5-ht1

GR 113808 is a selective 5-HT4 receptor antagonist that inhibits 5-HT1B, 5-HT2A, 5-HT2C, and 5-HT3 receptors, and attenuates dopamine release.

Metergoline (Methergoline) is a dopamine agonist and serotonin antagonist. It has been used similarly to BROMOCRIPTINE as a dopamine agonist and also for migraine disorder therapy.

5-HT1A modulator 1 exhibits high affinities for the 5-HT1A, α1-adrenergic receptor, and D2 receptor (IC50s = 2 nM, 10 nM, and 40 nM).

5-HT1A modulator 2 hydrochloride, a derivative of 8-OH-DPAT, is a modulator of 5-HT1A with a Ki of 53 nM for 5-HT1A binding [1]. [1]. Naiman, N., et al. 2-(Alkylamino)tetralin derivatives: interaction with 5-HT1A serotonin binding sites. Journal of Medicinal Chemistry, 1989; 32(1), 253-256.

Compound 2o, also known as CB2R 5-HT1AR agonist 1, serves as a partial orally active agonist for the CB2 receptor (EC50 = 479.6 nM) and a full agonist for the 5-HT1A receptor (EC50 = 2.7 μM). This compound demonstrates both anti-anxiety and anti-depressive effects and has favorable pharmacokinetic properties [1].

5-HT1A antagonist 1 (compound 6f) is a potent and selective 5-HT1A receptor antagonist (Ki: 35 nM) and can be utilized in the study of central nervous system disorders.

5-HT1AR 5-HT6R ligand-1 (Compound PP13) functions as a ligand for the 5-HT receptor, demonstrating high affinity for 5-HT1AR, 5-HT6R, and 5-HT7R with Ki values of 19, 69, and 198 nM, respectively. In HEK293 cells, it inhibits cAMP production with EC50 values of 1535, 488, and 53 nM for these receptors. Additionally, 5-HT1AR 5-HT6R ligand-1 exhibits antiproliferative effects on several cancer cell lines, including 1321N1, U87MG, MCF7, and AsPC-1, with IC50 values of 9.6, 13.6, 19.3, and 14.6 μM, respectively. The compound also shows antagonistic activity towards the dopamine receptor D2R, with a Ki of 1903 nM.

5-HT1A modulator 4 (Compound 1) is a ligand for the 5-HT receptor, with Ki values of 2.18 μM for 5-HT1A and 19.7 μM for 5-HT2A.

5-HT1AR Agonist 2 (Compound 4f) is a potent agonist of the 5-HT1A receptor with a Ki value of 10.0 nM. It also binds to SERT, D2, and 5-HT6 receptors with Ki values of 2.8 nM, 23 nM, and 192 nM, respectively. Furthermore, this compound demonstrates stability in microsomes and induces hypothermia in mice.

(-)-Epigallocatechin Gallate (EGCG) is a phenolic antioxidant polyphenol flavonoid found in plants such as green and black tea, which inhibits telomerase and DNA methyltransferase, blocks the activation of EGF receptors and HER-2 receptors, inhibits cellular oxidation, and prevents free radical damage to cells.

Marimastat (BB2516) (BB-2516) is a potent, broad spectrum matrix metalloprotease (MMP) inhibitor. MMP-9 (IC50=3 nM), MMP-1 (IC50=5 nM), MMP-2 (IC50=6 nM), MMP-14 (IC50=9 nM)and MMP-7 (IC50=13 nM).

Resveratrol (SRT 501) is a polyphenolic natural product, a plant antitoxin with antioxidant and chemopreventive activities. Resveratrol has a wide range of targets including COX, SIRT, LOC, etc. Resveratrol induces autophagy and apoptosis.

Phorbol 12-myristate 13-acetate (PMA), a member of the phorbol ester group of natural products, activates PKC, SphK, and NF-κB, and induces THP1 cell differentiation.

Citronellol ((±)-β-Citronellol) is used in insect repellents and perfumes and as a mite attractant.

Trimethylamine N-oxide (TMAO) is a colorless amine oxide produced from choline, betaine, and carnitine via intestinal microbial metabolism that accumulates in tissues of marine animals and prevents the protein-damaging effects of urea.Trimethylamine N-oxide induces inflammation through activation of ROS NLRP3 inflammasomes, which can induce fibroblast differentiation and cardiac fibrosis.

Capsaicin ((E)-Capsaicin) is a natural product extracted from Capsicum annuum, and is a TRPV1 agonist (EC50=0.29 μM). Capsaicin has antitumor, anti-inflammatory, antioxidant and neuroprotective activities.

GIP (1-39) acetate is a gastric inhibitory peptide (GIP) purified from porcine intestine and stimulates insulin secretion.

AFMK (Formyl-N-acetyl-5-methoxykynurenamine) is an active metabolite of Melatonin with antioxidant and free radical scavenging activity. AFMK is a modulator of apoptosis and improves the anti-tumor effect of Gemcitabine in PANC-1 cells.

Exendin-4 (Exenatide) is a glucagon-like peptide-1 receptor (GLP-1) agonist (IC50: 3.22 nM). Exenatide is a 39 amino acid peptide. Compared to GLP-1, exenatide has a longer half-life of 2.4 hours.

Rutin (Quercetin 3-O-rutinoside), a flavonoid, has a variety of biological activities including antiallergic, anti-inflammatory, antiproliferative, and anticarcinogenic properties.

5-Aminosalicylic Acid (5-ASA) is an anti-inflammatory agent, structurally related to the SALICYLATES, which is active in INFLAMMATORY BOWEL DISEASE. It is considered to be the active moiety of SULPHASALAZINE.

Acetylcysteine (NAC) is an N-acetyl derivative of cysteine, a ROS inhibitor and mucolytic agent. Acetylcysteine induces apoptosis, can be used to reduce mucus thickness, and has anti-influenza viral activity.

Corticosterone (Kendall's compound B) is an adrenocortical steroid with salocorticoid and glucocorticoid activity that is orally active. Corticosterone is involved in the regulation of energy, immune responses, and stress responses in the body.

Balsalazide sodium hydrate (Balsalazide disodium) is an anti-inflammatory compound used in the treatment of Inflammatory Bowel Disease.Balsalazide sodium hydrate is a new 5-aminosalicylic acid (5-ASA) containing prodrug. High dose Balsalazide sodium hydrate(3.0 g twice daily) was superior in maintaining remission in patients with ulcerative colitis compared with a low dose (1.5 g twice daily) or a standard dose of mesalazine (0.5 g three times daily). All three treatments were safe and well tolerated [1]. Balsalazide sodium hydrate is approved for the treatment of mild-to-moderate active UC. It is efficacious for the induction of remission in mild to moderate UC and has a favorable safety profile, with the added advantages of greater efficacy of remission induction and rapidity of onset [2].