TCB-2 explained

TCB-2 is a hallucinogen discovered in 2006 by Thomas McLean working in the lab of David Nichols at Purdue University.^[1] It is a conformationally-restricted derivative of the phenethylamine 2C-B, also a hallucinogen, and acts as a potent agonist for the 5-HT_2A and 5-HT_2C receptors with a K_i of 0.26 nM at the human 5-HT_2A receptor. In drug-substitution experiments in rats, TCB-2 was found to be of similar potency to both LSD and Bromo-DragonFLY, ranking it among the most potent phenethylamine hallucinogens yet discovered.^[1] This high potency and selectivity has made TCB-2 useful for distinguishing 5-HT_2A mediated responses from those produced by other similar receptors.^[2] TCB-2 has similar but not identical effects in animals to related phenethylamine hallucinogens such as DOI, and has been used for studying how the function of the 5-HT_2A receptor differs from that of other serotonin receptors in a number of animal models, such as studies of cocaine addiction and neuropathic pain.^{[3] [4] [5] [6]}

See also

• β-Methyl-2C-B
• 2CB-Ind
• 2CBCB-NBOMe
• Ivabradine
• Jimscaline
• LPH-5 (drug)
• S33005
• ZC-B

Notes and References

1. McLean TH, Parrish JC, Braden MR, Marona-Lewicka D, Gallardo-Godoy A, Nichols DE . 1-Aminomethylbenzocycloalkanes: conformationally restricted hallucinogenic phenethylamine analogues as functionally selective 5-HT2A receptor agonists . Journal of Medicinal Chemistry . 49 . 19 . 5794–803 . September 2006 . 16970404 . 10.1021/jm060656o . 10.1.1.688.9849 .
2. Chang CW, Poteet E, Schetz JA, Gümüş ZH, Weinstein H . Towards a quantitative representation of the cell signaling mechanisms of hallucinogens: measurement and mathematical modeling of 5-HT1A and 5-HT2A receptor-mediated ERK1/2 activation . Neuropharmacology . 56 . 213–25 . 2009 . Suppl 1 . 18762202 . 2635340 . 10.1016/j.neuropharm.2008.07.049 .
3. Fox MA, French HT, LaPorte JL, Blackler AR, Murphy DL . The serotonin 5-HT(2A) receptor agonist TCB-2: a behavioral and neurophysiological analysis . Psychopharmacology . 212 . 1 . 13–23 . September 2010 . 19823806 . 10.1007/s00213-009-1694-1 . 22499760 .
4. Aira Z, Buesa I, Salgueiro M, Bilbao J, Aguilera L, Zimmermann M, Azkue JJ . Subtype-specific changes in 5-HT receptor-mediated modulation of C fibre-evoked spinal field potentials are triggered by peripheral nerve injury . Neuroscience . 168 . 3 . 831–41 . July 2010 . 20412834 . 10.1016/j.neuroscience.2010.04.032 . 207248287 .
5. Katsidoni V, Apazoglou K, Panagis G . Role of serotonin 5-HT2A and 5-HT2C receptors on brain stimulation reward and the reward-facilitating effect of cocaine . Psychopharmacology . 213 . 2–3 . 337–54 . February 2011 . 20577718 . 10.1007/s00213-010-1887-7 . 1580337 .
6. Zhang G, Ásgeirsdóttir HN, Cohen SJ, Munchow AH, Barrera MP, Stackman RW . Stimulation of serotonin 2A receptors facilitates consolidation and extinction of fear memory in C57BL/6J mice . Neuropharmacology . 64 . 403–13 . January 2013 . 1 . 22722027 . 3477617 . 10.1016/j.neuropharm.2012.06.007 .