5-ht1a

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-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 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-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-HT1A antagonist 2 (example 1) is a 5-HT1A receptor antagonist that can be used to investigate depression or attention-deficit hyperactivity disorder (ADHD).

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.

Fiduxosin is a selective and potent α1-adrenoceptor antagonist with inhibitory effects on α1a-adrenoceptor, α1b-adrenoceptor and α1d-adrenoceptor, with Ki values of 0.160 nM, 24.9 nM and 0.920 nM, respectively. Fiduxosin can be used for the treatment of benign prostatic hyperplasia.

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.

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.

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-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-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^.

Didesmethyl cariprazine, a metabolite of Cariprazine, is the major cyclic active part. Didesmethyl cariprazine has a long half-life of 1-3 weeks. Cariprazine is a potent D3 preference D3/D2 receptor partial agonist of dopamine for the treatment of schizophrenia, bipolar mania, and depression, with a high affinity for d3 and d2 receptors and a moderate affinity for 5-HT 1A receptors.

Naluzotan(PRX 00023) is a novel and potent 5-HT1A agonist with IC50 and Ki values of approximately 20 nM and 5.1 nM, respectively.Naluzotan is a potent hERG K+ channel blocker with an IC50 value of 3800 nM.Naluzotan exhibits anxiolytic activity and can be used to study depression.

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.

Lesopitron is an anxiolytic with pre- and postsynaptic 5-HT1A agonist activity and is more effective than 5-HT1A agonists in rat social interaction and marmoset anxiety models. lesopitron counteracts benzodiazepine withdrawal-induced anxiety in rodents with low acute toxicity and does not potentiate the effects of alcohol or barbiturates.

Roxindole (EMD 49980) is a selective dopamine autoreceptor and 5-HT1A dual agonist and inhibitor of 5-hydroxytryptamine (5-HT) uptake with antipsychotic and antidepressant activity.Roxindole can be used to study Parkinson's and neurodivergence.

Enciprazine (D-3112) has anxiolytic activity with high affinity for 5-HT1A receptor and ADRA1, which can be used for the treatment of anxiety disorders and can be used to study depression.

Org-13011 fumarate1 is an agonist of the 5-HT1A receptor and can be used to study neurological disorders.

Org 13011 has CNS activity and induces conditioned taste aversion by mediating 5-HT 1A receptors.

Osemozotan HCl (Osemozotan hydrochloride) is a novel and selective 5-HT1A receptor agonist that reduces methamphetamine-induced c-Fos expression in the medial prefrontal cortex and striatum.Osemozotan HCl is used in the study of mechanical abnormalities of pain and depression.

Piclozotan (anhydrous), a 5-HT1A receptor agonist, demonstrated significant neuroprotective activity in a transient middle cerebral artery occlusion (t-MCAO) model, ameliorating motor complications in patients with advanced Parkinson's disease.

Repinotan HCl (Bay-x-3702) is an orally active, selective and potent 5-HT1A receptor agonist across the blood-brain barrier and is an aminomethylbenzidine derivative.Repinotan HCl has potent neuroprotective effects and can be used in studies of ischemic stroke and traumatic brain injury.