5-ht2

5-HT2 antagonist 1 is a potent 5-HT2 receptor antagonist with weak α1 adrenoceptor blocking activity.

Compound 24, a 5-HT2 agonist-1, selectively activates 5-HT2A, 5-HT2B, and 5-HT2C receptors with IC50 values of 10 nM, 8.3 nM, and 1.6 nM, respectively. The free base form of this compound is utilized in research pertaining to depression, alcoholism, tobacco and cocaine addiction, inflammation, cluster headaches, PTSD, seizure disorders, and additional CNS disorders [1].

Compound 24 (5-HT2 agonist-1 free base) is a potent agonist for 5-HT2A, 5-HT2B, and 5-HT2C receptors, exhibiting IC50 values of 10 nM, 8.3 nM, and 1.6 nM, respectively. It is utilized in research pertaining to depression, alcoholism, tobacco and cocaine addiction, inflammation, cluster headache, PTSD, seizure disorders, and other central nervous system disorders. [1]

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

5-HT2B antagonist-1 is an orally active 5-HT2B receptor antagonist with an IC50 of 33.4 nM, suitable for studies of diseases characterized by 5-HT2B receptor signaling, such as hepatocellular carcinoma, cardiovascular disease, or gastrointestinal disease [1] [2].

Compound (−)-19, also known as (-)-5-HT2C agonist-3, is a selective 5-HT2C agonist exhibiting a preference for Gq signaling. It demonstrates efficiency with EC50 values for 5-HT2 receptor subtypes as follows: 5-HT2C at 103 nM, 5-HT2B at 570 nM, and 5-HT2A at 72 nM. This compound is utilized in research on antipsychotics.

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/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.

Compound 3i, a 5-HT2C agonist-4, acts as an agonist for the 5-HT2C receptor with an EC50 of 5.7 nM. It is capable of reducing locomotor activity in zebrafish larvae.

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-HT2B antagonist-2 (Compound 19c) is a 5HT2B receptor antagonist with an IC50 of 1.09 nM. It effectively downregulates the expression of fibrosis-related genes α-SMA, Timp1, Col1a1, and Col3a1, significantly reducing cellulose deposition. In a CCl4-induced liver fibrosis mouse model, it decreases the fibrotic area and inhibits the progression of fibrosis. This compound is useful for research into immune-inflammatory related diseases, particularly pulmonary fibrosis.

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-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-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-HT2C agonist-5 (Compound 3A) functions as a 5-HT2C receptor agonist with an EC50 of less than 1 nM. It is applicable in the research of neurological disorders.

5-HT2C agonist-9 (Compound 33) is a 5-HT2C receptor agonist with an EC50 of 1.4 nM for h5-HT2C. It is utilized in research related to conditions such as depression, drug addiction, alcohol dependence, PTSD, and neuropathic pain.

5-HT2C agonist-6 (Compound 13) is a tricyclic hallucinogen and a 5-HT2C agonist with an EC50 of 13.8 nM, useful for research in neurological disorders.

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.