antidepressant effect

AMN082 is an mGluR7 agonist with antidepressant effects. AMN082 has a neuroprotective effect on neuronal apoptosis in rats with traumatic brain injury and attenuates cocaine- and morphine-induced locomotor sensitization and cross-sensitization in mice.

Tipepidine hydrochloride is a reversible inhibitor of dopamine (DA) D2 receptor-mediated GIRK currents (IDA(GIRK)) (IC50: 7.0 μM), with antidepressant-like effect.

Hyperforin dicyclohexylammonium salt is a transient receptor canonical 6 channel activator with antidepressant effect. It modulates Ca2+ levels by activating Ca2+-conducting non-selective canonical TRPC6 channels.

Amoxapine (CL-67772) exerts its antidepressant effect by inhibiting the re-uptake of norepinephrine and, to a lesser degree, of serotonin, at adrenergic nerve endings and blocks the response of dopamine receptors to dopamine. Amoxapine is a tricyclic antidepressant of the dibenzoxazepine class. This drug is used to treat symptoms of depression and may cause tardive dyskinesia. Amoxapine also binds to alpha-adrenergic, histaminergic, and cholinergic receptors which accounts for many of the side effects seen with this agent.

RU 43044 is a selective glucocorticoid receptor antagonist that has exhibited an antidepressant-like effect.

Kaempferitrin (Lespenephryl) has antidepressant-like effect related to the serotonergic system, principally 5-HT1A. Kaempferitrin exerts cytotoxic and antitumor effects against HeLa cells. Kaempferitrin stimulates glucose-metabolizing enzymes, promotes glucose homeostasis. Kaempferitrin exerts immunostimulatory effects on immune responses mediated by splenocytes, macrophages, PBMC and NK cells. Kaempferitrin induces cytotoxic effects to include: cell cycle arrest in G1 phase and apoptosis via the intrinsic pathway in a caspase-dependent pathway.

Crocin II (Crocetin gentiobiosylglucosyl ester) has anti-inflammatory and anti-apoptotic effects against gastric ischemia-reperfusion injury in rats, the effect of crocin is mainly mediated by reducing the protein expression of iNOS and caspase-3. Crocin II can ameliorate CCl4-induced liver injury via inhibition of inflammatory cytokines, caspase3 and oxidative stress along with modulation of liver metabolizing enzymes favoring elimination of CCl4 toxic metabolite. Crocin II has antihyperlipidemic effect, may be due to the inhibition of pancreatic lipase and crocin, and its metabolite, Crocin II , can improve hyperlipidemia. Crocin has antidepressant effects by increasing CREB, BDNF and VGF levels in hippocampus.

CX 717 is a positive allosteric modulator of the AMPA receptor with antidepressant-like effects and potential use in adult attention deficit hyperactivity disorder (ADHD) research [1] [2].

HIV-1 inhibitor-47 is a compound that effectively inhibits HIV-1 by preventing the vif-dependent degradation of human APOBEC3G. It has a notable inhibition effect, with an IC50 value of 14.33 μM. Additionally, HIV-1 inhibitor-47 is involved in the synthesis of derivatives of 1-(2-pyrimidinyl)piperazine, which have the potential to exhibit antianxiety, antidepressant, and antipsychotic effects [1] [2] [3].

Tipepidine is a non-narcotic antitussive with an antidepressant-like effect. Tipepidine reversibly inhibits dopamine (DA) D2 receptor-mediated GIRK currents (IDA(GIRK) ) (IC 50 = 7.0 μM) and subsequently activates VTA dopamine neurons.

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.

1. Orientin (Luteolin-8-glucoside) may be regarded as a candidate therapeutic agent for treatment of vascular inflammatory diseases via inhibition of the HMGB1 signaling pathway. 2. Orientin protects vascular barrier integrity by inhibiting hyperpermeability, expression of CAMs, and adhesion and migration of leukocytes, thereby endorsing its usefulness as a therapy for vascular inflammatory diseases. 3. Orientin has neuroprotection effect by the intracellular mediation of caspase activity; may alleviate cognitive deficits and oxidative stress in AD mice; can exert antidepressant-like effects on CUMS mice, specifically by improving central oxidative stress, neurotransmission, and neuroplasticity.

Clorgyline (M&B 9302), an irreversible and selective MAO-A inhibitor with the advantages of oral activity and blood-brain barrier permeability, has an antidepressant effect by structurally altering the enzyme through the formation of intermediate radical cations, and reduces 1% fbs-stimulated VSMC (vascular smooth muscle cell) growth.

(Glu2)-TRH, a metabolically stable analogue of Thyrotropin-releasing hormone (TRH), acts as a negative modulator of TRH's cholinergic effect in the mouse brain, significantly reducing TRH-induced release of extracellular acetylcholine in the hippocampus. Resistant to metabolism by thyroliberinase, (Glu2)-TRH exhibits neuroprotective, antidepressant, and anticonvulsant properties in the CNS [1].

Tianeptine metabolite MC5, an active derivative of the atypical antidepressant tianeptine produced through β-oxidation, exhibits selective G protein activation in bioluminescence resonance energy transfer (BRET) assays. Utilizing HEK293T cells expressing the human μ-opioid receptor (MOR) over the human δ-opioid receptor (DOR; EC50s = 0.454 and >100 µM, respectively), it demonstrates specificity. Moreover, this metabolite reduces immobility in wild-type mice during the forced swim test at a dose of 30 mg/kg, an effect not observed in MOR knockout mice, suggesting its antidepressant-like activity is MOR-dependent.

TIP39, a neuropeptide and an agonist for the parathyroid hormone receptor type 2 (PTH2R), effectively increases cAMP levels in COS-7 cells featuring recombinant PTH2R from humans or rats (EC50s = 0.5 and 0.8 nM, respectively), as well as in F-11 cells that naturally express PTH2R (EC50 = 1.15 nM). Furthermore, TIP39 at 1 nM halts the cell cycle at the G0/G1 phase and reduces Sox9 expression, a crucial regulator of cartilage differentiation, in CFK2 rat chondrocytes. Additionally, administering 100 pmol/animal of TIP39 reduces the immobility period in the forced swim test in mice, indicating a potential antidepressant effect.

Phenelzine is an antidepressant and mania drug, which is a monoamine oxidase inhibitor. Its antidepressant effect is similar to that of niacinamide. It can reduce the degradation of catecholamines (norepinephrine, dopamine, and serotonin) in the brain and increase the content of catecholamines. , and play an antidepressant effect. It has a good effect on endogenous depression but has a poor effect on exogenous and reactive depression.

Bacopaside I is a saponin isolated from Bacopa monniera. Bacopaside I is a modulator of Aquaporin-1 channel, has neuroprotective functions, it has anti-Alzheimer's disease, it ameliorates cognitive impairment in APP/PS1 mice via immune-mediated clearance of α2-amyloid,exbibits antioxidant properties and free radical scavenging capacity and exerts antidepressant-like effect.

Tandospirone (SM-3997) is a selective and potent 5-HT1A receptor partial agonist with anxiolytic and antidepressant activity that potentiates the anticardiac fibrotic effect of valsartan in spontaneously hypertensive rats, and can be used in the study of central nervous system disorders.