6-APB: Difference between revisions

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==Pharmacology==

6-APB is a [[serotonin]]–[[norepinephrine]]–[[dopamine]] [[reuptake inhibitor]] (SNDRI) with Ki values of 117, 150, and 2698 nM for the norepinephrine transporter (NET), dopamine transporter (DAT), and serotonin transporter (SERT), respectively.<ref name="6APBpharm1">Iversen L, Gibbons S, Treble R, Setola V, Huang XP, Roth BL (2013). "Neurochemical profiles of some novel psychoactive substances". Eur. J. Pharmacol. 700 (1-3): 147–51. PMID 23261499. https://doi.~~org10~~.1016/j.ejphar.2012.12.006</ref> 6-APB also possesses additional activity as a [[releasing agent]] of these [[monoamine neurotransmitters]].<ref>Rickli A, Kopf S, Hoener MC, Liechti ME (2015). "Pharmacological profile of novel psychoactive benzofurans". Br. J. Pharmacol. 172 (13): 3412–25. PMID 25765500. https://doi.org/10.1111/bph.13128</ref>

6-APB is a [[serotonin]]–[[norepinephrine]]–[[dopamine]] [[reuptake inhibitor]] (SNDRI) with Ki values of 117, 150, and 2698 nM for the norepinephrine transporter (NET), dopamine transporter (DAT), and serotonin transporter (SERT), respectively.<ref name="6APBpharm1">Iversen L, Gibbons S, Treble R, Setola V, Huang XP, Roth BL (2013). "Neurochemical profiles of some novel psychoactive substances". Eur. J. Pharmacol. 700 (1-3): 147–51. PMID 23261499. https://doi.org/10.1016/j.ejphar.2012.12.006 https://www.sciencedirect.com/science/article/abs/pii/S0014299912010114?via=ihub</ref> 6-APB also possesses additional activity as a [[releasing agent]] of these [[monoamine neurotransmitters]].<ref>Rickli A, Kopf S, Hoener MC, Liechti ME (2015). "Pharmacological profile of novel psychoactive benzofurans". Br. J. Pharmacol. 172 (13): 3412–25. PMID 25765500. https://doi.org/10.1111/bph.13128</ref>

6-APB is a potent [[Agonists#Types of agonist|full agonist]] of the serotonin 5-HT2B receptor (Ki = 3.7 nM)<ref name="6APBpharm1" />, with higher affinity for this target than any other site.<ref name="5HT2C">Canal CE, Murnane KS (2017). "The serotonin 5-HT2C receptor and the non-addictive nature of classic hallucinogens". J. Psychopharmacol. (Oxford). 31 (1): 127–143. PMID 27903793. https://doi.org/10.1177/0269881116677104</ref> Moreover, unlike MDMA, 6-APB shows 100-fold selectivity for the 5-HT2B receptor over the 5-HT2A and 5-HT2C receptors.<ref name="5HT2C" /><ref>US patent 7045545, Karin Briner, Joseph Paul Burkhart, Timothy Paul Burkholder, Matthew Joseph Fisher, William Harlan Gritton, Daniel Timothy Kohlman, Sidney Xi Liang, Shawn Christopher Miller, Jeffrey Thomas Mullaney, Yao-Chang Xu, Yanping Xu, "Aminoalkylbenzofurans as serotonin (5-HT(2c)) agonists", published 19 January 2000, issued 16 May 2006</ref>

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 ==Pharmacology==
--APB is a [[serotonin]]–[[norepinephrine]]–[[dopamine]] [[reuptake inhibitor]] (SNDRI) with Ki values of 117, 150, and 2698 nM for the norepinephrine transporter (NET), dopamine transporter (DAT), and serotonin transporter (SERT), respectively.<ref name="6APBpharm1">Iversen L, Gibbons S, Treble R, Setola V, Huang XP, Roth BL (2013). "Neurochemical profiles of some novel psychoactive substances". Eur. J. Pharmacol. 700 (1-3): 147–51. PMID 23261499. https://doi.org10.1016/j.ejphar.2012.12.006</ref> 6-APB also possesses additional activity as a [[releasing agent]] of these [[monoamine neurotransmitters]].<ref>Rickli A, Kopf S, Hoener MC, Liechti ME (2015). "Pharmacological profile of novel psychoactive benzofurans". Br. J. Pharmacol. 172 (13): 3412–25. PMID 25765500. https://doi.org/10.1111/bph.13128</ref>
+-APB is a [[serotonin]]–[[norepinephrine]]–[[dopamine]] [[reuptake inhibitor]] (SNDRI) with Ki values of 117, 150, and 2698 nM for the norepinephrine transporter (NET), dopamine transporter (DAT), and serotonin transporter (SERT), respectively.<ref name="6APBpharm1">Iversen L, Gibbons S, Treble R, Setola V, Huang XP, Roth BL (2013). "Neurochemical profiles of some novel psychoactive substances". Eur. J. Pharmacol. 700 (1-3): 147–51. PMID 23261499. https://doi.org/10.1016/j.ejphar.2012.12.006 https://www.sciencedirect.com/science/article/abs/pii/S0014299912010114?via=ihub</ref> 6-APB also possesses additional activity as a [[releasing agent]] of these [[monoamine neurotransmitters]].<ref>Rickli A, Kopf S, Hoener MC, Liechti ME (2015). "Pharmacological profile of novel psychoactive benzofurans". Br. J. Pharmacol. 172 (13): 3412–25. PMID 25765500. https://doi.org/10.1111/bph.13128</ref>
 -APB is a potent [[Agonists#Types of agonist|full agonist]] of the serotonin 5-HT<sub>2B</sub> receptor (Ki = 3.7 nM)<ref name="6APBpharm1" />, with higher affinity for this target than any other site.<ref name="5HT2C">Canal CE, Murnane KS (2017). "The serotonin 5-HT2C receptor and the non-addictive nature of classic hallucinogens". J. Psychopharmacol. (Oxford). 31 (1): 127–143. PMID 27903793. https://doi.org/10.1177/0269881116677104</ref> Moreover, unlike MDMA, 6-APB shows 100-fold selectivity for the 5-HT<sub>2B</sub> receptor over the 5-HT<sub>2A</sub> and 5-HT<sub>2C</sub> receptors.<ref name="5HT2C" /><ref>US patent 7045545, Karin Briner, Joseph Paul Burkhart, Timothy Paul Burkholder, Matthew Joseph Fisher, William Harlan Gritton, Daniel Timothy Kohlman, Sidney Xi Liang, Shawn Christopher Miller, Jeffrey Thomas Mullaney, Yao-Chang Xu, Yanping Xu, "Aminoalkylbenzofurans as serotonin (5-HT(2c)) agonists", published 19 January 2000, issued 16 May 2006</ref>