(+)- and (-)-cis-2-aminomethylcyclopropanecarboxylic acids show opposite pharmacology at recombinant ρ1 and ρ2 GABA(C) receptors

Journal of Neurochemistry

Volumn 75, Issue 6, 2000, Pages 2602-2610

  Duke, Rujee K ^a   Chebib, Mary ^a   Balcar, Vladimir J ^a   Allan, Robin D ^a   Mewett, Kenneth N ^a   Johnston, Graham A R ^a  

^a University of Sydney   (Australia)

Author keywords

( ) cis and ( ) trans 2 Aminomethylcyclopropanecarboxylic acids; GABA(A) receptors; GABA(c) receptors; Molecular modeling; Xenopus oocytes

Indexed keywords

2 AMINOMETHYLCYCLOPROPANECARBOXYLIC ACID; 4 AMINOBUTYRIC ACID A RECEPTOR; 4 AMINOBUTYRIC ACID C RECEPTOR; 4 AMINOBUTYRIC ACID DERIVATIVE; CYCLOPROPANECARBOXYLIC ACID DERIVATIVE; PARTIAL AGONIST; RECEPTOR SUBTYPE; RECOMBINANT RECEPTOR; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; CIS TRANS ISOMERISM; CONTROLLED STUDY; DRUG RECEPTOR BINDING; GABAERGIC SYSTEM; HUMAN; NONHUMAN; PRIORITY JOURNAL; PROTEIN EXPRESSION; VOLTAGE CLAMP; XENOPUS LAEVIS;

AMINO ACIDS, CYCLIC; ANIMALS; BINDING, COMPETITIVE; BRAIN; CELLS, CULTURED; CROTONIC ACIDS; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DESIGN; GABA AGONISTS; GAMMA-AMINOBUTYRIC ACID; HUMANS; MODELS, MOLECULAR; OOCYTES; RECEPTORS, GABA; RECEPTORS, GABA-A; RECOMBINANT PROTEINS; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; TRANSFECTION; XENOPUS LAEVIS;

ANIMALIA; XENOPUS LAEVIS;

EID: 0033769321     PISSN: 00223042     EISSN: None     Source Type: Journal    
DOI: 10.1046/j.1471-4159.2000.0752602.x     Document Type: Article

References (52)

1. The synthesis and activity of cis- and trans-2-(aminomethyl)cyclopropanecarboxylic acid as conformationally restricted analogues of GABA
2. Synthesis of analogues of GABA. XIII. An alternative route to (Z)-4-aminocrotonic acid
3. Homomeric rho 1 GABA channels: Activation properties and domains
4. High affinity uptake of transmitters: Studies on the uptake of L-aspartate, GABA, L-glutamate and glycine in cat spinal cord
5. Liberation of amino acids during the preparation of brain slices
6. Autoradiography of P2X ATP receptors in the rat brain
7. International Union of Pharmacology. XV. Subtypes of GABA(A) receptors: Classification on the basis of subunit structure and receptor function
8. GABA(B) receptors: Drugs meet clones
9. GABA transporter heterogeneity: Pharmacology and cellular localization
10. Tiagabine, SKandF 89976A, CI-966 and NNC-771 are selective for the cloned GABA transporter GAT-1
11. GABA(c) receptors
12. Analogues of γ-aminobutyric acid (GABA) and trans-4-aminocrotonic acid (TACA) substituted in the 2 position as GABA(c) receptor antagonists
13. 2 receptors expressed in Xenopus oocytes
14. Functional expression and CNS distribution of a β-alanine sensitive neuronal GABA transporter
15. Structural selectivity and molecular nature of L-glutamate transport in cultured human fibroblasts
16. 1 cDNA: A novel GABA subunit highly expressed in the retina
17. 1 to human chromosome 6q14-q21 and the mouse chromosome 4
18. Insensitivity to anaesthetic agents conferred by class of GABA(A) receptor subunit
19. Bicuculline-insensitive GABA receptors: Studies on the binding of (-)baclofen to rat cerebellar membranes
20. Resolution and conformational analysis of diastereoisomeric esters of cis- and trans-2-(aminomethyl)-1-carboxycyclopropanes
21. Resolution, absolute stereochemistry, and pharmacology of the S-(+)- and R-(-)-isomers of the apparent partial AMPA receptor agonist (R, S)-2-amino-3-(3-hydroxy-5-phenylisoxazol-4-yl)propionic acid [(R, S)-APPA]
22. Molecular pharmacology of γ-aminobutyric acid type A receptor agonists and partial agonists in oocytes injected with different α, β and γ receptor subunit combinations
23. Cloning and expression of a rat brain GABA transporter
24. The N-terminal domain of human GABA receptor rhol subunits contains signals for homooligomeric and heterooligomeric interaction
25. Sequences in the amino termini of GABA ρ and GABA(A) subunits specify their selective interaction in vitro
26. Structural and physicochemical factors in drug action
27. GABA uptake in central nervous system: Comparison of uptake in slices and homogenates and the effects of some inhibitors
28. GABA(A) receptor pharmacology
29. GABA(c) receptors relatively simple transmitter-gated ion-channels?
30. cis- and trans-4-Aminocrotonic acid as GABA analogues of restricted conformation
31. GABA(B) receptors function as a heteromeric assembly of the subunits GABA(B)R1 and GABA(B)R2
32. Expression cloning of GABA(B) receptors uncovers similarity to metabotropic glutamate receptors
33. GABA(B)-receptor subtypes assemble into functional heteromeric complexes
34. GABA(B) receptors
35. Synthesis of novel GABA uptake inhibitors. 3. Diaryloxime and diarylvinyl ether derivatives of nipecotic acid and guvacine as anticonvulsant agents
36. 1 and GABA α/β receptors expressed in Xenopus oocytes and COS cells
37. 1
38. Which GABA(A)-receptor subtypes really occur in the brain?
39. GAT-1, a high affinity GABA plasma membrane transporter, is localized to neurones and astroglia in the cerebral cortex
40. Fitting curves to data using non-linear regression: A practical and non-mathematical review
41. LIGAND: A versatile computerised approach for characterisation of ligand binding systems
42. The first selective antagonist for GABA(c) receptors
43. 3 cDNA
44. 2-subunit cDNA
45. A light and electron microscopic study of GAT-1-positive cells in the cerebral cortex of man and monkey
46. Design and in vitro pharmacology for a selective γ-aminobutyric acid(c) receptor antagonist
47. Barbiturate interactions at the GABA(A) receptor: Dependence on receptor subunit combination
48. 2) cloned from human retina forms bicuculline-insensitive homooligomeric receptors in Xenopus oocytes
49. Heterodimerization is required for the formation of a functional GABA(B) receptor
50. Characterization of bicuculline/baclofen-insensitive (ρ-like) γ-aminobutyric acid receptors expressed in Xenopus oocytes. II. Pharmacology of γ-aminobutyric acid(A) and γ-aminobutyric acid(B) receptor agonists and antagonists
51. 3H]α,β-methylene-ATP binding in rat brain
52. Cloning of gamma-aminobutyric acid type C receptor subunit in rat retina with a methionine residue critical for picrotoxinin channel block