Saclofen is a competitive antagonist for the GABAB receptor. This drug is an analogue of the GABAB agonist baclofen. The GABAB receptor is heptahelical receptor, expressed as an obligate heterodimer, which couples to the Gi/o class of heterotrimeric G-proteins. The action of saclofen on the central nervous system is understandably modest, because G-proteins rely on an enzyme cascade to alter cell behavior while ionotropic receptors immediately change the ionic permeability of the neuronal plasma membrane, thus changing its firing patterns. These particular receptors, presynaptically inhibit N- and P/Q- voltage-gated calcium channels (VGCCs) via a direct interaction of the dissociated beta gamma subunit of the g-protein with the intracellular loop between the 1st and 2nd domain of the VGCC's alpha-subunit; postsynaptically, these potentiate Kir currents. Both result in inhibitory effects.

CAS：125464-42-8
中文别名：3-氨基-2-(4-氯苯基-丙烷磺酸;Β-(氨甲基)-4 氯代苯乙烷磺酸;Beta-(氨基甲基)-4 氯代苯乙烷磺酸;
英文别名：3-amino-2-(4-chlorophenyl)propane-1-sulfonic acid;
分子式：C9H12ClNO3S
分子量：249.714
精确质量：249.023
Psa：88.77
Logp：3.0512

MDL号：MFCD00216817

外观与性状：白色结晶固体
密度：1.437 g/cm3
折射率：1.6

WGK Germany：3
海关编码：2921499090