RH-34 is a
compound which acts as a
potent and
selective partial agonist
In pharmacology, partial agonists are drugs that bind to and activate a given Receptor (biochemistry), receptor, but have only partial Intrinsic activity, efficacy at the receptor relative to a full agonist. They may also be considered Ligand (bio ...
for the
5-HT2A 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, ...
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 ...
subtype. It was derived by structural modification of the selective 5-HT
2A 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.[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 ...](_b ...<br></span></div> <div class=)
, with the 4-(p-fluorobenzoyl)piperidine
moiety
Moiety may refer to:
__NOTOC__ Anthropology
* Moiety (kinship), either of two groups into which a society is divided
** A division of society in the Iroquois societal structure in North America
** An Australian Aboriginal kinship group
** Native Ha ...
replaced by the ''N''-(2-methoxybenzyl)
pharmacophore
300px, An example of a pharmacophore model
In medicinal chemistry and molecular biology, a pharmacophore is an abstract description of molecular features that are necessary for molecular recognition of a ligand by a biological macromolecule. IUPAC ...
found in such potent 5-HT
2A agonists as
NBOMe-2C-B
25B-NBOMe, also known as NBOMe-2C-B and Cimbi-36, is a psychedelic drug of the 25-NB (NBOMe) family derived from 2C-B. It acts as a potent full agonist for the 5HT2A receptor. Duration of effects lasts about 3 to 10hours, although the parent co ...
and
NBOMe-2C-I. This alteration was found to retain 5-HT
2A 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 ...
and selectivity, but reversed activity from an antagonist to a moderate
efficacy
Efficacy is the ability to perform a task to a satisfactory or expected degree. The word comes from the same roots as '' effectiveness'', and it has often been used synonymously, although in pharmacology a distinction is now often made betwee ...
partial agonist.
Legal status
RH-34 is a controlled substance in Hungary and Brazil.
Anvisa
/ref>
See also
* EZS-8
EZS-8, also known as 3-(2-aminoethyl)quinazoline-2,4-dione, is a very-low-potency serotonin 5-HT2A receptor partial agonist related to ketanserin. It has about 0.15% of the potency ( = 66,000nM) and 46% of the efficacy () of serotonin as a serot ...
* 5-MeO-NBpBrT
* IHCH-7113
IHCH-7113 is a putative psychedelic drug which acts as an agonist at the 5-HT2A serotonin receptor. It was derived by structural simplification of the 5-HT2A receptor antagonist atypical antipsychotic drug lumateperone along with several relate ...
* 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 ...
* Efavirenz
Efavirenz (EFV), sold under the brand names Sustiva among others, is an antiretroviral medication used to treat and prevent HIV/AIDS. It is generally recommended for use with other antiretrovirals. It may be used for prevention after a needlesti ...
References
{{Serotonergics
Abandoned drugs
Secondary amines
2-Methoxyphenyl compounds
Psychedelic drugs
Pyrimidinediones
Quinazolines
Serotonin receptor agonists