Schönenberger, Helmut and Petter, A. and Zwez, W. (1972) Mechanism of action of local anesthetics. 6. Binding of local anesthetics to complementary membrane structures. Pharmazie 27 (12), pp. 760-767.
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The function of various mol. groups in anesthetic agents such as N-(N-dimethylalanyl)-2,6-dimethylaniline (I) [19216-39-8], N-(N-dimethylphenylalanyl)-2,6-dimethylaniline [19216-40-1], and N-(N-dimethylphenylalanyl)ephedrine (II) [10385-91-8] and their interaction with structural proteins of innervated membrane (frog heart) was given. Under various pH conditions (6.2-8.3), the anesthetics were more active as the free base than as the acidic form. A comparison of the 50% inhibitory dose (LD50) of the acidic and basic forms of II isomers indicated that isomers having a D configuration in the amino acid portion of the mol. were more active than those with an L configuration; the basic II isomers were more active anesthetics than the acidic isomers; and the basic enantiomeric isomers differed in their order of decreasing activity from that of the acidic enantiomeric isomers.
|Additional information (public):||CAN 78:79558 1-3 Pharmacodynamics 2480-20-8; 2673-32-7; 5042-94-4; 7232-10-2; 7232-11-3; 7232-12-4; 7275-84-5; 7278-68-4; 19216-71-8; 19216-72-9; 19216-73-0; 19237-86-6 Role: PROC (Process) (membrane binding of, anesthetic activity in relation to)|
|Institutions:||Chemistry and Pharmacy > Institute of Pharmacy > Retired Professors > Prof. Schönenberger|
|Keywords:||Molecular structure-biological activity relationship (anesthetic, of aminoacryldimethylaniline derivs.) Anesthetics (membrane binding of, aminoacryldimethylaniline derivs. in relation to) Membranes (protein, aminoacryldimethylaniline derivs. binding to) Isomerism and Isomers (stereo-, of dimethylphenylalanylephedrine, membrane binding in relation to) anesthetic interaction membrane protein ephedrine isomer anesthesia membrane|
|Subjects:||500 Science > 540 Chemistry & allied sciences|
|Refereed:||Yes, this version has been refereed|
|Created at the University of Regensburg:||Unknown|
|Deposited On:||19 Nov 2010 09:54|
|Last Modified:||19 Nov 2010 09:54|
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