ht1

Sumatriptan (GR 43175 free base) is an orally active and potent 5-hydroxytryptamine 1 (5-HT1) receptor agonist that crosses the blood-brain barrier and has anti-inflammatory activity with high affinity for 5-HT1D, 5-HT1B, and 5-HT1F receptors for use in acute migraines and acute myocardial infarction.

NEO 376 (SPI-376) is a selective 5-HT1 receptor, GABA receptor and dopamine receptor modulator, showing anti-psychotic actively.

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.

Rodatristat ethyl (KAR5585) is a groundbreaking, orally active, and potent inhibitor of tryptophan hydroxylase 1 (TPH1) that significantly reduces 5-hydroxytryptamine (5-HT) levels and decreases pulmonary arterial hypertension (PAH) at low concentrations.

Cinitapride Hydrogen Tartrate is a gastroprokinetic agent that acts as an antagonist of the 5-HT2 receptors and as an agonist of the 5-HT1 and 5-HT4 receptors

5-Carboxamidotryptamine maleate (5-CT maleate) is a receptor agonist with antihypertensive and glucose-raising effects.

Methiothepin maleate (Metitepine) is a 5-HT1, 5-HT6, 5-HT7 serotonin receptor antagonist, which blocks serotonin autoreceptors.

Naratriptan Hydrochloride is the hydrochloride salt form of naratriptan, a sulfonamide with selective serotonin (5-HT) 1 receptor agonistic activity and anti-migraine property. Naratriptan hydrochloride (GR-85548A hydrochloride) binds selectively and with high affinity to the 5-HT1D and 5-HT1B receptor subtypes. Activation of these 5-HT1D/B receptors located on intracranial blood vessels leads to vasoconstriction and provides relief of migraine headaches. Naratriptan hydrochloride may also exerts its effect by stimulation of 5-HT1D/1B receptors on sensory nerve endings in the trigeminal system thereby decreasing the release of pro-inflammatory neuropeptides.

Espindolol, a β-adrenoceptor antagonist, is used potentially for the treatment of cachexia related to cancer.

Nitisinone (SC0735)(SC0735) is an enzyme 4-hydroxyphenylpyruvate dioxygenase inhibitor.

Pipamperone (McN-JR 3345) binds 5-HT2A closely as receptor.

Cinitapride (Blaston) is a gastroprokinetic agent. It slows the actions of the muscles to reduce the symptoms of conditions such as acid reflux, delayed gastric emptying, and ulcer dyspepsia. Cinitapride acts as an antagonist of the 5-HT2 receptors and as an agonist of the 5-HT1 and 5-HT4 receptors.

FAUC 213 is a selective full antagonist of the dopamine D4 receptor.

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.

Naratriptan is a selective agonist of 5-HT1 receptor and is is used for the treatment of migraine headaches.

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.

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.

HT1171 is a potent and selective inhibitor of the Mycobacterium tuberculosis proteasome. It exhibits strong antitubercular activity against Mycobacterium tuberculosis H37Rv, with a MIC90 of 2 μg/mL and MIC of 4 μg/mL. At a concentration of 100 μM, HT1171 shows an inhibition rate of 53.8% against normal human liver cells (L02). HT1171 is applicable in antituberculosis drug research.

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 1 (Compound A3) displays a relatively balanced multi-target activity profile, including 5-HT1AR agonist (EC50= 34 nM), SERT reuptake inhibitor (IC50= 12 nM), NET reuptake inhibitor (IC50= 78 nM), and DAT reuptake inhibitor (IC50= 135 nM). It demonstrates significant antidepressant effects, excellent bioavailability, and low clearance, making it a promising candidate for research in the field of antidepressant drugs^.

5-HT1A agonist 1 (Compound Ex.37) is a highly selective 5-HT1A receptor agonist with an EC50 of 0.18 nM. This compound mimics serotonin binding to receptors, promoting postsynaptic membrane depolarization, inhibiting excessive neuronal excitability, and reducing the release of neurotransmitters associated with anxiety. 5-HT1A agonist 1 holds potential for research in neuropsychiatric disorders.

5-HT1AR agonist 3 (Compound 77) is a 5-HT1A receptor agonist that exhibits receptor activation activity with an EC50 of 1.3 nM. It primarily functions by activating the 5-HT1A receptor and can be utilized in research related to neuropsychiatric conditions, such as anxiety, depression, and sleep disorders.