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trans‐4‐Amino‐2‐methylbut‐2‐enoic acid (2‐MeTACA) and (±)‐trans‐2‐aminomethylcyclopropanecarboxylic acid ((±)‐TAMP) can differentiate rat ρ3 from human ρ1 and ρ2 recombinant GABAC receptors
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trans‐4‐Amino‐2‐methylbut‐2‐enoic acid (2‐MeTACA) and (±)‐trans‐2‐aminomethylcyclopropanecarboxylic acid ((±)‐TAMP) can differentiate rat ρ3 from human ρ1 and ρ2 recombinant GABAC receptors
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trans‐4‐Amino‐2‐methylbut‐2‐enoic acid (2‐MeTACA) and (±)‐trans‐2‐aminomethylcyclopropanecarboxylic acid ((±)‐TAMP) can differentiate rat ρ3 from human ρ1 and ρ2 recombinant GABAC receptors
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Journal Article
trans‐4‐Amino‐2‐methylbut‐2‐enoic acid (2‐MeTACA) and (±)‐trans‐2‐aminomethylcyclopropanecarboxylic acid ((±)‐TAMP) can differentiate rat ρ3 from human ρ1 and ρ2 recombinant GABAC receptors
2002
Overview
This study investigated the effects of a number of GABA analogues on rat ρ3 GABAC receptors expressed in Xenopus oocytes using 2‐electrode voltage clamp methods. The potency order of agonists was muscimol (EC50=1.9±0.1 μM) (+)‐trans‐3‐aminocyclopentanecarboxylic acids ((+)‐TACP; EC50=2.7±0.9 μM) trans‐4‐aminocrotonic acid (TACA; EC50=3.8±0.3 μM) GABA (EC50=4.0±0.3 μM) > thiomuscimol (EC50=24.8±2.6 μM) > (±)‐cis‐2‐aminomethylcyclopropane‐carboxylic acid ((±)‐CAMP; EC50=52.6±8.7 μM) > cis‐4‐aminocrotonic acid (CACA; EC50=139.4±5.2 μM). The potency order of antagonists was (±)‐trans‐2‐aminomethylcyclopropanecarboxylic acid ((±)‐TAMP; KB=4.8±1.8 μM) (1,2,5,6‐tetrahydropyridin‐4‐yl)methylphosphinic acid (TPMPA; KB=4.8±0.8 μM) > (piperidin‐4‐yl)methylphosphinic acid (P4MPA; KB=10.2±2.3 μM) 4,5,6,7‐tetrahydroisoxazolo[5,4‐c]pyridin‐3‐ol (THIP; KB=10.2±0.3 μM) imidazole‐4‐acetic acid (I4AA; KB=12.6±2.7 μM) > 3‐aminopropylphosphonic acid (3‐APA; KB=35.8±13.5 μM). trans‐4‐Amino‐2‐methylbut‐2‐enoic acid (2‐MeTACA; 300 μM) had no effect as an agonist or an antagonist indicating that the C2 methyl substituent is sterically interacting with the ligand‐binding site of rat ρ3 GABAC receptors. 2‐MeTACA affects ρ1 and ρ2 but not ρ3 GABAC receptors. In contrast, (±)‐TAMP is a partial agonist at ρ1 and ρ2 GABAC receptors, while at rat ρ3 GABAC receptors it is an antagonist. Thus, 2‐MeTACA and (±)‐TAMP could be important pharmacological tools because they may functionally differentiate between ρ1, ρ2 and ρ3 GABAC receptors in vitro. British Journal of Pharmacology (2002) 135, 883–890; doi:10.1038/sj.bjp.0704432
Publisher
Wiley,Blackwell Publishing Ltd,Nature Publishing
Subject
Aminoacid receptors (glycine, glutamate, gaba)
/ Animals
/ Biological and medical sciences
/ Cell structures and functions
/ Fundamental and applied biological sciences. Psychology
/ Humans
/ Molecular and cellular biology
/ Oocytes
/ Rats
/ Structure-Activity Relationship
