social

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.

Venlafaxine (Wy 45030), an arylalkanolamine serotonin-norepinephrine reuptake inhibitor (SNRI), is used to treat major generalised anxiety disorder (GAD), depressive disorder (MDD), panic disorder and social phobia.

SB 242084 hydrochloride is a 5-HT2C receptor antagonist(pKi=9.0) that displays 158- and 100-fold selectivity over 5-HT2A and 5-HT2B receptors respectively.IC50 value: 9.0(pKi) [1]Target: 5-HT2C antagonistin vitro: SB 242084 had over 100-fold selectivity over a range of other 5-HT, dopamine and adrenergic receptors. In studies of 5-HT-stimulated phosphatidylinositol hydrolysis using SH-SY5Y cells stably expressing the cloned human 5-HT2C receptor, SB 242084 acted as an antagonist with a pKb of 9.3, which closely resembled its corresponding receptor binding affinity [1].in vivo: SB 242084 potently inhibited m-chlorophenylpiperazine (mCPP, 7 mgkg i.p. 20 min pre-test)-induced hypolocomotion in rats, a model of in vivo central 5-HT2C receptor function, with an ID50 of 0.11 mg kg i.p., and 2.0 mg kg p.o. SB 242084 (0.1-1 mg kg i.p.) exhibited an anxiolytic-like profile in the rat social interaction test, increasing time spent in social interaction, but having no effect on locomotion. SB 242084 (0.1-1 mg kg i.p.) also markedly increased punished responding in a rat Geller-Seifter conflict test of anxiety, but had no consistent effect on unpunished responding [1].

Irdabisant (CEP-26401) (CEP-26401) is a selective, orally active and blood-brain barrier (BBB) penetrant antagonist inverse agonist of histamine H3 receptor (H3R) (rat H3R Ki= 7.2 nM, human H3R Ki= 2.0 nM). Irdabisant exhibits relatively low inhibitory activity against hERG current (IC50= 13.8 μM). Irdabisant exhibits cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant can be used for research on schizophrenia or cognitive impairment.

U 99194 maleate (U-99194A maleate) is a D3 antagonist and increases social behaviors of isolation-induced aggressive male mice.

TCS 1105 is a GABAA benzodiazepine receptor (BZR) ligand. TCS 1105 blocks Sema3A induced axonal growth cones collapse. TCS 1105 reduces anxiety-like behavior and enhances offensive behavior and social dominance in mice.

Unifiram is a nootropic agent.1It increases acetylcholine (ACh) release in the rat cerebral cortexin vivoand induces a long-lasting increase in the amplitude of field excitatory postsynaptic potentials (fEPSPs) in the rat hippocampal CA1 region (EC50= 27 nM). It does not bind to serotonin (5-HT), dopamine, muscarinic, nicotinic, adrenergic, glutamate, histamine, opioid, or GABA receptors at 1 μM. Unifiram (0.1 mg kg) improves memory in non-memory-impaired rats in a social learning test.2It also prevents memory deficits induced by the anticholinergic agent scopolamine, nicotinic receptor antagonist mecamylamine, GABABreceptor agonist baclofen, or α2-adrenergic receptor agonist clonidine in the passive avoidance test in mice when administered at a dose of 0.01 mg kg and prevents memory deficits induced by the AMPA kainate glutamate receptor antagonist NBQX at 0.1 mg kg.1 1.Romanelli, M.N., Galeotti, N., Ghelardini, C., et al.Pharmacological characterization of DM232 (unifiram) and DM235 (sunifiram), new potent cognition enhancersCNS Drug Rev.12(1)39-52(2006) 2.Ghelardini, C., Galeotti, N., Gualtieri, F., et al.The novel nootropic compound DM232 (unifiram) ameliorates memory impairment in mice and ratsDrug Develop. Res.56(1)23-32(2002)

GPR139 agonist-2 (compound 20a), a potent GPR139 agonist with an EC50 of 24.7 nM, has demonstrated efficacy in rescuing social interaction deficits and alleviating cognitive deficits in murine schizophrenia models, indicating its potential in antischizophrenia drug research [1].

Corazonin, a highly conserved neuropeptide hormone prevalent in insects, acts as a key regulator of caste identity and behavior in social insects. It is preferentially expressed in workers and or foragers across various social insect species [1] [2].

Oxytocin free acid, also known as 9-Deamidooxytocin, is an analog of oxytocin where the glycinamide residue at position 9 has been substituted with a glycine residue. Oxytocin, a pleiotropic peptide hormone, has wide-ranging implications for general health, adaptation, development, reproduction, and social behavior.

Urocortin III, mouse TFA is a corticotropin-releasing factor (CRF)-related peptide. Urocortin III preferentially binds and activates CRF-R2. Urocortin III (Ucn3) is a known component of the behavioral stress response system. Urocortin III and CRF-R2 in th

α-Helical CRF (9-41) is a synthetic peptide antagonist that targets corticotropin-releasing factor (CRF), effectively inhibiting CRF-induced adrenocorticotropic hormone (ACTH) release both in vitro, with isolated rat anterior pituitary cells at concentrations of 0.5 to 5 µM, and in vivo, in non-anesthetized, intact rats at doses ranging from 0.02 to 0.6 µmol/kg. Moreover, it prevents stress-induced ACTH release at a dose of 0.6 µmol/kg in rats and demonstrates the ability to enhance social interaction times in a rat model addressing nicotine-induced conditioned anxiety, in addition to decreasing binge-like ethanol consumption in mice.

Sertraline Free Base is a Selective Serotonin Reuptake Inhibitor (SSRI). It can treat depression, obsessive-compulsive disorder (OCD), posttraumatic stress disorder (PTSD), premenstrual dysphoric disorder (PMDD), social anxiety disorder, and panic disorder.

5α-Androst-16-en-3-one, a mammalian pheromone present in boar saliva, plays a crucial role in facilitating social and sexual interactions by acting as a volatile chemical cue. It is utilized to prime sows in estrus for mating or artificial insemination, underscoring its significance in reproductive behavior. Additionally, this compound is detected in human sweat and urine, where it is involved in studies concerning receptor-mediated odorant detection and the genetic foundations of anosmias, thereby broadening its scope of relevance beyond the animal kingdom.

LIT-001 free base improves social interaction in a mouse model of autism. LIT-001 free base is the first nonpeptide oxytocin receptor (OT-R) agonist (EC50=55 nM; Ki=226 nM).

Trofinetide, derived from the neuroprotective tripeptide Gly-Pro-Glu (an N-terminal sequence of insulin-like growth factor-1, IGF-1), shows promise in various neuroprotective models. At a concentration of 10 nM, it mitigates cell death in primary rat embryonic striatal neurons caused by okadaic acid. Additionally, Trofinetide reduces the expression of pro-inflammatory markers (IL-1β, TNF-α, IL-6, and E-selectin) in a rat model simulating neuroinflammation from penetrating ballistic-like brain injuries. In cases of brain injury induced by middle cerebral artery occlusion (MCAO), administration of Trofinetide at 30 and 60 mg kg reduces the area of cortical and striatal infarct. Furthermore, a daily dose of 100 mg kg reverses social recognition and contextual fear conditioning deficits, diminishes the number of dendritic spines, and decreases testicular weight gain in an fmr1- - knockout mouse model of fragile X syndrome. Trofinetide formulations have been employed in treating Rett syndrome, highlighting its versatility across various neurological conditions.

SOMCL-668, a selective and potent sigma-1 receptor allosteric modulator, demonstrates positive modulation in ameliorating social deficits and cognitive impairment triggered by the selective sigma-1 agonist PRE084. Additionally, SOMCL-668 exhibits anti-seizure properties, making it useful for research in psychotic illnesses [1].

The mating and social behaviors of insects are largely orchestrated by a suite of volatile cuticular hydrocarbon pheromones. 7(Z),11(Z)-Heptacosadiene is the predominant female-specific courtship pheromone of the fruit fly D. melanogaster. At amounts above 100 ng, 7(Z),11(Z)-heptacosadiene elicits wing vibrations in male D. melanogaster flies in a dose-dependent manner.

Irdabisant hydrochloride (CEP-26401) is a selective, orally active, and blood-brain barrier penetrating histamine H3 receptor (H3R) inverse agonist, demonstrating high affinity with K*i values of 7.2 nM and 2.0 nM for rat and human H3R, respectively. Exhibiting relatively low hERG current inhibitory activity with an IC*50 of 13.8 μM, this compound has shown to enhance cognition and promote wakefulness in rat social recognition models, suggesting potential applications in schizophrenia or cognitive impairment research.

TAK-041 (NBI-1065846) is a potent and selective GPR139 agonist.

Oxytocin (Syntocinon) is a mammalian neuropituitary hormone, a pleiotropic hypothalamic peptide and ligand for the oxytocin receptor, which contributes to labor, lactation, and pro-social behavior. Oxytocin has the ability to stimulate mammary secretion of breast milk, promote contraction of uterine smooth muscle during labor, and facilitate mothering.

Ampullosporin A is a peptaibol-type polypeptide isolated from the fungus Sepedonium ampullosporum (HKI-0053), exhibiting neuromodulatory activity. It inhibits hyperactivity induced by the NMDA receptor antagonist MK-801 and ameliorates social behavior abnormalities caused by subchronic ketamine treatment. Ampullosporin A modulates glutamate receptor activity without affecting dopamine D1 and D2 receptors.

Blonanserin (AD-5423) is an atypical antipsychotic approved in Japan in January, 2008. Relative to many other antipsychotics, blonanserin has an improved tolerability profile, lacking side effects such as extrapyramidal symptoms, excessive sedation, or hypotension.

2-Methylhexacosane is a saturated hydrocarbon and an insect pheromone. It has been found in the cuticle of M. dasystomus females, but not males, contributing to the mating behavior of males, as well as in D. melanogaster females where it modulates male aggression. 2-Methylhexacosane has also been found in yellow jacket (V. vulgaris) trail extracts.