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Ro60-0175
Chemical compound From Wikipedia, the free encyclopedia
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Ro60-0175, or Ro-600175, also known as (S)-5-fluoro-6-chloro-α-methylisotryptamine ((S)-5-F-6-Cl-isoAMT), is a serotonin 5-HT2 receptor agonist of the isotryptamine family developed by Hoffmann–La Roche, which has applications in scientific research.[1][2][3] It is the enantiopure (S)- isomer of the 5-fluoro and 6-chloro derivative of α-methylisotryptamine (isoAMT).[1]
It acts as a potent and selective agonist of both the serotonin 5-HT2B and 5-HT2C receptor subtypes, with good selectivity over the closely related serotonin 5-HT2A subtype, and little or no affinity at other receptors.[4][5] However, Ro60-0175 also activates the serotonin 5-HT2A receptor less potently than the serotonin 5-HT2B and 5-HT2C receptors.[6] Its EC50 and Emax values have been found to be 0.91–2.4 nM (79–130%) at the serotonin 5-HT2B receptor, 32–52 nM (84–88%) at the serotonin 5-HT2C receptor, and 400–447 nM (69–91%) at the serotonin 5-HT2A receptor.[1]
The drug has been found to produce hypolocomotion and sedative-like effects,[7] antidepressant-like effects,[8] anxiolytic-like effects[9] or no change in anxiety-like responses,[7][10] anti-obsessive-like effects,[10] antipsychotic-like effects,[10] appetite suppression,[11] and penile erections in rodent animal studies.[12] It fully generalizes with the preferential serotonin 5-HT2C receptor agonist meta-chlorophenylpiperazine (mCPP) in rodent drug discrimination tests, which can be blocked by the selective serotonin 5-HT2C receptor antagonist SB-242084.[13] Ro60-0175 also generalizes with the selective serotonin reuptake inhibitor (SSRI) citalopram in rodent drug discrimination tests, which can likewise be blocked by SB-242084, suggesting a major role for the serotonin 5-HT2C receptor in the interoceptive effects of SSRIs.[14] The drug has been found to inhibit dopaminergic signaling in the mesolimbic pathway.[15][16]
Ro60-0175 does not induce the head-twitch response, a behavioral proxy of psychedelic effects, when administered alone in rodents.[17][6] In addition, it suppresses the head-twitch response induced by the psychedelic drug (R)-DOI.[18][19] However, in combination with the selective serotonin 5-HT2C receptor antagonist SB-242084, Ro60-0175 robustly induces the head-twitch response.[17][6] This effect is abolished by addition of the selective serotonin 5-HT2A receptor antagonist ketanserin or volinanserin.[6] The preceding findings suggest that Ro60-0175 may be a serotonergic psychedelic and may have hallucinogenic effects in humans at sufficiently high doses or in combination with a serotonin 5-HT2C receptor antagonist.[6]
The drug was first described in the scientific literature by 1996.[8]
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