C3220 Unit 2 Assignment 1
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XAP044 is a mGluR7 antagonist.
The function of metabotropic glutamate receptor subtype 7 (mGlu7), an critical presynaptic regulator of neurotransmission in the mammalian CNS, has been linked to drug abuse, anxiety, autism, as well as depression. However, it is difficult to develop specific blockers of native mGlu7 signaling in relevant brain areas such as limbic cortex and amygdala.
In vitro: Previous study showed that in contrast to all previous mGlu7-selective drugs, XAP044 did not act through the seven-transmembrane region but rather via a binding pocket localized in mGlu7 's extracellular Venus flytrap domain, a region identified for orthosteric agonist binding, which was suggested by the chimeric receptor
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