Ro60-0175
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Ro60-0175, also known as (''S'')-5,6-difluoroindolmethylethylamine, is a
serotonin receptor agonist A serotonin receptor agonist is an agonist of one or more serotonin receptors. They activate serotonin receptors in a manner similar to that of serotonin (5-hydroxytryptamine; 5-HT), a neurotransmitter and hormone and the endogenous ligand of t ...
of the isotryptamine group developed by Hoffmann–La Roche, which has applications in scientific research. It acts as a potent and selective
agonist An agonist is a chemical that activates a Receptor (biochemistry), receptor to produce a biological response. Receptors are Cell (biology), cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an R ...
of both the
serotonin Serotonin (), also known as 5-hydroxytryptamine (5-HT), is a monoamine neurotransmitter with a wide range of functions in both the central nervous system (CNS) and also peripheral tissues. It is involved in mood, cognition, reward, learning, ...
5-HT2B and 5-HT2C
receptor Receptor may refer to: * Sensory receptor, in physiology, any neurite structure that, on receiving environmental stimuli, produces an informative nerve impulse *Receptor (biochemistry), in biochemistry, a protein molecule that receives and respond ...
subtypes, with good selectivity over the closely related serotonin 5-HT2A subtype, and little or no
affinity Affinity may refer to: Commerce, finance and law * Affinity (law), kinship by marriage * Affinity analysis, a market research and business management technique * Affinity Credit Union, a Saskatchewan-based credit union * Affinity Equity Pa ...
at other receptors. However, Ro60-0175 also activates the serotonin 5-HT2A receptor less potently than the serotonin 5-HT2B and 5-HT2C receptors. In
combination In mathematics, a combination is a selection of items from a set that has distinct members, such that the order of selection does not matter (unlike permutations). For example, given three fruits, say an apple, an orange and a pear, there are ...
with the selective serotonin 5-HT2C receptor
antagonist An antagonist is a character in a story who is presented as the main enemy or rival of the protagonist and is often depicted as a villain.SB-242084, Ro60-0175 robustly induces the
head-twitch response The head-twitch response (HTR), also sometimes known as wet dog shakes (WDS) in rats, is a rapid side-to-side head movement that occurs in mice and rats in association with serotonin 5-HT2A receptor activation. Serotonergic psychedelics like lys ...
, a behavioral proxy of psychedelic effects, in rodents. This effect is abolished by addition of the selective serotonin 5-HT2A receptor antagonist
ketanserin Ketanserin, sold under the brand name Sufrexal, is an antihypertensive agent which is used to treat arterial hypertension and vasospasm, vasospastic disorders. It is also used in scientific research as an antiserotonergic medication, agent in th ...
or volinanserin. The preceding findings suggest that Ro60-0175 may be a
serotonergic psychedelic Psychedelics are a subclass of hallucinogenic drugs whose primary effect is to trigger non-ordinary mental states (known as psychedelic experiences or "trips") and a perceived "expansion of consciousness". Also referred to as classic halluci ...
and may have
hallucinogen Hallucinogens, also known as psychedelics, entheogens, or historically as psychotomimetics, are a large and diverse class of psychoactive drugs that can produce altered states of consciousness characterized by major alterations in thought, mo ...
ic effects in humans at sufficiently high doses.


See also

*
AL-34662 AL-34662 is an indazole derivative drug that is being developed for the treatment of glaucoma. It acts as a selective serotonin 5-HT2 receptor agonist, including of the 5-HT2A, 5-HT2B, and 5-HT2C receptors (affinity () = 14.5, 8.1, and 3.0n ...
*
AL-38022A AL-38022A is an indazole derivative drug which is one of a range of similar drugs developed for scientific research and with some possible clinical applications such as in the treatment of glaucoma. It acts as a potent and selective agonist for ...
* Ro60-0213 *
VER-3323 VER-3323 is a drug which acts as a selective agonist for both the 5-HT2B receptor, 5-HT2B and 5-HT2C receptor, 5-HT2C serotonin Receptor (biochemistry), receptor subtypes, with moderate selectivity for 5-HT2C, but relatively low affinity for 5-HT ...
* YM-348


References

5-HT2A agonists 5-HT2B agonists 5-HT2C agonists Chloroarenes Drugs developed by Hoffmann-La Roche Fluoroarenes Isotryptamines Psychedelic drugs Serotonin receptor agonists {{Psychoactive-stub