1Z2MAP1O
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1Z2MAP1O
1Z2MAP1O, also known as 1-(indolizin-3-yl)-2-(methylamino)propan-1-one, is a monoamine releasing agent and serotonin receptor receptor modulator, modulator of the indolizine class. It is an structural analog, analogue of BK-NM-AMT (β-keto-''N''-methyl-α-methyltryptamine) in which the indole ring (chemistry), ring has been replaced with an indolizine ring. 1Z2MAP1O has been found to be a serotonin releasing agent, serotonin and dopamine releasing agent as well as a weak serotonin 5-HT1B receptor, 5-HT1B receptor agonist and serotonin 5-HT2B receptor, 5-HT2B receptor receptor antagonist, antagonist. Conversely, its activity as a norepinephrine releasing agent was not reported, and it was inactive at the remaining sites of the 47screened biological target, targets. The drug's values for induction of monoamine release were 109nM for serotonin and 227nM for dopamine in Chinese hamster ovary cell, Chinese hamster ovary (CHO) cell (biology), cells expressing the human monoamine transp ...
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Monoamine Releasing Agent
A monoamine releasing agent (MRA), or simply monoamine releaser, is a drug that induces the release of one or more monoamine neurotransmitters from the presynaptic neuron into the synapse, leading to an increase in the extracellular concentrations of the neurotransmitters and hence enhanced signaling by those neurotransmitters. The monoamine neurotransmitters include serotonin, norepinephrine, and dopamine; MRAs can induce the release of one or more of these neurotransmitters. MRAs work by reversing the direction of the monoamine transporters (MATs), including the serotonin transporter (SERT), norepinephrine transporter (NET), and/or dopamine transporter (DAT), causing them to promote efflux of non-vesicular cytoplasmic monoamine neurotransmitter rather than reuptake of synaptic monoamine neurotransmitter. Many, but not all MRAs, also reverse the direction of the vesicular monoamine transporter 2 (VMAT2), thereby additionally resulting in efflux of vesicular monoamine neuro ...
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