5-ht7

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 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-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].

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.

Compound 6.4, also known as 5-HT7R antagonist 3, is a selective antagonist of the 5-HT7R with a Ki of 8 nM. It exhibits significantly less affinity towards D2R, 5-HT1AR, and 5-HT2AR with Ki values of 511 nM, 8930 nM, and 5786 nM, respectively. In mice, 5-HT7R antagonist 3 demonstrates anti-depressant and anti-anxiety activities.

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].

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.

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

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

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.

Tiaspirone hydrochloride (BMY-13859 hydrochloride) exhibits antipsychotic activity. Tiaspirone hydrochloride influences the electrophysiological activity of dopaminergic neurons in the substantia nigra zona compacta (A9 DA cells) and ventral tegmental area (A10 DA cells) in the brain of the rat.

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.

Ziprasidone hydrochloride monohydrate (CP 88059) is a united 5-HT (serotonin) and dopamine receptor antagonist which shows potent effects of the antipsychotic activity.

Ziprasidone hydrochloride (CP-88059 hydrochloride) is a united 5-HT (serotonin) and dopamine receptor antagonist which shows potent effects of antipsychotic activity.

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

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.

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.

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.

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).

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.

(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.

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.

Ziprasidone (Geodon) is a united 5-HT (serotonin) and dopamine receptor antagonist which shows potent effects of antipsychotic activity.

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.