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

5-HT7 agonist 2 is a highly potent 5-HT7 receptor agonist, exhibiting an IC50 value of 28.7 nM. This compound holds promise for studying and understanding various Central Nervous System (CNS) disorders [1].

AVN-101 is a potent 5-HT7 receptor antagonist.

Repinotan (BAY x 3702 free base) is an orally active and selective 5-HT1A receptor agonist that crosses the blood-brain barrier (BBB), has neuroprotective activity, antagonizes morphine-induced depression of ventilation in anesthetized rats, and can be used in studies of acute ischemic stroke and traumatic brain injury.

Tiospirone (BMY 13859-1 free base) is a 5-HT2 receptor antagonist and dopamine blocker that inhibits D2, 5-HT1a, 5-HT7, and sigma receptors.Tiospirone is used in the study of neurological disorders such as schizophrenia.

SB-269970 hydrochloride (SB-269970A) , a hydrochloride salt form of SB-269970, is a 5-HT7 receptor antagonist (pKi of 8.3) and exhibits >50-fold selectivity against other receptors.

Perphenazine dihydrochloride is an orally active and potent dopamine receptor and histamine-1 receptor antagonist that inhibits D2, D3, and 5-HT2A.Perphenazine dihydrochloride inhibits the proliferation of cancer cells and induces apoptosis, and has been used in studies of schizophrenia and endometrial cancer.

Lusaperidone (R107474) is a potent α2-adrenergic receptor antagonist, a potential radioligand for the α (2)-adrenergic receptor, with inhibitory effects on α2A and α2C, with Ki values of 0.13 and 0.15 nM, respectively.

SB 243213 is an orally available and selective 5-HT2C receptor antagonist.SB 243213 has anxiolytic and antidepressant activity and is used in schizophrenia and movement disorders.

SB 258719 is a selective antagonist of 5-HT7 receptor(pKi of 7.5).

Lurasidone (SM-13496) is an antagonist of both dopamine D2 and 5-HT7(IC50=1.68 and 0.495 nM, respectively).It also a partial agonist of 5-HT1A receptor(IC50 : 6.75 nM).

Lurasidone hydrochloride (Lurasidone HCl) is a thiazole derivative and atypical antipsychotic agent that functions as a dopamine D2 receptor antagonist; serotonin 5-HT2 receptor antagonist, serotonin 5-HT7 receptor antagonist, an antagonist of the adrenergic α2A and α2C receptors, as well as a partial serotonin 5-HT1A receptor agonist. It is used in the treatment of schizophrenia and bipolar disorder.

SEP-363856 is an agent of orally active and CNS active psychotropic with a unique, non-D2/5-HT2A mechanism of action, exerts its antipsychotic-like effects, has the potential to treatment of schizophrenia.

Vortioxetine (Lu AA 21004) is a serotonergic antidepressant used for major depression disorders. Vortioxetine has been associated with a low rate of minor serum aminotransferase elevations during treatment.

5-hydroxy-Nω-methyl Tryptamine is a metabolite of serotonin in humans that has also been found in plants. It is an agonist of the 5-HT receptor subtype 5-HT7 (IC50 = 23 pM in a radioligand binding assay). 5-hydroxy-Nω-methyl Tryptamine increases intracellular cyclic AMP production in HEK293 cells expressing 5-HT7 (EC50 = 22 nM). It inhibits serotonin uptake in HEK293 cells expressing human serotonin transporters (IC50 = 490 nM). Elevated levels of urinary 5-hydroxy-Nω-methyl tryptamine have been found in patients with schizophrenia, depression, and epilepsy.

Amisulpride is an antagonist of 5-HT7 receptor and dopamine D2 and D3 receptors. It modulates beta 2- arresting signaling and increases neurite outgrowth.

Rotigotine Hydrochloride (N-0924), a dopamine receptor agonist prefering for D3 receptors over D1 and D2, has effective activity of anti-Parkinsonian. Racemic rotigotine hydrochloride is about 50 times as potent as quinpirole, the gold standard D2 agonist.

ST1936 (ST 1936 oxalate) is a selective and highly potent 5-HT6 receptor agonist that inhibits human 5-HT6, 5-HT7 and 5-HT2B receptors by fully activating cloned human 5-HT6 receptors. body to stimulate cAMP, Ca2+, ERK1/2 and Fyn kinase.

AS19 is a potent, selective 5-HT7 receptor agonist (IC50: 0.83 nM; Ki: 0.6 nM). AS19 is selective for 5-HT7 over 5-HT1A, 5-HT1B, 5-HT1D, and 5-HT5A receptors (Kis: 89.7 nM, 490 nM, 6.6 nM and 98.5 nM, respectively).

Lurasidone-d8 HCl is a deuterated compound of Lurasidone HCl. Lurasidone HCl has a CAS number of 367514-88-3. Lurasidone hydrochloride is a thiazole derivative and atypical antipsychotic agent that functions as a dopamine D2 receptor antagonist; serotonin 5-HT2 receptor antagonist, serotonin 5-HT7 receptor antagonist, an antagonist of the adrenergic α2A and α2C receptors, as well as a partial serotonin 5-HT1A receptor agonist. It is used in the treatment of schizophrenia and bipolar disorder.

Vortioxetine hydrobromide (Lu AA21004 hydrobromide) is a serotonin (5-HT) modulator and stimulator (SMS), inhibits 5-HT1A/1B/3A/7 receptor and SERT (IC50: 15/33/3.7/19/1.6 nM).

5-HT2/5-HT7 receptor antagonist

Frovatriptan succinate hydrate (Frova) is effective in treating the full spectrum of migraine including the associated symptoms of nausea, vomiting, photophobia, and phonophobia. Frovatriptan succinate hydrate can also be used as in mini-prophylaxis in menstrual migraine. Frovatriptan succinate hydrate is a potent, high affinity, selective and orally active 5-HT1B, HT1D receptor agonist and a moderately potent 5-HT7 receptor agonist, with pKi values of 8.6, 8.4, and 6.7, respectively.

8-OH-Dpat (8-Hydroxy-DPAT) is a serotonin 1A-receptor agonist that is used experimentally to test the effects of serotonin.

5-HT7 antagonist

Rotigotine (N-0923) is a non-ergot dopamine receptor agonist used in the therapy of Parkinson disease and restless leg syndrome. Administered as a once-daily transdermal patch, Rotigotine has not been associated with serum enzyme elevations during treatment or with episodes of clinically apparent liver injury.

Iloperidone hydrochloride is a D(2)/5-HT(2) receptor antagonist. It is also an atypical antipsychotic for the treatment of schizophrenia symptoms.

Asenapine hydrochloride (Org 5222 hydrochloride) is a 5-hydroxytryptamine receptor, adrenergic receptor, dopamine receptor and histamine receptor antagonist with antipsychotic effects used in neurological disorders such as schizophrenia and bipolar disorder.

Asenapine Maleate (Org 5222 maleate) is a second generation (atypical) antipsychotic agent that is taken sublingually and used in the treatment of schizophrenia and manic or mixed episodes associated with bipolar 1 disorder. Asenapine is associated with a low rate of transient and mild serum aminotransferase elevations during therapy but has not been linked to instances of clinically apparent acute liver injury.

Sarizotan (EMD 128130) is an orally active compound that acts as an agonist for serotonin 5-HT 1A receptors and dopamine receptors. It has shown potent activity with IC 50 values of 6.5 nM for rat 5-HT 1A , 0.1 nM for human 5-HT 1A , 15.1 nM for rat D 2 , 17 nM for human D 2 , 6.8 nM for human D 3 , and 2.4 nM for human D 4.2 .

SEP-363856 hydrochloride (SEP-856 hydrochloride) is an agent of orally active and CNS active psychotropic with a unique, non-D2/5-HT2A mechanism of action, exerts its antipsychotic-like effects, has the potential to treatment of schizophrenia.

LP 12 hydrochloride is a selective 5-HT7 receptor agonist (Ki=0.13 nM). LP 12 hydrochloride is selective for 5-HT7 over D2, 5-HT1A, and 5-HT2A receptors (Ki values of 224 nM, 60.9 nM, and >1000 nM, respectively).

Chlorprothixene (Truxal) is a typical antipsychotic drug of the thioxanthene class, which was the first of the series to be synthesized.

5-HT7 receptor agonist

JNJ-18038683 is a 5-Hydroxytryptamine Type 7 (5-HT7) receptor antagonist, with pKis of 8.19, 8.20 for rat and human 5-HT7 in HEK293 cells, respectively.

ST1936 oxalate is a selective, nanomolar affinity agonist of 5-HT6 receptor(Ki values of 13 nM, 168 nM and 245 nM for human 5-HT6, 5-HT7 and 5-HT2B receptors, respectively).

LP 12 hydrochloride hydrate is a selective and potent agonist at the 5-HT7 receptor (Ki: 0.13 nM). LP 12 hydrochloride hydrate is more selective for the 5-HT7 than the D2 receptor (Ki: 224 nM), 5-HT1A receptor (Ki: 60.9 nM) and 5-HT2A receptor (Ki: 60.9 nM). HT2A receptors (Ki>1000 nM).

AVN-101 is a very potent 5-HT7 receptor antagonist, with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors. It is a multi-target drug candidate for the treatment of CNS disorders.

This compound is a dual 5-HT1A/5-HT7 receptor antagonist (5-HT1A Ki = 8 nM, Kb = 0.04 nM; 5-HT7 Ki = 451 nM, Kb = 460 nM) with additional inhibitory activity against PDE4B/PDE7A (PDE4B IC50 = 80.4 μM; PDE7A IC50 = 151.3 μM). Its antidepressant-like effect surpasses that of the reference agent, escitalopram.

LP-211 is a brain penetrant selective agonist for a 5-HT7 receptor (Ki: 0.58 nM), and >300-fold selectivity over the 5-HT1A receptor.

Vortioxetine D8 is a deuterium labeled Vortioxetine. Vortioxetine is an 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT inhibitor (Kis: 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively).

BRL-15572 dihydrochloride (BRL 15573 dihydrochloride) is a 5-HT1D receptor antagonist with pKi of 7.9, also shows a considerable affinity at 5-HT1A and 5-HT2B receptors, exhibiting 60-fold selectivity over 5-HT1B receptor.

ligand of the 5-HT7 receptor

Nuciferine ((-)-Nuciferine) is an alkaloid found within the plants Nymphaea caerulea and Nelumbo nucifera. It has a profile of action associated with dopamine receptor blockade.

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

Lurasidone D8 Hydrochloride is an inhibitor of Dopamine D2, 5-HT2A, 5-HT7, 5-HT1A and noradrenaline α2C, and is the deuterium labeled Lurasidone.

Brilaroxazine (RP5063) is a potent multimodal dopamine/5-HT modulator. Brilaroxazine is a partial agonist of dopamine D2, D3, and D4 receptors, 5-HT1A (Ki =1.5 nM) and 5-HT2A (Ki = 2.5 nM), and has antagonist activity 5-HT2B, and 5-HT7 receptors with Kis of 0.19 nM and 2.7 nM, respectively. Brilaroxazine can be used for research about cognitive impairments in neuropsychiatric and neurological diseases.

(S)-Amisulpride ((S) Amisulpride) (Esamisulpride) is a potent dopamine D2/D3 receptor antagonist. (S)-Amisulpride is an antagonist at the 5-HT7 receptor with a Ki of 900 nM. (S)-Amisulpride has antipsychotic and antidepressant effects.

SB-269970 is a antagonist of 5-HT7 receptor(pKi of 8.3).