GABAB Receptor by Giancarlo Colombo

By Giancarlo Colombo

An up to date accomplished review of the GABA B receptor method with a selected concentrate on the newest healing functions and capability. This receptor procedure has lately been implicated in different ailments and issues together with gastroesophageal reflux illness, epilepsy, temper problems, melancholy, and alcohol and substance use disease. The authors, top researchers within the box, discover a few techniques, together with medicinal chemistry, molecular biology, body structure, and preclinical and scientific pharmacology. This evaluate offers a translational standpoint at the strength of the GABA B receptor pharmacology.

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Penn, R. , & Kroin, J. S. (1984). Intrathecal baclofen alleviates spinal cord spasticity. Lancet, 323(8385), 1078. 1 A Brief History of the GABAB Receptor 13 Penn, R. , & Kroin, J. S. (1985). Continuous intrathecal baclofen for severe spasticity. Lancet, 326(8447), 125–127. Santos, A. , Carvalho, C. , Macedo, T. , & Carvalho, A. P. (1995). Regulation of intracellular [Ca2+] GABA release by presynaptic GABAB receptors in rat cerebrocortical synaptosomes. Neurochemistry International, 27, 397–406.

Salyer, A. , Kim, E. , Jarrard, R. , Powers, M. , et al. (2013). Evaluation of difluoromethylketones as agonists of the γ-aminobutyric acid type B (GABAB) receptor. Journal of Medicinal Chemistry, 56, 2456–2465. , & Johnston, G. A. R. (2008). Enantioselective actions of 4-amino-3hydroxybutanoicacid and (3-amino-2-hydroxypropyl)methylphosphinic acid at recombinant GABAC receptors. Bioorganic and Medicinal Chemistry Letters, 18, 402–404. , & Zhang, L. (2009). An efficient synthesis of (R)- and (S)-baclofen via desymmetrization.

De Boer, A. , & Breimer, D. D. (1991). Stereoselective transport of baclofen across the blood-brain barrier in rats as determined by the unit impulse response methodology. Pharmaceutical Research, 8, 259–262. Wagner, P. , & Deakin, M. S. (1993). GABAB receptors are coupled to a barium-insensitive outward rectifying potassium conductance in premotor respiratory neurons. Journal of Neurophysiology, 69, 286–289. White, J. , Fraser, N. , Disney, G. , et al. (1998). Heterodimerization is required for the formation of a functional GABAB receptor.

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