3-Methoxytyramine occurs naturally in the prickly pear cactus (genus Opuntia),[3] and is in general widespread throughout the Cactaceae.[4] It has also been found in crown gall tumors on Nicotiana sp.[5]
Originally thought to be physiologically inactive, 3-MT was subsequently found to act as an agonist of the rodent and human TAAR1.[1][9][2] 3-MT can induce weak hyperlocomotion in mice and this effect is partially attenuated in TAAR1 knockout mice.[2][10]
^ abcKhan MZ, Nawaz W (October 2016). "The emerging roles of human trace amines and human trace amine-associated receptors (hTAARs) in central nervous system". Biomed. Pharmacother. 83: 439–449. doi:10.1016/j.biopha.2016.07.002. PMID27424325.
^ abcMiller GM (January 2011). "The emerging role of trace amine-associated receptor 1 in the functional regulation of monoamine transporters and dopaminergic activity". Journal of Neurochemistry. 116 (2): 164–176. doi:10.1111/j.1471-4159.2010.07109.x. PMC3005101. PMID21073468. The data support the hypothesis that TAAR1 inhibits locomotor activity via a down-modulation of dopamine neurotransmission (Lindemann et al. 2008) and that the overruling effect of blocking TAAR1 is a net increase in the firing rate of DA neurons (Bradaia et al. 2009). However, a more recent study by Sotnikova et al. (2010) reports that the major extracellular metabolite of dopamine, 3-methoxytyramine, which is an agonist at rat TAAR1 (Bunzow et al. 2001), can induce mild hyperactivity in normal mice and a complex set of abnormal involuntary movements in normal mice acutely depleted of dopamine, and that these effects were attenuated in TAAR1 knockout mice. These data suggest that TAAR1 activation may stimulate locomotor activity. Collectively, the data illustrate a complexity of TAAR1 neurobiology that is still not fully understood.
^Neuwinger HD (1996). "Cactaceae". African ethnobotany: poisons and drugs: chemistry, pharmacology, toxicology. CRC Press. p. 271. ISBN978-3-8261-0077-2. Retrieved on June 12, 2009 through Google Book Search.
^Lindemann L, Hoener MC (May 2005). "A renaissance in trace amines inspired by a novel GPCR family". Trends in Pharmacological Sciences. 26 (5): 274–281. doi:10.1016/j.tips.2005.03.007. PMID15860375.
^Wang X, Li J, Dong G, Yue J (February 2014). "The endogenous substrates of brain CYP2D". European Journal of Pharmacology. 724: 211–218. doi:10.1016/j.ejphar.2013.12.025. PMID24374199.
Notes: (1) TAAR1 activity of ligands varies significantly between species. Some agents that are TAAR1 ligands in some species are not in other species. This navbox includes all TAAR1 ligands regardless of species. (2) See the individual pages for references, as well as the List of trace amines, TAAR, and TAAR1 pages. See also:Receptor/signaling modulators
