Conformational adaptability at GABA-sensitive inhibitory synapses

Steward, E. G.; Clarke, G. R.

doi:10.1016/0022-5193(75)90015-6

Cited by 11 publications

(3 citation statements)

References 25 publications

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“…1. It has been pointed out that the greater the proportion of molecules that exist in the ideal conformation, the stronger the binding (Steward and Clark, 1975). Shortened-chain analogues like taurine (12) as usual show decreased activity.…”

Section: Carboxyl Analoguesmentioning

confidence: 99%

“…On the other hand, the 4-sulphonic acid (5) in a boat conformation offers essentially the precise requirements for strong binding. It has been pointed out that the greater the proportion of molecules that exist in the ideal conformation, the stronger the binding (Steward and Clark, 1975). Thus piperidine-4-sulphonic acid can be considered to 'profit' from its ring structure which removes rotational degrees of freedom present in acyclic analogues (7,9).…”

Section: Carboxyl Analoguesmentioning

confidence: 99%

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Inhibition of [³H]GABA Binding to Postsynaptic Receptors in Human Cerebellar Synaptic Membranes by Carboxyl and Amino Derivatives of GABA

Breckenridge

Nicholson

Nicol

et al. 1981

Journal of Neurochemistry

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Fifty synthetic analogues of GABA were tested for their ability ot interact with GABA receptors, using [3H]GABA binding to human cerebellar membranes as an in vitro model. The most active compounds were found to be aliphatic and heterocyclic aminosulphonic acids. Compounds with highly substituted nitrogen atoms were only weakly active unless a long alkyl chain, which can interact with the postsynaptic membrane, was present. It was concluded that a pyramidal nitrogen atom is favoured fro binding of GABA analogues to human cerebellar membranes.

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Section: Carboxyl Analoguesmentioning

confidence: 99%

Section: Carboxyl Analoguesmentioning

confidence: 99%

Inhibition of [³H]GABA Binding to Postsynaptic Receptors in Human Cerebellar Synaptic Membranes by Carboxyl and Amino Derivatives of GABA

Breckenridge

Nicholson

Nicol

et al. 1981

Journal of Neurochemistry

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show abstract

“…Such knowledge should prove valuable in the design of potential pharmacologically active GABA-mimetic compounds and also in the study of the mechanism of action of the GABA receptor itself. STEWARD & CLARK, 1975; MATERIALS AND METHODS Studies of GABA-binding were performed using human cerebellar cortex as the source of the synaptic membrane prcparation. The assay was based upon the method of ENNA & SNYDER (1975).…”

mentioning

confidence: 99%

GABA analogues: conformational analysis of effects on [³H]GABA binding to postsynaptic receptors in human cerebellum

Nicholson

Suckling

Iversen

1979

Journal of Neurochemistry

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Magnesium and calcium cation–ligand interactions within the pseudopotential approach. II. Cation–GABA interactions

Leś

Blake

1981

Int J of Quantum Chemistry

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AbstractsWe performed ab initio pseudopotential and CNDO calculations on y-aminobutyric acid (GABA) and its Ca*+ and Mgz+ clathrates. We were particularly interested in the rotational barrier existing between two extreme conformers of GABA and its modification upon metal complexing. We found that the pseudopotential method predicts a coordination of the ions to GABA and that this coordination inverts the rotational barrier observed for the isolated molecule. We also looked into the adequacy of CNDO for the study of this type of coordination and found several shortcomings in its predictions. The biological implications of these findings are discussed and a hypothesis on the role of a GABA-Ca*+ complex is presented.Nous avons fait des calculs ab inifio a l'aide de pseudopotentiels, et des calculs de type CNDO pour I'acide y-aminobutyrique (GABA) et ses clathrates avec Ca2+ et Mg2+. Nous avons etudit en particulier la barrikre rotationelle entre deux conformations extrsmes du GABA et de sa modification suivant la formation d'un complexe mttallique. La mtthode utilisant le pseudopotentiel prtdit une coordination des ions au GABA et cette coordination invertit la barrikre rotationelle observte pour la moltcule isolte. Nous avons examint aussi I'aptitude de la mtthode CNDO pour l'ttude de ce type de coordination et nous avons trouvt plusieurs dtsaccords dans ses prtdictions. Les implications biologiques des ces rksultats sont discutees, et une hypothese sur le r61e d'un complexe GABA-Ca2+ est prtsentee.Ab-initio-Pseudopotential-und CNDO-Rechnungen sind fur y-Aminobutyrsaure (GABA) und ihre Ca2+ und Mg*+-Clathraten ausgefiihrt worden. Wir interessieren uns besonders fur die Rotationsschwelle zwischen den zwei Extremkonformationen von GABA und ihrer metallkomplexierten Modifikation. Nach der Pseudopotentialmethode sind die Ionen zu GABA koordiniert, und diese Koordination invertiert die fur das isolierte Molekiil observierte Rotationsschwelle. Wir haben auch die Angemessenheit der cNDo-Methode fur die Untersuchung dieses Koordinationstyps studiert und mehrere falschen Vorhersagungen gefunden. Die biologischen Implikationen dieser Ergebnisse werden diskutiert und eine Hypothese iiber der Rolle eines GABA-Ca'+-Komplexes wird prasentiert.

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Conformational adaptability at GABA-sensitive inhibitory synapses

Cited by 11 publications

References 25 publications

Inhibition of [³H]GABA Binding to Postsynaptic Receptors in Human Cerebellar Synaptic Membranes by Carboxyl and Amino Derivatives of GABA

Inhibition of [³H]GABA Binding to Postsynaptic Receptors in Human Cerebellar Synaptic Membranes by Carboxyl and Amino Derivatives of GABA

GABA analogues: conformational analysis of effects on [³H]GABA binding to postsynaptic receptors in human cerebellum

Magnesium and calcium cation–ligand interactions within the pseudopotential approach. II. Cation–GABA interactions

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Conformational adaptability at GABA-sensitive inhibitory synapses

Cited by 11 publications

References 25 publications

Inhibition of [3H]GABA Binding to Postsynaptic Receptors in Human Cerebellar Synaptic Membranes by Carboxyl and Amino Derivatives of GABA

Inhibition of [3H]GABA Binding to Postsynaptic Receptors in Human Cerebellar Synaptic Membranes by Carboxyl and Amino Derivatives of GABA

GABA analogues: conformational analysis of effects on [3H]GABA binding to postsynaptic receptors in human cerebellum

Magnesium and calcium cation–ligand interactions within the pseudopotential approach. II. Cation–GABA interactions

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Inhibition of [³H]GABA Binding to Postsynaptic Receptors in Human Cerebellar Synaptic Membranes by Carboxyl and Amino Derivatives of GABA

Inhibition of [³H]GABA Binding to Postsynaptic Receptors in Human Cerebellar Synaptic Membranes by Carboxyl and Amino Derivatives of GABA

GABA analogues: conformational analysis of effects on [³H]GABA binding to postsynaptic receptors in human cerebellum