메뉴 건너뛰기




Volumn 35, Issue 2, 2000, Pages 144-150

Agonist high and low affinity state ratios predict drug intrinsic activity and a revised ternary complex mechanism at serotonin 5-HT(2A) and 5- HT(2C) receptors

Author keywords

5 HT(2A) receptors; 5 HT(2C) receptors; Intrinsic activity; K(L) K(H) ratio; Revised ternary complex; Serotonin; Ternary complex

Indexed keywords

(3 CHLOROPHENYL)PIPERAZINE; 1 (3 TRIFLUOROMETHYLPHENYL)PIPERAZINE; 2,5 DIMETHOXY 4 METHYLAMPHETAMINE; 4 IODO 2,5 DIMETHOXYAMPHETAMINE; 5 METHOXY N,N DIMETHYLTRYPTAMINE; 5 METHOXYTRYPTAMINE; BUFOTENINE; GUANINE NUCLEOTIDE BINDING PROTEIN; LISURIDE; LYSERGIDE; PHOSPHATIDYLINOSITOL; QUIPAZINE; RADIOLIGAND; SEROTONIN; SEROTONIN 2A RECEPTOR; SEROTONIN 2C RECEPTOR;

EID: 0033987382     PISSN: 08874476     EISSN: None     Source Type: Journal    
DOI: 10.1002/(SICI)1098-2396(200002)35:2<144::AID-SYN7>3.0.CO;2-K     Document Type: Article
Times cited : (69)

References (11)
  • 1
    • 0019137579 scopus 로고
    • A ternary complex model explains the agonist-specific binding properties of the adenylate cyclase-coupled beta-adrenergic receptor
    • De Lean A, Stadel JM, Lefkowitz RJ. 1980. A ternary complex model explains the agonist-specific binding properties of the adenylate cyclase-coupled beta-adrenergic receptor. J Biol Chem 255:7108-7117.
    • (1980) J Biol Chem , vol.255 , pp. 7108-7117
    • De Lean, A.1    Stadel, J.M.2    Lefkowitz, R.J.3
  • 2
    • 0031846352 scopus 로고    scopus 로고
    • Creation of a constitutively activated state of the 5-hydroxytryptamine2A receptor by site-directed mutagenesis: Inverse agonist activity of antipsychotic drugs
    • Egan CT, Herrick-Davis K, Teitler M. 1998. Creation of a constitutively activated state of the 5-hydroxytryptamine2A receptor by site-directed mutagenesis: inverse agonist activity of antipsychotic drugs. J Pharmacol Exp Ther 286:85-90.
    • (1998) J Pharmacol Exp Ther , vol.286 , pp. 85-90
    • Egan, C.T.1    Herrick-Davis, K.2    Teitler, M.3
  • 3
    • 0030757387 scopus 로고    scopus 로고
    • Activating mutations of the serotonin 5-HT2C receptor
    • Herrick-Davis K, Egan C, Teitler M. 1997. Activating mutations of the serotonin 5-HT2C receptor. J Neurochem 69:1138-1144.
    • (1997) J Neurochem , vol.69 , pp. 1138-1144
    • Herrick-Davis, K.1    Egan, C.2    Teitler, M.3
  • 4
    • 0018862848 scopus 로고
    • A quantitative analysis of beta-adrenergic receptor interactions: Resolution of high and low affinity states of the receptor by computer modeling of ligand binding data
    • Kent RS, De Lean A, Lefkowitz RJ. 1980. A quantitative analysis of beta-adrenergic receptor interactions: resolution of high and low affinity states of the receptor by computer modeling of ligand binding data. Mol Pharmacol 17:14-23.
    • (1980) Mol Pharmacol , vol.17 , pp. 14-23
    • Kent, R.S.1    De Lean, A.2    Lefkowitz, R.J.3
  • 5
    • 0027297275 scopus 로고
    • Constitutive activity of receptors coupled to guanine nucleotide regulatory proteins
    • Lefkowitz RJ, Cotecchia S, Samama P, Costa T. 1993. Constitutive activity of receptors coupled to guanine nucleotide regulatory proteins. Trends Pharmacol Sci 14:303-307.
    • (1993) Trends Pharmacol Sci , vol.14 , pp. 303-307
    • Lefkowitz, R.J.1    Cotecchia, S.2    Samama, P.3    Costa, T.4
  • 6
    • 0027065043 scopus 로고
    • Molecular pharmacological differences in the interaction of serotonin with 5-hydroxytryptamine1C and 5-hydroxytryptamine2 receptors
    • Leonhardt S, Gorospe E, Hoffman BJ, Teitler M. 1992. Molecular pharmacological differences in the interaction of serotonin with 5-hydroxytryptamine1C and 5-hydroxytryptamine2 receptors. Mol Pharmacol 42:328-335.
    • (1992) Mol Pharmacol , vol.42 , pp. 328-335
    • Leonhardt, S.1    Gorospe, E.2    Hoffman, B.J.3    Teitler, M.4
  • 7
    • 0023165026 scopus 로고
    • 3H-DOB (4-bromo-2,5-dimethoxy-phenylisopropylamine) labels a guanyl nucleotide-sensitive state of cortical 5-HT2 receptors
    • 3H-DOB (4-bromo-2,5-dimethoxy-phenylisopropylamine) labels a guanyl nucleotide-sensitive state of cortical 5-HT2 receptors. Mol Pharmacol 31:194-199.
    • (1987) Mol Pharmacol , vol.31 , pp. 194-199
    • Lyon, R.A.1    Davis, K.H.2    Titeler, M.3
  • 8
    • 0030899598 scopus 로고    scopus 로고
    • High-affinity agonist binding is not sufficient for agonist intrinsic activity at 5-hydroxytryptamine2A receptors: Evidence in favor of a modified ternary complex model
    • Roth BL, Choudary MS, Khan N, Uluer AZ. 1997. High-affinity agonist binding is not sufficient for agonist intrinsic activity at 5-hydroxytryptamine2A receptors: evidence in favor of a modified ternary complex model. J Pharmacol Exp Ther 280:576-583.
    • (1997) J Pharmacol Exp Ther , vol.280 , pp. 576-583
    • Roth, B.L.1    Choudary, M.S.2    Khan, N.3    Uluer, A.Z.4
  • 9
    • 0027513982 scopus 로고
    • A mutation-induced activated state of the beta 2-adrenergic receptor. Extending the ternary complex model
    • Samama P, Cotecchia S, Costa T, Lefkowitz RJ. 1993. A mutation-induced activated state of the beta 2-adrenergic receptor. Extending the ternary complex model. J Biol Chem 268:4625-4636.
    • (1993) J Biol Chem , vol.268 , pp. 4625-4636
    • Samama, P.1    Cotecchia, S.2    Costa, T.3    Lefkowitz, R.J.4
  • 10
    • 0025194760 scopus 로고
    • 4-[125I]iodo-(2,5-dimethoxy)phenylisopropylamine and [3H]ketanserin labeling of 5-hydroxytryptamine2 (5HT2) receptors in mammalian cells transfected with a rat 5HT2 cDNA: Evidence for multiple states and not multiple 5HT2 receptor subtypes
    • Teitler M, Leonhardt S, Weisberg EL, Hoffman BJ. 1990. 4-[125I]iodo-(2,5-dimethoxy)phenylisopropylamine and [3H]ketanserin labeling of 5-hydroxytryptamine2 (5HT2) receptors in mammalian cells transfected with a rat 5HT2 cDNA: evidence for multiple states and not multiple 5HT2 receptor subtypes. Mol Pharmacol 38:594-598.
    • (1990) Mol Pharmacol , vol.38 , pp. 594-598
    • Teitler, M.1    Leonhardt, S.2    Weisberg, E.L.3    Hoffman, B.J.4
  • 11
    • 0023199529 scopus 로고
    • Selectivity of serotonergic drugs for multiple brain serotonin receptors. Role of [3H]-4-bromo-2,5-dimethoxyphenylisopropylamine ([3H]DOB), a 5-HT2 agonist radioligand
    • Teitler M, Lyon RA, Davis KH, Glennon RA. 1987. Selectivity of serotonergic drugs for multiple brain serotonin receptors. Role of [3H]-4-bromo-2,5-dimethoxyphenylisopropylamine ([3H]DOB), a 5-HT2 agonist radioligand. Biochem Pharmacol 36:3265-3271.
    • (1987) Biochem Pharmacol , vol.36 , pp. 3265-3271
    • Teitler, M.1    Lyon, R.A.2    Davis, K.H.3    Glennon, R.A.4


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.