular mechanism of action". European Journal of Pharmacology. 166 (3): 493–504. doi:10.1016/0014-2999(89)90363-4. PMID 2530094.
  8. ^ Cherpillod C, Omer LM (1981). "A controlled trial with diclofensine, a new psychoactive drug, in the treatment of depression". The Journal of International Medical Research. 9 (5): 324–9. doi:10.1177/030006058100900505. PMID 7028532. S2CID 41618656.
  9. ^ Omer OL, Díaz-Olivera M, Ismail S (March 1984). "Therapeutic efficacy and tolerance of diclofensine in psychoreactive depression--a double-blind comparison with placebo". Methods and Findings in Experimental and Clinical Pharmacology. 6 (3): 147–51. PMID 6379345.
  10. ^ Funke HJ, Holtmann W, Ismail S, Jansen W, Leonhardt KF, Muth H, et al. (May 1986). "Double-blind comparison of diclofensine with nomifensine in outpatients with dysphoric mood". Pharmacopsychiatry. 19 (3): 120–3. doi:10.1055/s-2007-1017168. PMID 3725890.
  11. ^ Culig J, Ehsanullah RS, Hallett C, Iliopoulou A, Matheson I, Turner P (May 1983). "A clinical pharmacological comparison of diclofensine (Ro 8-4650) with nomifensine and amitriptyline in normal human volunteers". British Journal of Clinical Pharmacology. 15 (5): 537–43. doi:10.1111/j.1365-2125.1983.tb02087.x. PMC 1427714. PMID 6860528.
  12. ^ Lamb RJ, Griffiths RR (1990). "Self-administration in baboons and the discriminative stimulus effects in rats of bupropion, nomifensine, diclofensine and imipramine". Psychopharmacology. 102 (2): 183–90. doi:10.1007/bf02245920. PMID 2125734. S2CID 25043692.
  13. ^ Nakachi N, Kiuchi Y, Inagaki M, Inazu M, Yamazaki Y, Oguchi K (August 1995). "Effects of various dopamine uptake inhibitors on striatal extracellular dopamine levels and behaviours in rats". European Journal of Pharmacology. 281 (2): 195–203. doi:10.1016/0014-2999(95)00246-h. PMID 7589207.