5 ht

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

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

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

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

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-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.

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

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

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 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].

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].

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-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].

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&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].

Clozapine N-oxide is the major metabolite of Clozapine and is blood-brain barrier permeable. Clozapine N-oxide is an agonist of DREADDs and activates the DREADD receptors hM3Dq and hM4Di. Clozapine N-oxide is also a dopamine antagonist and selective muscarinic M4 receptor agonist.

Tedatioxetine hydrobromide (Lu AA 24530 hydrobromide) is a serotonin-norepinephrine-dopamine reuptake inhibitor and an antagonist of 5-HT2A, 5-HT2C, 5-HT3, and α1A-adrenergic receptors, which can be used to treat depression and anxiety.

SPD-473 citrate (BTS 74398 citrate) is a dopamine reuptake inhibitor, a norepinephrine transporter protein (NET) inhibitor, and a 5-hydroxytryptamine reuptake inhibitor, and is used in the study of neurological disorders and endocrine and metabolic diseases.