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-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].

5-HT2A receptor agonist-3 represents the highest selectivity for the human 5-HT2A receptor currently identified, exhibiting a K i of 2.5 nM. It also demonstrates a remarkable 124-fold selectivity over its structurally analogous 5-HT2C receptor [1].

5-HT2A antagonist 2 is an orally active, selective 5HT2A antagonist with an IC50 of 14 nM. It exhibits good chemical, hepatocyte, and plasma stability, without significant cytotoxicity in cell lines VERO, HFL-1, L929, NIH3T3, CHO-K1 [1].

DREADD agonist 21 is a potent agonist of human muscarinic acetylcholine M3 receptors (EC50=1.7 nM).

5-HT2AR ligand 1 (Compound 2 cis) is a ligand for the 5-HT2AR with nanomolar affinity (Ki: 32 nM). It can induce the recruitment of β-arrestin2 and is applicable for research in neurological disorders.

5-HT6/5-HT2AR antagonist-1 is a potent dual antagonist for the 5-HT6 and 5-HT2A receptors, demonstrating high efficacy with K_i values of 11 nM and 39 nM, respectively [1].