0-Adrenergic structure-activity

Risperidone (11) was also included among a a 1-adrenergic receptor antagonists to study a quantitative structure-activity relationship (99BMC2437). A pharmacophore model for atypical antipsychotics, including 11, was established (00MI41). An increased plasma level of 11 and 9-hydroxyrisperidone (12) was observed in combination with paroxetine (01 MI 13). The effect of vanlafaxine on the pharmacokinetics of 11 was reported (99MI13). 

Rastelli, G., Fanelli, F., Menziani, M.C., Cocchi, M. and De Benedetti, P.G. (1991) Conformational analysis, molecular modeling and quantitative structure-activity relationships studies of 2,4-diamino-6,7-dimethoxy-2-substituted quinazoline al-adrenergic antagonists. Journal of Molecular Structure (Theochem), 251, 307—318. 

Menziani, M.C., Montorsi, M., De Benedetti, P.G. and Karelson, M. (1999) Relevance of theoretical molecular descriptors in quantitative structure-activity relationship analysis of alphal-adrenergic receptor antagonists. Bioorganic el Medicinal Chemistry, 7, 2437-2451. 

Quantitative structure-activity relationships of alphal adrenergic antagonists. Journal of Molecular Modelling, 10, 139-150. 

Lopez-Rodriguez, M.L., Morcillo, M.J., Fernandez, E., Porras, E., Orensanz, L., Beneytez, M.E., Manzanares, J. and Fuentes, J.A. (2001) Synthesis and structure-activity relationships of a new model of arylpiperazines. 5. Study of the physicochemical influence of the pharmacophore on 5-HT]A/ai-adrenergic receptor affinity. Synthesis of a new selective derivative with mixed 5-HT1A/D2 antagonist properties. Journal of Medicinal Chemistry, 44, 186-197. 

STRUCTURE-ACTIVITY RELATIONSHIPS FOR ADRENERGIC NEURONE BLOCKADE 139... 

Hansch, C. and Lien, E. J. (1968) An analysis of the structure-activity relationship in the adrenergic blocking activity of the P-haloalkylamines. Biochem. Pharmacol. 17, 709-720. 

Unger, S. H. and Hansch, C. (1973) On model building in structure-activity relationships. A reexamination of adrenergic blocking activity of p-halo-p-arylakylamines. J. Med. Chem. 16, 745-749. 

Adrenergic drugs may also exert postsynaptic effects. There is a considerable body of classical structure-activity correlation studies in the adrenergic field for these effects. It may be summarized as follows ... 

The Eg parameter was first introduced by Hansch and Lien into biological structure-activity studies 24). They showed that the adrenergic blocking activity of p-haloalkyl-... 

Structure and activity at adrenergic receptors of catecholamines and related compounds, 2, 127 Structure-activity relationships and mechanism of action of antibacterial sulphanilamides and... 

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