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Chemical Compound Review:

TACA (E)-4-aminobut-2-enoic acid

Synonyms: CHEMBL33086, AC1NSJS2, BSPBio_002528, T1694_SIGMA, CCG-39246, ...

Akasu, T. et al., Nakayama, Y. et al., Ulloor, J. et al., Park, J.S. et al., Gamel-Didelon, K. et al., et al.

Gisselmann, Plonka, Pusch, Hatt, Nakayama, Hattori, Otani, Inagaki,

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Psychiatry related information on cis-4-Aminocrotonic acid

In contrast, when GABAA and GABAC receptors were activated by microinjecting their receptor selective agonists, isoguvacine (ISGV) and cis-4-aminocrotonic acid (CACA), respectively, the total percentages of REM sleep did not change compared with the control values [1].

High impact information on cis-4-Aminocrotonic acid

GABA-induced Cl- currents were recorded using the whole cell patch clamp technique; these currents were insensitive to bicuculline (a GABA-A antagonist) but could be induced by the GABA-C agonist cis-4-aminocrotonic acid [2].
gamma-Aminobutyric acid (GABA), trans-4-aminocrotonic acid (TACA), muscimol, imidazole-4-acetic acid (I4AA), cis-4-aminocrotonic acid (CACA), and isoguvacine are all GABA(C) receptor agonists [3].
GABA-C receptor subunits (rho1, rho2, rho3) and GABA synthesizing enzymes (GAD 65 and GAD 67) were shown to be expressed as assayed by RT-PCR, and GABA-C receptor stimulation by CACA obviously increased intracellular Ca2+ concentration in the anterior pituitary cells [4].
The heteromultimeric receptor is activated by GABA (EC50=4.5 microm), muscimol (EC50=4.8 microm) and trans-4-aminocrotonic acid (EC50=104.5 microm), and partially by cis-4-aminocrotonic acid (EC50=106.3 microm) [5].
CGP55845A (3 microM), a selective GABAB receptor antagonist, did not affect the GABA-induced responses. cis-4-Aminocrotonic acid (CACA, 1 mM) and trans-4-aminocrotonic acid (TACA, 1 mM), selective GABAC receptor agonists, produced late biphasic responses in the MPG neurons [6].

Biological context of cis-4-Aminocrotonic acid

From several potent inhibitors showing IC50 values at mGAT3 and mGAT4 in the low microM range cis-4-aminocrotonic acid and (RS)-2,3-diaminopropionic acid turned out to be most subtype selective for these transporters [7].

Associations of cis-4-Aminocrotonic acid with other chemical compounds

DRG neurons also responded to micromolar concentrations of pentobarbital and alphaxalone but not to cis-4-aminocrotonic acid (CACA), glycine, or taurine [8].
Unlike GABA(A) receptors, the GABA(C) receptor is a bicuculline-resistant chloride channel that is selectively activated by cis-4-aminocrotonic acid (CACA), and antagonized by imidazole-4-acetic acid (I4AA) and to some extent by picrotoxin [9].

Gene context of cis-4-Aminocrotonic acid

The selective GABA(C) receptor agonist cis-4-aminocrotonic acid (CACA) induced dose-dependent increases both of [Ca2+]i and of hormone (cholecystokinin) secretion [10].

References

Spontaneous REM sleep is modulated by the activation of the pedunculopontine tegmental GABAB receptors in the freely moving rat. Ulloor, J., Mavanji, V., Saha, S., Siwek, D.F., Datta, S. J. Neurophysiol. (2004) [Pubmed]
Molecular and physiological evidence for functional gamma-aminobutyric acid (GABA)-C receptors in growth hormone-secreting cells. Gamel-Didelon, K., Kunz, L., Fohr, K.J., Gratzl, M., Mayerhofer, A. J. Biol. Chem. (2003) [Pubmed]
Correlation of the apparent affinities and efficacies of gamma-aminobutyric acid(C) receptor agonists. Chang, Y., Covey, D.F., Weiss, D.S. Mol. Pharmacol. (2000) [Pubmed]
Gamma-aminobutyric acid (GABA)-C receptor stimulation increases prolactin (PRL) secretion in cultured rat anterior pituitary cells. Nakayama, Y., Hattori, N., Otani, H., Inagaki, C. Biochem. Pharmacol. (2006) [Pubmed]
Drosophila melanogaster GRD and LCCH3 subunits form heteromultimeric GABA-gated cation channels. Gisselmann, G., Plonka, J., Pusch, H., Hatt, H. Br. J. Pharmacol. (2004) [Pubmed]
Role of GABAA and GABAC receptors in the biphasic GABA responses in neurons of the rat major pelvic ganglia. Akasu, T., Munakata, Y., Tsurusaki, M., Hasuo, H. J. Neurophysiol. (1999) [Pubmed]
Novel parent structures for inhibitors of the murine GABA transporters mGAT3 and mGAT4. Kragler, A., Höfner, G., Wanner, K.T. Eur. J. Pharmacol. (2005) [Pubmed]
GABA-Induced Cl- current in cultured embryonic human dorsal root ganglion neurons. Valeyev, A.Y., Hackman, J.C., Holohean, A.M., Wood, P.M., Katz, J.L., Davidoff, R.A. J. Neurophysiol. (1999) [Pubmed]
Bicuculline-resistant, Cl- dependent GABA response in the rat spinal dorsal horn. Park, J.S., Higashi, H., Nagata, K., Yoshimura, M. Neurosci. Res. (1999) [Pubmed]
GABA(C) receptors in neuroendocrine gut cells: a new GABA-binding site in the gut. Jansen, A., Hoepfner, M., Herzig, K.H., Riecken, E.O., Scherübl, H. Pflugers Arch. (2000) [Pubmed]

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