T-Type Ca2+ channel inhibitors hold tremendous therapeutic potential for the treatment of pain, epilepsy, sleep disorders, essential tremor, and other neurological disorders . ML 218 is a selective, potent inhibitor of T-type Ca2+ channels (IC50 values are 270 and 310 nM for CaV3.3 and CaV3.2 respectively in a patch EP assay). It has no effect on other members of the Ca2+ family of ion channels (L- and N-type Ca2+ channels) as well as multiple Na+ and K+ channels. ML 218 was found to be non-selective against hERG and many other ion channels. ML 218 possess excellent DMPK properties, acceptable in vivo rat PK, excellent brain levels and was efficacious in a haloperidol-induced catalepsy assay, a preclinical Parkinsonian model. ML 218 decreases burst activity in subthalamic nucleus (STN) neurons. Thus, ML 218 is a powerful new probe to study T-Type Ca2+ function both in vitro and in vivo .
产品描述
A Selective Blocker of T-type Channels
产品形式
T-Type Ca2+ channel inhibitors hold tremendous therapeutic potential for the treatment of pain, epilepsy, sleep disorders, essential tremor, and other neurological disorders . ML 218 is a selective, potent inhibitor of T-type Ca2+ channels (IC50 values are 270 and 310 nM for CaV3.3 and CaV3.2 respectively in a patch EP assay). It has no effect on other members of the Ca2+ family of ion channels (L- and N-type Ca2+ channels) as well as multiple Na+ and K+ channels. ML 218 was found to be non-selective against hERG and many other ion channels. ML 218 possess excellent DMPK properties, acceptable in vivo rat PK, excellent brain levels and was efficacious in a haloperidol-induced catalepsy assay, a preclinical Parkinsonian model. ML 218 decreases burst activity in subthalamic nucleus (STN) neurons. Thus, ML 218 is a powerful new probe to study T-Type Ca2+ function both in vitro and in vivo .