5 ht

2-Methyl-5-HT (2-Methyl-5-hydroxytryptamine) is a potent, selective 5-HT3 receptor agonist exhibiting anti-depressive-like effects.

5-HT NA Reuptake Inhibitor-1 (compound 9) is a selective dual 5-HT and NA reuptake inhibitor with IC50 values of 660 nM and 70 nM, respectively. It demonstrates good in vitro human metabolic stability, hERG selectivity, and passive membrane permeability [1].

2-Methyl-5-HT maleate (2-Methyl-5-hydroxytryptamine maleate) is a potent and selective 5-HT3 receptor agonist with demonstrated anti-depressive-like effects[1].

2-Methyl-5-HT hydrochloride (2-Methyl-5-hydroxytryptamine) is a potent and selective 5-HT3 receptor agonist, exhibiting anti-depressive-like effects.

5-HT6 7 antagonist 1 is a dual 5-HT6 7 2A and D2 receptor antagonist used in the study of dementia and Alzheimer's disease.

5HT6-ligand-1 is an orally active ligand of 5-HT6 receptor (Ki = 1.43 nM).

Serotonin hydrochloride (Serotonin HCl) is an endogenous 5-HT receptor agonist, a monoamine neurotransmitter in the CNS, and a catechol O-methyltransferase (COMT) inhibitor(Ki=44 μM).

5-HT7 agonist 1 (4-[4-[(2-chlorophenyl)methyl]piperazin-1-yl]-1H-indole) is a selective agonist of 5-HT7 (IC50 = 222.93 nM). 5-HT7 agonist 1 can be used in studies about CNS disorders.

5-HT3 antagonist 3 (Compound 15b) is a high-affinity 5-HT3 receptor antagonist that binds to 5-HT3 receptors in rat brain cortical membranes (Ki: 0.25 nM).

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

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

5-HT4 antagonist 1 is an antagonist of 5-HT4 (pKi = 9.6).

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).

Serotonin (5-hydroxytryptamine) is a natural product from animals

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-HT3 antagonist 5 is a quinoxalin-2-carboxamide compound that acts as a 5-HT3 receptor antagonist, counteracting 5-HT3 agonist and 2-methyl-5-HT, and demonstrating an anti-depressant effect in mice [1].

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].

5-HT7R antagonist 1 (free base) is a G protein-biased antagonist for the 5-HT7R receptor, with a dissociation constant (K_i) of 6.5 nM.

The compound 5-HT2CR agonist 1 (compound 8), a 7-chloro analogue, is a selective partial agonist for the 5-HT2C receptor, exhibiting an Emax of 71.09% and an EC50 of 121.5 nM, with no activity observed toward 5-HT2A or 5-HT2B receptors. It does not recruit β-arrestin and shows low hERG inhibition at 10 μM [1].

5-HT7R antagonist 1 is a G protein-biased antagonist with a Ki of 6.5 nM for 5-HT7R.

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].

Compound 4h, also known as 5-HT7R antagonist 2, is a selective inhibitor of the 5-HT7R that disrupts both G protein and β-arrestin signaling pathways. It exhibits a K_i value of 67 nM, with IC_50 values of 2.59 μM in cAMP assays and 39.57 μM in Tango tests. This antagonist is noted for its potential to mitigate repetitive behaviors associated with autism spectrum disorder (ASD) and to foster the restoration of neurogenesis impaired by ASD [1]. Pharmacokinetic analysis in ICR male mice following intravenous and intraperitoneal administration shows a T_max of 0.08 hours and 0.25 hours, a T_1 2 of 0.77 hours and 1.06 hours, and a C_max of 33.07 ng mL and 156.44 ng mL, respectively. The AUC_last was recorded at 28.31 ng·h mL and 143.27 ng·h mL, with a clearance rate (CL) of 41.61 L h kg for intravenous administration. The volume of distribution at steady state (V_ss) was 32.43 L kg, the mean residence time (MRT) was 0.79 hours and 0.93 hours, and the bioavailability (F) was calculated at 50.60% [1].

SB 206553 is a 5-HT2C inverse agonist that can attenuate methamphetamine-seeking behavior in rats. It exhibits activity for 5-HT2 receptor ligands with pKi values of 5.6 nM (5-HT2A), 7.7 nM (5-HT2B), and 7.8 nM (5-HT2C) in HEK-293 or CHO-K1 cells expressing human recombinant 5-HT2 receptors. SB 206553 can be used for research into psychostimulant abuse disorders [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-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-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].

5-HT3 antagonist 2 is an antagonist of 5-HT3 receptor.

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-HT7 agonist 2 is a highly potent 5-HT7 receptor agonist with an IC50 value of 28.7 nM, and it holds promise for studying and understanding various Central Nervous System (CNS) disorders [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].

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]

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].

5-HT3-In-1 (compound example 8) exhabits with 5-HT3 inhibition activity.

5-HT7 receptor ligand 1 (Compound 5c) is a potent 5-HT7 receptor ligand with a K i value of 8 nM, exhibiting non-hepatotoxic properties and moderate potential for drug-drug interactions with CYP3A4 or CYP2D6 substrates [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-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].

5-HT3 antagonist 1 is a potent and selective inhibitor of the 5-HT3 receptor.

5-HT2C agonist-3 ((+)-19), a selective 5-HT2C agonist (EC50: 24 nM, Ki: 78 nM), exhibits antipsychotic-like activity by blocking amphetamine-induced hyperactivity [1].

5-HT6R MAO-B modulator 1 is an antagonist of 5-HT6R (at Gs signaling) and an irreversible inhibitor of MAO-B that exhibits glial protective activity and induces scopolamine-induced memory deficits.

5-HT2C agonist-3 ((+)-19) free base is a selective 5-HT2C agonist (EC50: 24 nM, Ki: 78 nM) that exhibits antipsychotic drug-like activity and inhibits Amphetamine-induced hyperactivity [1].

BHQ-O-5HT is a serotonin form that is photoactivatable.

Compound 29 is a 5-HT6R antagonist that acts by inhibiting the 5-HT6 receptor.

Compound 8 (5-HT6R antagonist 1), a 5-HT6R antagonist (K i : 5 nM), not only demonstrates inhibition of platelet aggregation and excellent metabolic stability but also reverses MK-801-induced memory impairments in rats, suggesting its utility in Alzheimer's disease (AD) research [1].

Compound 19, a 5-HT6 agonist with an affinity (K i : 5 nM), exhibits antidepressant-like effects and enhances cognitive function while also inhibiting platelet aggregation. It demonstrates high metabolic stability [1].

5-HT2A&5-HT2C agonist-1 (Example 2) is a dual-acting agent targeting 5-HT2A and 5-HT2C receptors with IC50 values of 196 nM and 0.9 nM, respectively. It is applicable in studying central nervous system disorders, including depression, alcoholism, tobacco and cocaine addiction, inflammation, cluster headaches, post-traumatic stress disorder (PTSD), and seizure disorders [1].

5-HT7 receptor ligand 2 (compound 32) is an arylpiperazine hydrazone ligand of the 5-HT7R (Ki=178 nM). This compound exhibits high plasma protein binding, good membrane permeability, and low hepatotoxicity and cardiotoxicity. Additionally, it demonstrates neuroprotective effects in SH-SY5Y cells, making it suitable for research on central nervous system-related diseases.

Prexasertib (LY2606368) is an inhibitor of checkpoint kinase 1 (chk1) with potential antineoplastic activity.

SLV-310 is a potent dopamine D2 receptor antagonist and 5-HT reuptake receptor inhibitor used in the study of neurological disorders such as bipolar disorder and schizophrenia.