|
1-Methyltryptamine
1-Methyltryptamine (1-methyl-T, 1-MT or 1-Me-T; code name PAL-637) is a serotonin receptor agonist and monoamine releasing agent of the substituted tryptamine, tryptamine family. It is the 1-methyl group, methyl chemical derivative, derivative of tryptamine (T; PAL-235). The drug is known to act as a serotonin 5-HT2A receptor, 5-HT2A receptor agonist (Ki = 473nM; = 209–4,560nM; = 55–99%), as a serotonin releasing agent ( = 53.1nM), and to be inactive in inducing the release of norepinephrine and dopamine ( = >10,000nM). Its activities at other serotonin receptors were not reported. 1-Methyltryptamine shows dramatically reduced affinity (pharmacology), affinity and receptor activation, activational potency (pharmacology), potency as well as reduced intrinsic activity, efficacy at the serotonin 5-HT2A receptor compared to tryptamine (which showed Ki = 13.1nM; = 7.36–99nM; = 101–104%). It also shows slightly reduced potency as a serotonin releasing agent and abolished act ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
