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

Rauwolscine hydrochloride (Isoyohimbine hydrochloride) , a natural alkaloid, is a specific and reversible α2-adrenergic receptor antagonist (Ki: 12 nM) [1]. It is a stereoisomer of yohimbine, which potently antagonizes both α1- and α2-adrenergic receptors [1]. Rauwolscine hydrochloride also acts as a receptor antagonist at the serotonin 5-HT2B receptor (Ki: 14.3 nM) and as a weak partial agonist at 5-HT1A (IC50: 1.3 μM) [3]. The α2-adrenergic receptor has diverse physiological functions and antagonists like rauwolscine have numerous applications, including the modulation of mood and behavior [5].

Aripiprazole (OPC-14597) is an antipsychotic agent that is structurally related to piperazines and quinolones. It is a partial agonist of SEROTONIN RECEPTOR, 5-HT1A and DOPAMINE D2 RECEPTORS, where it also functions as a post-synaptic antagonist, and an antagonist of SEROTONIN RECEPTOR, 5-HT2A.

Lesopitron HCl is a 5-HT1A receptor agonist with anxiolytic effects that reverses dark avoidance behavior associated with cocaine withdrawal in mice.

Vilazodone (SB659746A) is a selective serotonin (5-HT) reuptake inhibitor (SSRI) and a 5-HT-1A receptor partial agonist, with antidepressant and anti-anxiety activities. Vilazodone inhibits the reuptake of serotonin from the synaptic cleft while stimulating the release of 5-HT into the synaptic cleft. This increases the concentration of 5-HT in the synaptic cleft and potentiates serotonergic neurotransmission in the central nervous system.

Cannabigerol is a high affinity α±2-adrenergic receptor agonist, moderate affinity 5-HT1A receptor antagonist, and low affinity CB1 receptor antagonist ; also binds to the CB2 receptor; it can relieve interocular pressure, which may be of benefit in the treatment of glaucoma.

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

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.

MM 77 dihydrochloride is an effecitve 5-HT1A receptor postsynaptic antagonist with anxiolytic-like activity.

Pimethixene (Calmixen) is a highly potent 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2 receptors antagonist(pKis of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively).

Binospirone (MDL 73005EF) is a 5-HT1A receptor agonist with anxiolytic activity used in the study of glaucoma and movement disorders associated with neurologic dysfunction.

NLX-204 hydrochloride is a potent and selective ERK1/2 phosphorylation-preferring serotonin 5 HT1A receptor agonist(pKi = 10.19).

EMD 56551 is a selective small molecule 5-HT1A receptor agonist with anxiolytic activity for the study of anxiety disorders.

Adatanserin (WY 50324) is a mixed 5-HT1A receptor partial agonist and a 5-HT2A and 5-HT2C receptor antagonist with potential neuroprotective activity for the study of coke oven and 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.

Sarizotan HCl (EMD 128130 HCl) is an hERG channel inhibitor and 5-hydroxytryptamine 5-HT1A receptor agonist with potential antidepressant effects for the study of Parkinson's Dyskinesia.

3-(2-aminopropyl)phenol hydrochloride is a phenethylamine analog used as a molecular structural unit. It is a psychoactive drug that is a partial agonist at several serotonin receptors, including 5-HT1A, 5-HT1B, and 5-HT2C, as well as an antagonist at the 5-HT2A receptor.

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.

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.

Sarizotan 2HCl is an hERG channel inhibitor and 5-hydroxytryptamine 5-HT1A receptor agonist with potential antidepressant effects for the study of Parkinsonian movement disorders.

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.

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.

Befiradol (NLX-112) is an agonist of 5-HT1A receptor.

F13714 fumarate, a selective biased agonist of the 5-HT1A receptor, exhibits antidepressant-like effects upon single administration in the mouse model of chronic mild stress[1].

OPC-14523 hydrochloride (VPI 013 hydrochloride) is an orally active and potent sigma and 5-HT1A receptor agonist with antidepressant activity for the study of neurological disorders.

5-HT1A modulator 1 displays very high affinities for the 5-HT1A, α1-adrenergic receptor, and D2 receptor (IC50s = 2 nM, 10 nM, and 40 nM).

Adoprazine (SLV313) is a potential atypical antipsychotic bearing potent D2 receptor antagonist and 5-HT1A receptor agonist properties.

OPC-14523, a 5-HT1A receptor agonist, is used potentially for the treatment of depression and neuropathic pain.

Pradigastat (LCQ-908) is an orally active, potent and selective diacylglycerol acyltransferase 1 (DGAT1) inhibitor for the treatment of constipation, which may be used in the study of obesity and diabetes.

Lisuride maleate is an agonist of Dopamine receptor and anti-Parkinson's agent. Displays high affinity for D2, D3 and D4 receptors along with 5-HT1A. Exhibits some 5-HT2B receptor antagonist properties. Decreases prolactin release; reduces inflammatory me

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).

RU 24969 (5-methoxy-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole) is a selective agonist of 5-HT1A and 5-HT1B receptors.

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.

WAY-607695 is a potential 5-HT1A receptor agonist.

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.

Naftopidil dihydrochloride (KT-611 2HCl) is a selective 5-HT1A and α1-adrenergic receptor antagonist with IC50 of 0.1 μM and 0.2 μM, respectively.

Aripiprazole D8 (OPC-14597 D8) is the deuterium-labeled Aripiprazole. Aripiprazole is a human 5-HT1A receptor partial agonist (Ki: 4.2 nM).

Niaprazine is a histamine H1-receptor antagonist with marked sedative properties. Niaprazine has antihistamine and antiserotonin activities and can be used for sleep disorder research[1][2]. Niaprazine exhibits a low affinity for the vesicular monoamine transporter and for D2, α2, β, H1 and mAch receptors. Niaprazine, particularly the (+)stereoisomer, has a higher affinity for α1 (Ki = 77 nM) and 5-HT2 (Ki = 25 nM) binding sites, but is poorly recognized by 5-HT1A and 5-HT1B binding sites[2]. Niaprazine (60 mg/kg; i.p.; once) treatment increases rat brain 5-hydroxyindole acetic acid (5-HIAA) concentrations 30 min after treatment, and reduced them at 3-8 hr after treatment. Niaprazine also produces a short-lasting depletion of rat brain noradrenaline (NA) and dopamine (DA)[3]. Animal Model: Male Sprague-Dawley rats (150-200 g)[3] [1]. D Scherman, et al. Molecular pharmacology of niaprazine. Prog Neuropsychopharmacol Biol Psychiatry. 1988;12(6):989-1001. [2]. P G Rossi, et al. Niaprazine in the treatment of autistic disorder. J Child Neurol. 1999 Aug;14(8):547-50. [3]. P E Keane, et al. The effect of niaprazine on the turnover of 5-hydroxytryptamine in the rat brain. Neuropharmacology. 1982 Feb;21(2):163-9.

Alpha-Yohimbine is a 5-HT1A receptor agonist, it is strong selective 2-adrenoceptor antagonist. Alpha-Yohimbine possess aphrodisiac effect.

Urapidil (Ebrantil), a sympatholytic antihypertensive drug, acts as a 5-HT1A receptor agonist and as an α1-adrenoceptor antagonist.

N-Methyllaurotetanine is a natural product with good affinity for the 5-HT1A receptor.

Cariprazine D6 (RGH-188 D6) is a deuterium-labeled Cariprazine. Cariprazine is an antipsychotic agent (D3 receptors, Ki: 0.085 nM; D2 receptors, Ki: 0.49 nM).

1-Dehydro-6-gingerdione is a 5-HT1A receptor partial agonist.

Pardoprunox hydrochloride (SLV-308 hydrochloride) is a novel partial dopamine D2 and D3 receptor agonist and serotonin 5-HT1A receptor agonist, D2 (pKi = 8.1) and D3 receptor (pKi = 8.6) partial agonist and 5-HT1A receptor (pKi = 8.5) full agonist.

Perospirone hydrochloride (Perospirone HCl) is an atypical antipsychotic agent for the treatment of schizophrenia. It also displays affinity towards 5HT1A receptors as a partial agonist.

Dsp-1053 is a powerful SERT (Ki=1.02 nM) inhibitor with partial 5-HT1A receptor (Ki=5.05 nM) agonizing activity.

6-Hydroxy Buspirone, an active metabolite of the anxiolytic compound buspirone, is produced via the cytochrome P450 (CYP) isoform CYP3A4. This compound exhibits affinity for the serotonin (5-HT) receptor subtype 5-HT1A, demonstrating efficacy in the rat hippocampus and dorsal raphe with half-maximal effective concentrations (EC50s) of 4 and 1 µM, respectively. Furthermore, 6-Hydroxy Buspirone acts as a potent antagonist against dopamine D2, D3, and D4 receptors with half-maximal inhibitory concentrations (IC50s) of 3.1, 4.9, and 0.85 µM, respectively, and inhibits the organic cation transporters 1 (OCT1), OCT2, and OCT3 in S2 proximal tubule cells expressing human transporters, showcasing a concentration-dependent mechanism.

β-adrenoceptor and 5-HT1A/1B receptor antagonist

AR-A 2 is a selective 5-HT1B receptor antagonist, with a high affinity to guinea pig cortex 5HT1B/1D and recombinant guinea pig 5-HT1B receptors (Ki: 0.24 and 0.47 nM) and with 10-fold lower affinity to guinea pig 5-HT1D receptor (Ki: 5 nM).

Wf-516 is a 5-HT reuptake inhibitor (Kis: 5 nM and 40 nM for 5-HT1A receptor and 5-HT2A receptor in humans, respectively), and with potent antidepressant activity.