메뉴 건너뛰기




Volumn 331, Issue 1, 2009, Pages 96-103

APD791, 3-methoxy-N-(3-(1-methyl-1H-pyrazol-5-yl)-4-(2-morpholinoethoxy) phenyl)benzamide, a novel 5-hydroxytryptamine 2A receptor antagonist: Pharmacological profile, pharmacokinetics, platelet activity and vascular biology

Author keywords

[No Author keywords available]

Indexed keywords

3 METHOXY N [3 [1 METHYL 1H PYRAZOL 5 YL] 4 (2 MORPHOLINOETHOXY)PHENYL]BENZAMIDE; APD 791; DRUG METABOLITE; G PROTEIN COUPLED RECEPTOR; INOSITOL PHOSPHATE; SEROTONIN 2A ANTAGONIST; SEROTONIN 2A RECEPTOR; SEROTONIN 2B RECEPTOR; SEROTONIN 2C RECEPTOR; UNCLASSIFIED DRUG;

EID: 70349338807     PISSN: 00223565     EISSN: 15210103     Source Type: Journal    
DOI: 10.1124/jpet.109.153189     Document Type: Article
Times cited : (21)

References (27)
  • 2
    • 0022578083 scopus 로고
    • Serotonin as a mediator of cyclic flow variations in stenosed canine coronary arteries
    • Ashton JH, Benedict CR, Fitzgerald C, Raheja S, Taylor A, Campbell WB, Buja LM, and Willerson JT (1986) Serotonin as a mediator of cyclic flow variations in stenosed canine coronary arteries. Circulation 73:572-578. (Pubitemid 16133036)
    • (1986) Circulation , vol.73 , Issue.3 , pp. 572-578
    • Ashton, J.H.1    Benedict, C.R.2    Fitzgerald, C.3
  • 3
    • 0015861774 scopus 로고
    • Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction
    • Cheng Y and Prusoff WH (1973) Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction. Biochem Pharmacol 22:3099-3108.
    • (1973) Biochem Pharmacol , vol.22 , pp. 3099-3108
    • Cheng, Y.1    Prusoff, W.H.2
  • 4
    • 33750555770 scopus 로고    scopus 로고
    • The safety and efficacy of aspirin and clopidogrel as a combination treatment in patients with coronary heart disease
    • DOI 10.1517/14740338.5.6.815
    • Cooke GE and Goldschmidt-Clermont PJ (2006) The safety and efficacy of aspirin and clopidogrel as a combination treatment in patients with coronary heart disease. Expert Opin Drug Saf 5:815-826. (Pubitemid 44669496)
    • (2006) Expert Opinion on Drug Safety , vol.5 , Issue.6 , pp. 815-826
    • Coole, G.E.1    Goldschmidt-Clermont, P.J.2
  • 5
    • 0020565085 scopus 로고
    • 5-Hydroxytryptamine and platelet aggregation
    • De Clerck FF and Herman AG (1983) 5-Hydroxytryptamine and platelet aggregation. Fed Proc 42:228-232.
    • (1983) Fed Proc , vol.42 , pp. 228-232
    • De Clerck, F.F.1    Herman, A.G.2
  • 6
    • 0025687562 scopus 로고
    • Amplification mechanisms in platelet activation and arterial thrombosis
    • De Clerck FF and Janssen PA (1990) Amplification mechanisms in platelet activation and arterial thrombosis. J Hypertens Suppl 8:S87-S93.
    • (1990) J Hypertens Suppl , vol.8
    • De Clerck, F.F.1    Janssen, P.A.2
  • 7
    • 0016154281 scopus 로고
    • Proceedings: Platelet release reaction induced by 5-hydroxytryptamine
    • Drummond AH and Gordon JL (1974) Proceedings: platelet release reaction induced by 5-hydroxytryptamine. J Physiol 240:39P-40P.
    • (1974) J Physiol , vol.240
    • Drummond, A.H.1    Gordon, J.L.2
  • 8
    • 0034100396 scopus 로고    scopus 로고
    • Serotonin and the heart
    • Frishman WH and Grewall P (2000) Serotonin and the heart. Ann Med 32:195-209.
    • (2000) Ann Med , vol.32 , pp. 195-209
    • Frishman, W.H.1    Grewall, P.2
  • 10
    • 0033039831 scopus 로고    scopus 로고
    • Differences in agonist-independent activity of 5-Ht2A and 5-HT2c receptors revealed by heterologous expression
    • Grotewiel MS and Sanders-Bush E (1999) Differences in agonist-independent activity of 5-Ht2A and 5-HT2c receptors revealed by heterologous expression. Naunyn Schmiedebergs Arch Pharmacol 359:21-27.
    • (1999) Naunyn Schmiedebergs Arch Pharmacol , vol.359 , pp. 21-27
    • Grotewiel, M.S.1    Sanders-Bush, E.2
  • 12
    • 0003633755 scopus 로고    scopus 로고
    • Institute of Laboratory Animal Resources Institute of Laboratory Animal Resources, Commission on Life Sciences, National Research Council, Washington, DC
    • Institute of Laboratory Animal Resources (1996) Guide for the Care and Use of Laboratory Animals, 7th ed. Institute of Laboratory Animal Resources, Commission on Life Sciences, National Research Council, Washington, DC.
    • (1996) Guide for the Care and Use of Laboratory Animals, 7th Ed.
  • 13
    • 0036216159 scopus 로고    scopus 로고
    • Binding and functional affinity of sarpogrelate, its metabolite M-1 and ketanserin for human recombinant alpha-1-adrenoceptor subtypes
    • DOI 10.1159/000056189
    • Israilova M, Suzuki F, Tanaka T, Nagatomo T, Taniguchi T, and Muramatsu I (2002) Binding and functional affinity of sarpogrelate, its metabolite m-1 and ketanserin for human recombinant alpha-1-adrenoceptor subtypes. Pharmacology 65:69-73. (Pubitemid 34298008)
    • (2002) Pharmacology , vol.65 , Issue.2 , pp. 69-73
    • Israilova, M.1    Suzuki, F.2    Tanaka, T.3    Nagatomo, T.4    Taniguchi, T.5    Muramatsu, I.6
  • 14
    • 33746335649 scopus 로고    scopus 로고
    • 5-Hydroxytryptamine receptors in the human cardiovascular system
    • DOI 10.1016/j.pharmthera.2005.12.004, PII S016372580500286X
    • Kaumann AJ and Levy FO (2006) 5-Hydroxytryptamine receptors in the human cardiovascular system. Pharmacol Ther 111:674-706. (Pubitemid 44118434)
    • (2006) Pharmacology and Therapeutics , vol.111 , Issue.3 , pp. 674-706
    • Kaumann, A.J.1    Levy, F.O.2
  • 15
    • 0035930832 scopus 로고    scopus 로고
    • 2A receptor antagonist, in rat arterial thrombosis model and its effect on bleeding time
    • DOI 10.1016/S0014-2999(01)01432-7, PII S0014299901014327
    • Kihara H, Koganei H, Hirose K, Yamamoto H, and Yoshimoto R (2001) Antithrombotic activity of AT-1015, a potent 5-HT(2A) receptor antagonist, in rat arterial thrombosis model and its effect on bleeding time. Eur J Pharmacol 433:157-162. (Pubitemid 34045174)
    • (2001) European Journal of Pharmacology , vol.433 , Issue.2-3 , pp. 157-162
    • Kihara, H.1    Koganei, H.2    Hirose, K.3    Yamamoto, H.4    Yoshimoto, R.5
  • 16
    • 0036599358 scopus 로고    scopus 로고
    • Molecular biology of serotonin receptors structure and function at the molecular level
    • Kroeze WK, Kristiansen K, and Roth BL (2002) Molecular biology of serotonin receptors structure and function at the molecular level. Curr Top Med Chem 2:507-528.
    • (2002) Curr Top Med Chem , vol.2 , pp. 507-528
    • Kroeze, W.K.1    Kristiansen, K.2    Roth, B.L.3
  • 17
    • 33644872570 scopus 로고    scopus 로고
    • Inhibition of 5-hydroxytryptamine receptor prevents occlusive thrombus formation on neointima of the rabbit femoral artery
    • Nishihira K, Yamashita A, Tanaka N, Kawamoto R, Imamura T, Yamamoto R, Eto T, and Asada Y (2006) Inhibition of 5-hydroxytryptamine receptor prevents occlusive thrombus formation on neointima of the rabbit femoral artery. J Thromb Haemost 4:247-255.
    • (2006) J Thromb Haemost , vol.4 , pp. 247-255
    • Nishihira, K.1    Yamashita, A.2    Tanaka, N.3    Kawamoto, R.4    Imamura, T.5    Yamamoto, R.6    Eto, T.7    Asada, Y.8
  • 18
    • 0037146931 scopus 로고    scopus 로고
    • 2A receptor antagonist R-102444
    • DOI 10.1016/S0014-2999(02)02654-7, PII S0014299902026547
    • Ogawa T, Sugidachi A, Tanaka N, Fujimoto K, and Asai F (2002) Pharmacological profiles of R-96544, the active form of a novel 5-HT2A receptor antagonist R-102444. Eur J Pharmacol 457:107-114. (Pubitemid 35447652)
    • (2002) European Journal of Pharmacology , vol.457 , Issue.2-3 , pp. 107-114
    • Ogawa, T.1    Sugidachi, A.2    Tanaka, N.3    Fujimoto, K.4    Asai, F.5
  • 21
    • 69249236278 scopus 로고    scopus 로고
    • Abstract 1034: Targeted inhibition of the serotonin 5-HT2A receptor improves coronary patency in an in vivo model of recurrent thrombosis
    • Przyklenk K, Linden MD, Frelinger AL III, Teegarden B, Adams J, and Michelson AD (2007) Abstract 1034: Targeted inhibition of the serotonin 5-HT2A receptor improves coronary patency in an in vivo model of recurrent thrombosis. Circulation 116:II-206.
    • (2007) Circulation , vol.116
    • Przyklenk, K.1    Linden, M.D.2    Frelinger III, A.L.3    Teegarden, B.4    Adams, J.5    Michelson, A.D.6
  • 22
    • 0038401338 scopus 로고    scopus 로고
    • Identification of the binding sites and selectivity of sarpogrelate, a novel 5-HT2 antagonist, to human 5-HT2A, 5-HT2B and 5-HT2C receptor subtypes by molecular modeling
    • Rashid M, Manivet P, Nishio H, Pratuangdejkul J, Rajab M, Ishiguro M, Launay JM, and Nagatomo T (2003) Identification of the binding sites and selectivity of sarpogrelate, a novel 5-HT2 antagonist, to human 5-HT2A, 5-HT2B and 5-HT2C receptor subtypes by molecular modeling. Life Sci 73:193-207.
    • (2003) Life Sci , vol.73 , pp. 193-207
    • Rashid, M.1    Manivet, P.2    Nishio, H.3    Pratuangdejkul, J.4    Rajab, M.5    Ishiguro, M.6    Launay, J.M.7    Nagatomo, T.8
  • 23
    • 0141523216 scopus 로고    scopus 로고
    • 2A receptor as missing link?
    • DOI 10.1097/01.PSY.0000088596.42029.10
    • Schins A, Honig A, Crijns H, Baur L, and Hamulyák K (2003) Increased coronary events in depressed cardiovascular patients: 5-HT2A receptor as missing link?. Psychosom Med 65:729-737. (Pubitemid 37163376)
    • (2003) Psychosomatic Medicine , vol.65 , Issue.5 , pp. 729-737
    • Schins, A.1    Honig, A.2    Crijns, H.3    Baur, L.4    Hamulyak, K.5
  • 26
    • 0033520025 scopus 로고    scopus 로고
    • Serotonin is associated with coronary artery disease and cardiac events
    • Vikenes K, Farstad M, and Nordrehaug JE (1999) Serotonin is associated with coronary artery disease and cardiac events. Circulation 100:483-489. (Pubitemid 29360156)
    • (1999) Circulation , vol.100 , Issue.5 , pp. 483-489
    • Vikenes, K.1    Farstad, M.2    Nordrehaug, J.E.3
  • 27
    • 0029880769 scopus 로고    scopus 로고
    • 2 antagonist (SR46349)
    • DOI 10.1016/0049-3848(96)00030-8
    • Yang LH, Callas D, Herbert JM, and Fareed J (1996) Modulation of platelet function and vascular smooth muscle contractile actions by a novel, selective, highly potent 5-HT2 antagonist (SR46349). Thromb Res 81:555-567. (Pubitemid 26101335)
    • (1996) Thrombosis Research , vol.81 , Issue.5 , pp. 555-567
    • Yang, L.H.1    Callas, D.2    Herbert, J.M.3    Fareed, J.4


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.