5-ht2a

5-HT2A antagonist 1 is a 5-HT2A receptor blocker that may be useful in treating gastrointestinal and circulatory disorders.

5-HT2A/5-HT2C inverse agonist 1 serves as a dual and potent inverse agonist for the 5-HT2A and 5-HT2C receptors, with hERG inhibition properties that mitigate cardiovascular risks. Demonstrating significant antipsychotic efficacy in the MK-801-induced mouse model, this compound holds potential for psychosis research.

5-HT2A receptor agonist-6 (compound 47) is a selective agonist of the 5-HT2A receptor with a pEC50 value of 6.58.

5-HT2A receptor agonist-5 (compound I-3) is a potent 5-HT2A agonist with a Ki value of 0.017 µM and exhibits antidepressant activity.

5-HT2A antagonist 3 (Formula (III)) functions as both an antagonist and an inverse agonist of the 5-HT2A receptor, exhibiting a pIC50 value of 8.7 and a pKi value of 9. It is applicable for research in neuroscience.

5-HT2A receptor agonist-7 (517) functions as a modulator of the 5-HT2A receptor, with an EC50 value of less than 100 nM.

5-HT2A receptor agonist-8 (compound 8) is a potent 5-HT2A receptor agonist with an EC50 of 0.6784 nM. It is suitable for research related to depression and bipolar disorder.

5-HT2A receptor agonist-9 is a β-arrestin-biased agonist of the 5-HT2A receptor. It may be utilized in research related to neurological conditions such as depression and psychedelia.

5-HT2A agonist 2 (Compound 5) is a 5-HT2A agonist.

5-HT2A receptor agonist-10 (Compound (R)-I-121.HCl) acts as a 5-HT2A receptor agonist with IC50 values of 2192.39 nM for h5-HT2A and 33.57 nM for h5-HT1A. It is applicable in research related to psychiatric disorders, mental illnesses, and central nervous system diseases.

5-HT2A agonist 4 (Compound 70) is a 5-HT2A agonist with an EC50 value of 0.30 nM for h5-HT2A. It can be utilized in research related to depression, substance addiction, alcoholism, post-traumatic stress disorder (PTSD), and neuropathic pain.

5-HT2A agonist 3 (Compound P-141) is a selective agonist of the 5-hydroxytryptamine 2A receptor (5-HT2A) with an EC50 value of 13.80 nM. It shows potential for use in research on mental disorders such as depression, post-traumatic stress disorder, obsessive-compulsive disorder, and other central nervous system-related conditions.

5-HT2A agonist 5 (Compound 88) is a 5-HT2A agonist with an EC50 of 0.01 nM for h5-HT2A. It can be utilized in research concerning depression, drug addiction, alcoholism, post-traumatic stress disorder (PTSD), and neuropathic pain.

5-HT2A receptor agonist-11 (Compound I-69) is a 5-HT2A receptor agonist with an EC50 of 22 nM, and is applicable in research on psychiatric disorders or central nervous system diseases.

5-HT2A agonist 7 (Compound 45) is an orally active and highly selective 5-HT2A receptor agonist with an EC50 of 12 nM. It holds potential for research in psychiatric disorders such as depression.

5-HT2A agonist 6 (compound 2-6) is a 5-HT2A receptor agonist with an EC50 of 1.7 nM. It is applicable in studies of stress-related disorders, including depression, anxiety, and post-traumatic stress disorder.

5-HT2A inverse agonist-1 is an inverse agonist of the 5-HT2A receptor with an IC50 value of 5.5 nM and negligible inhibition of hERG. This compound is applicable for research into neurological disorders, including Parkinson's disease.

5-HT2A receptor agonist-12 (compound 161-2) is a potent 5-HT2A agonist with an EC50 value of less than 100 nM for h5-HT2A.

5-HT7/5-HT2A receptor antagonist 1 is a high-affinity, orally active compound capable of crossing the blood-brain barrier, serving as a ligand for both 5-HT7 and 5-HT2A receptors with a pKi of 8.1 at each receptor. It acts as an antagonist in vitro in 5-HT2A functional assays and as an inverse agonist in 5-HT7 functional assays. This compound blocks hypothermia in rats induced by 5-Carboxamidotryptamine (5-CT) and prevents head twitches in mice caused by 2,5-Dimethoxy-4-iodoamphetamine (DOI). Additionally, it occupies 5-HT2A receptor binding sites in the frontal cortex of rat brains and is applicable in the study of neurological disorders.

5-HT2A agonist 9 (Compound I-53) is a 5-HT2A receptor agonist with an EC₅₀ of 34 nM. It is useful for research into psychiatric disorders and central nervous system conditions.

5-HT2A antagonist 4 methanesulfonate (Example 29) is an antagonist of the dopamine D2 receptor (D2 receptor) and the serotonin 5HT2A receptor (5HT2A receptor). It can be utilized in the study of central nervous system disorders.

5-HT6/5-HT2A receptor ligand-1 (compound 33) is a dual antagonist for the 5-HT6 and 5-HT2A receptors, exhibiting K i values of 2 nM and 11 nM for the respective receptors, holding promise for research in neurological and psychiatric disorders [1].

Compound 42, a 5-HT6/5-HT2A receptor ligand-2, serves as a dual antagonist for the 5-HT6 and 5-HT2A receptors with Ki values of 25 nM and 32 nM, respectively. This brain-penetrant compound exhibits pro-cognitive properties [1].

5-HT2A receptor agonist-2 is a potent compound that acts as an agonist on the serotonin 5-HT2 receptor, specifically stimulating the 5-HT 2A, 5-HT 2B, and 5-HT 2C receptors with EC50 values of 1.7 nM, 0.58 nM, and 0.50 nM, respectively [1].