Difference between revisions of "KM-233"
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| − | KM-233 is a drug which is an analogue of Δ8-tetrahydrocannabinol ([[THC]]), the less active but more stable isomer of the active component of [[Cannabis]]. km-233 differs from Δ8-THC by the pentyl side chain being replaced by a 1,1-dimethylbenzyl group. It has high binding affinity in vitro for both the [[CB1]] and [[CB2 receptor]]s, with a CB2 affinity of 0.91nM and 13x selectivity over the CB1 receptor. In animal studies it has been found to be effective for the treatment of glioma, a form of brain tumor. A large number of related analogues are known where the 1,1-dimethylbenzyl group is substituted or replaced by other groups, with a fairly well established structure-activity relationship. | + | '''KM-233''' is a drug which is an analogue of Δ8-tetrahydrocannabinol ([[THC]]), the less active but more stable isomer of the active component of [[Cannabis]]. km-233 differs from Δ8-THC by the pentyl side chain being replaced by a 1,1-dimethylbenzyl group. It has high binding affinity in vitro for both the [[CB1]] and [[CB2 receptor]]s, with a CB2 affinity of 0.91nM and 13x selectivity over the CB1 receptor. In animal studies it has been found to be effective for the treatment of glioma, a form of brain tumor. A large number of related analogues are known where the 1,1-dimethylbenzyl group is substituted or replaced by other groups, with a fairly well established structure-activity relationship. |
== See also == | == See also == | ||
Latest revision as of 02:59, 15 February 2015
KM-233 is a drug which is an analogue of Δ8-tetrahydrocannabinol (THC), the less active but more stable isomer of the active component of Cannabis. km-233 differs from Δ8-THC by the pentyl side chain being replaced by a 1,1-dimethylbenzyl group. It has high binding affinity in vitro for both the CB1 and CB2 receptors, with a CB2 affinity of 0.91nM and 13x selectivity over the CB1 receptor. In animal studies it has been found to be effective for the treatment of glioma, a form of brain tumor. A large number of related analogues are known where the 1,1-dimethylbenzyl group is substituted or replaced by other groups, with a fairly well established structure-activity relationship.
