EZS-8, also known as 3-(2-aminoethyl)quinazoline-2,4-dione, is a very-low-

potency Potency may refer to: * Potency (pharmacology), a measure of the activity of a drug in a biological system * Virility * Cell potency, a measure of the differentiation potential of stem cells * In homeopathic dilutions, potency is a measure of ho ...

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-HT_2A receptor

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 ...

related to

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 ...

. It has about 0.15% of the potency ( = 66,000nM) and 46% of the

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 ...

() of serotonin as a serotonin 5-HT_2A receptor agonist ''

in vitro ''In vitro'' (meaning ''in glass'', or ''in the glass'') Research, studies are performed with Cell (biology), cells or biological molecules outside their normal biological context. Colloquially called "test-tube experiments", these studies in ...

''. The ''N''-(2-methoxy)benzyl analogue of EZS-8,

RH-34 RH-34 is a compound which acts as a potent and selective partial agonist for the 5-HT2A receptor, 5-HT2A serotonin Receptor (biochemistry), receptor subtype. It was derived by structural modification of the selective 5-HT2A Antagonist (pharmac ...

, has 250-fold greater potency as a serotonin 5-HT_2A receptor agonist in comparison. EZS-8 was first described in the

scientific literature Scientific literature encompasses a vast body of academic papers that spans various disciplines within the natural and social sciences. It primarily consists of academic papers that present original empirical research and theoretical ...

by 1999. ''N''-Benzyl

derivative In mathematics, the derivative is a fundamental tool that quantifies the sensitivity to change of a function's output with respect to its input. The derivative of a function of a single variable at a chosen input value, when it exists, is t ...

s of EZS-8 like RH-34 had been described as early as 1996 or 1998.

References

External links

EZS-8 - Isomer Design
{{Serotonin receptor modulators 5-HT2A agonists Amines Ethyl compounds Ketones Quinazolinones