Receptorium GABA

Receptoria GABA sunt grex receptoriorum neurotransmissoris, quae in vertebratorum systemate nervoso centrali ab neurotransmissore inhibente GABA stimulantur^[1]. Adhuc tres classes inventae sunt: Receptoria GABA_A ac receptoria GABA_A-ρ ionotropicae enim et receptoria GABA_B proteino G copulata. Nimirum velocitates eorundem divertunt: Cum ionotropica celeriora essent, ita proteino G copulatum GABA_B tardius est.

Per receptoria GABA in vertebratorum systemate nervoso centrali operationes inhibentes principales^[2] excellunt.

Praeterea receptoriis GABA in iecoris hepatocytis quoque et cholangiocytis ductūs biliaris^[3] functiones enim, velut in pancreate^[4], sunt.

Acidum γ-aminobutyricum, "GABA" abbreviatum

Receptoria GABA_A

Quodque receptorium GABA_A est canalis ionticus imprimis chloridi, proinde ionotropicum receptorium.^[5] Subunitates receptorii variae, quo quinque partes (heteropentamero) sunt, descriptae sunt. Alkaloidum bicucullinum antagonista selectivus competitivusque haec receptoria inhibit.

Agonistae

Conferatur pagina principalis: Agonista (biochemia).

Diazepamum (non selectivus)^[6]
Muscimolum agonista selectivus receptorii GABA_A est.

Antagonistae

Bicucullinum (GABA_A, selectivus et competitivus)^[7]

Notae

↑ Watanabe M., Maemura K., Kanbara K., Tamayama T., Hayasaki H. (2002). "GABA and GABA receptors in the central nervous system and other organs". International Revue of Cytology 213: 1-47
↑ Olsen R. W., Tobin A. J. (1990). "Molecular biology of GABAA receptors". FASEB journal 4 (5): 1469-80
↑ Wang S., Zhang L., Liu C., Lu W. Y. (2017). "Protective roles of hepatic GABA signaling in liver injury". International journal of physiology, pathophysiology and pharmacology 9 (5): 153-6
↑ Dong H., Kumar M., Zhang Y., Gyulkhandanyan A., Xiang Y. Y., Ye B., Perrella J., Hyder A., Zhang N., Wheeler M., Lu W. Y., Wang Q. (2006). "Gamma-aminobutyric acid up- and downregulates insulin secretion from beta cells in concert with changes in glucose concentration". Diabetologia 49 (4): 697-705
↑ Olsen R. W., Sieghart W. (2008). "International Union of Pharmacology. LXX. Subtypes of gamma-aminobutyric acid(A) receptors: classification on the basis of subunit composition, pharmacology, and function. Update". Pharmacol Rev 60 (3): 243-60 .
↑ Atack J. R. (2005). "The benzodiazepine binding site of GABA(A) receptors as a target for the development of novel anxiolytics". Expert Opin Investig Drugs 14 (5): 601-18
↑ Curtis D. R., Duggan A. W., Felix D., Johnston G. A. (Sep 1971). "Bicuculline, an antagonist of GABA and synaptic inhibition in the spinal cord of the cat". Brain research 32 (1): 69-96 doi:10.1016/0006-8993(71)90156-9

Nexus interni

[1] Watanabe M., Maemura K., Kanbara K., Tamayama T., Hayasaki H. (2002). "GABA and GABA receptors in the central nervous system and other organs". International Revue of Cytology 213: 1-47

[2] Olsen R. W., Tobin A. J. (1990). "Molecular biology of GABAA receptors". FASEB journal 4 (5): 1469-80

[3] Wang S., Zhang L., Liu C., Lu W. Y. (2017). "Protective roles of hepatic GABA signaling in liver injury". International journal of physiology, pathophysiology and pharmacology 9 (5): 153-6

[4] Dong H., Kumar M., Zhang Y., Gyulkhandanyan A., Xiang Y. Y., Ye B., Perrella J., Hyder A., Zhang N., Wheeler M., Lu W. Y., Wang Q. (2006). "Gamma-aminobutyric acid up- and downregulates insulin secretion from beta cells in concert with changes in glucose concentration". Diabetologia 49 (4): 697-705

[5] Olsen R. W., Sieghart W. (2008). "International Union of Pharmacology. LXX. Subtypes of gamma-aminobutyric acid(A) receptors: classification on the basis of subunit composition, pharmacology, and function. Update". Pharmacol Rev 60 (3): 243-60 .

[6] Atack J. R. (2005). "The benzodiazepine binding site of GABA(A) receptors as a target for the development of novel anxiolytics". Expert Opin Investig Drugs 14 (5): 601-18

[7] Curtis D. R., Duggan A. W., Felix D., Johnston G. A. (Sep 1971). "Bicuculline, an antagonist of GABA and synaptic inhibition in the spinal cord of the cat". Brain research 32 (1): 69-96 doi:10.1016/0006-8993(71)90156-9

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