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Tiflucarbine (BAY-P 4495 or TVX P 4495) is an experimental drug which acts as an agonist of the 5-HT1 and 5-HT2 serotonin receptor families, and also acts as a calmodulin inhibitor. It has antidepressant effects in animal studies.[1][2][3][4] It produces the head-twitch response, a behavioral proxy of psychedelic effects, in rodents.[2][5] In addition, it partially substituted for DOM and 8-OH-DPAT in rodent drug discrimination tests, with further generalization but concomitant substantial behavioral disruption in 5-MeO-DMT-trained rodents.[2] Tiflucarbine is similar in structure to but distinct from β-carbolines, instead being a γ-carboline.

See also

References

  1. ^ Maj J, Rogóz Z, Sowińska H, Zalewski Z (1987). “Some central effects of tiflucarbine, a new potential antidepressant drug”. Polish Journal of Pharmacology and Pharmacy. 39 (1): 63–74. PMID 2823240.
  2. ^ a b c Glennon RA, De Vry J, Spencer DG, Glaser T (December 1990). “Stimulus properties of tiflucarbine: a novel antidepressant agent”. Pharmacol Biochem Behav. 37 (4): 769–771. doi:10.1016/0091-3057(90)90561-u. PMID 2151199. THE structurally novel antidepressant tiflucarbine (TVX P 4495) has been demonstrated to act primarily via a serotonergic mechanism (2,3). Tiflucarbine binds both at 5-HT1 and 5-HT2 sites and displays little affinity (i.e., K i >3,000 nM) for adrenergic, dopaminergic, gaba, benzodiazepine, and other binding sites (3). In behavioral studies with rodents, tiflucarbine produces effects indicative of 5-HT1 agonism (such as forepaw treading, hindlimb abduction and flat body posture) and 5-HT2 agonism (such as head-twitch behavior) (3). Whereas its affinity for 5-HTI sites is not particularly high, tiflucarbine binds at 5-HT2 sites with an affinity (K i – 115 nM) comparable to that of the 5-HT2 agonist l-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane (DOM) (3). Taken together, the available evidence suggests that this agent may be a novel 5-HT2 agonist.
  3. ^ Schmidt BH, Glaser T, Seidel PR, Traber J (December 1990). “Evidence for a specific recognition site for tiflucarbine on calmodulin”. European Journal of Pharmacology. 189 (6): 411–418. doi:10.1016/0922-4106(90)90039-z. PMID 1963605.
  4. ^ Hegemann L, Fruchtmann R, Bonnekoh B, Schmidt BH, Traber J, Mahrle G, et al. (1991). “Effects of tiflucarbine as a dual protein kinase C/calmodulin antagonist on proliferation of human keratinocytes and release of reactive oxygen species from human leukocytes”. Archives of Dermatological Research. 283 (7): 456–460. doi:10.1007/BF00371782. PMID 1801655.
  5. ^ Glaser, T., Dompert, W. U., Horvath, E., Schuurman, T., Spencer, D. G., & Traber, J. (1987, November). Tiflucarbine, a potential new antidepressant: Biochemical and behavioral pharmacology. In Abstract P22, International Conference on the Behavioral Pharmacology of Serotonin. https://scholar.google.com/scholar?cluster=15335975313192901460