locomotor

SB-334867 free base (SB334867A free base) is a selective antagonist of the orexin-1 (OX1) receptor.

CGP 3466B maleate (Omigapil maleate) is an orally bioavailable GAPDH nitrosylation inhibitor. Omigapil maleate abrogates Aβ1-42-induced tau acetylation, memory impairment, and locomotor dysfunction in mice. Omigapil maleate has the potential for the research of Alzheimer's disease. Omigapil maleate (CGP3446B maleate) is a apoptosis inhibitor. Omigapil maleate can be used for the research of congenital muscular dystrophy (CMD).

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.

Vamicamide (FK 176) is a novel anticholinergic compound. Vamicamide increases spontaneous locomotor activity in mice at 32 mg kg (p.o.) or higher and inhibits cataleptic convulsions in mice at 100 mg kg.

(S)-Vamicamide is a novel anticholinergic compound.Vamicamide increases spontaneous locomotor activity in mice at 32 mg kg or higher (p.o.) and inhibits tonic convulsions in mice at 100 mg kg.13483-86-1

Piribedil (Trivastan) is a dopamine D2 agonist, used in the treatment of Parkinson's disease.

L-Allylglycine is an amino acid derivative that reduces glutamate decarboxylase (GAD) activity by 60% when administered at a dose of 39.8 μmol g per hour ex vivo in mouse brain preparations. L-Allylglycine (1.2 mmol kg, i.p.) induces convulsions and decreases GABA concentration throughout the cerebellum, pons, medulla, striatum, cortex, and hippocampus in mice. Chronic administration (3.2 μg 0.5 μl per hour for 13 days) of L-allylglycine in rats increases locomotor activity in an open field test and impairs attention in the 5-choice serial reaction time task (5CSRTT). In vitro, L-allylglycine inhibits GAD only when used at high concentrations (1-80 mM). The more potent in vivo activity can be attributed to metabolic conversion of L-allylglycine to 2-keto-4-pentanoic acid, a more potent convulsant and GAD inhibitor.

Qingyangshengenin B (Otophylloside B) is a C-21 steroidal glycoside isolated from Qingyangshen. Qingyangshengenin B protects against Aβ toxicity, which decreases Aβ deposition by decreasing the expression of Aβ at the mRNA level. Qingyangshengenin B has antiepileptic and anti-aging effects, it can extend lifespan, increase heat stress-resistance, delay body paralysis, and increase the chemotaxis response in C. elegans models of Alzheimer's disease. Otophylloside B can suppress the seizure-like locomotor activity caused by pentylenetetrazole in zebrafish.

Fluopimomide (LH2010A), a powerful insecticide, is extensively utilized in the control of agricultural pests. It adversely affects the growth, locomotor behavior, reproduction, and lifespan of nematodes. Concurrently, it leads to increased production of reactive oxygen species (ROS), accumulation of lipids and lipofuscins, as well as a rise in malondialdehyde content. Additionally, Fluopimomide inhibits the antioxidant system of nematodes.

MS-153, identified as a compound that activates glutamate transporters, has been shown to reduce the conditioned reward effects of morphine, methamphetamine, and cocaine, without adversely affecting the acute locomotor response in mice.

RDS-127 induces biphasic dose-related changes in spontaneous locomotor activity in rats, similar to the reported effects of APO. Compared to APO, RDS-127 demonstrates a more potent stimulation of movement, with an efficacy that is tripled and lasts four times longer. In terms of selectivity, RDS-127 clearly outperforms APO, showing a preference for activating DA autoreceptors in the nigrostriatal pathway rather than postsynaptic DA receptors.

RTI-51 significantly enhances locomotor activity and holds potential as a treatment compound for cocaine use. It exhibits a highly effective, selective, and long-lasting substitution effect, which can reduce drug-seeking behavior.

(R)-AS-1 is a selective positive allosteric modulator of excitatory amino acid transporter 2 (EAAT2), with an EC50 of 11 nM. At doses of 60 and 90 mg kg, (R)-AS-1 enhances spontaneous locomotor activity in mice. It demonstrates anticonvulsant properties in mouse seizure models induced by maximal electroshock (MES), pentylenetetrazole (PTZ), or electric current stimulation (32 or 44 mA), with ED50 values of 66.3, 36.3, 15.6, and 41.6 mg kg, respectively. This compound is applicable in neurological disease research.

Compound 3i, a 5-HT2C agonist-4, acts as an agonist for the 5-HT2C receptor with an EC50 of 5.7 nM. It is capable of reducing locomotor activity in zebrafish larvae.

O-2050 is a high-affinity cannabinoid CB1 receptor antagonist with a Ki of 2.5 nM and inhibits the cannabinoid CB2 receptor with a Ki of 0.2 nM. O-2050 decreased food intake and stimulated locomotion in mice [1].

PD 117302 is a nonpeptide opioid compound. It is a selective kappa-opioid agonist. PD 117302 causes naloxone-reversible locomotor impairment and diuresis. It is an Anti-Arrhythmia Agent, an Anticonvulsants, a Cardiovascular Agent, and a Central Nervous Sy

ZCZ011 is a positive allosteric modulator of the cannabinoid CB1 receptor. ZCZ011 is brain penetrant, increased the potency of orthosteric agonists in mouse behavioral assays indicative of cannabimimetic activity, including antinociception, hypothermia, c

ZK-95962 is an agonist gamma-aminobutyric acid (GABA) receptor. ZK-95962 had selective effects on releasing exploratory locomotor activity suppressed by footshock (punished crossings). ZK-95962 had weak effects on the measures of anxiolytic activity. The

L 363572, a hexapeptide analog of MK 678, does not effect locomotor acitivity in rats.

The metallo-protein Cu/Zn-superoxide dismutase (SOD1) is a ubiquitous enzyme responsible for scavenging superoxide radicals. Mutations in SOD1, which alter its metal binding capacity and can result in protein misfolding and aggregation, have been linked to familial amyotrophic lateral sclerosis (ALS). Cu-ATSM is an orally bioavailable, blood-brain barrier permeable complex that has traditionally been used in cellular imaging experiments to selectively label hypoxic tissue via its susceptibility to reduction by oxygen-depleted mitochondria. More recently, Cu-ATSM has been reported to improve locomotor function and survival in a transgenic ALS mouse model by delivering copper specifically to cells in the spinal cords of mice producing misfolded SOD1 proteins. Copper chaperone for SOD (CCS) is presumed to utilize the copper from Cu-ATSM to prevent misfolding of the SOD1 protein.

SR9009 (Stenabolic), a REV-ERB agonist, increases the constitutive repression of genes regulated by REV-ERBα ERBβ (IC50: 670 800 nM). Through activation of REV-ERB, SR9009 can decrease circadian locomotor activity during the dark phase and alter the expression pattern of core clock genes in the hypothalami of mice. The circadian pattern of expression of an array of metabolic genes in the liver, skeletal muscle, and adipose tissue was also altered in mice exposed to SR9009, resulting in increased energy expenditure. In Diet-induced obese mice, SR9009 (100 mg kg, i.p., b.i.d., for 30 days) could decrease fat mass and markedly improve dyslipidemia and hyperglycemia.

Potent trace amine 1 (TA1) receptor agonist (EC50 values are 0.12, 35 and 17-85 nM for mouse, rat and human receptors, respectively). Increases wakefulness and reduces REM and NREM sleep duration in wild type mice. Inhibits spontaneous locomotor activity in dopamine transport (DAT) knockout mice. Espinoza et al (2018) Biochemical and functional characterization of the trace amine-associated receptor 1 (TAAR1) agonist RO5263397. Front.Pharmacol. 9 645 PMID:29977204 |Galley et al (2015) Discovery and characterization of 2-aminooxazolines as highly potent, selective, and orally active TAAR1 agonists. ACS.Med.Chem.Letts. 7 192 PMID:26985297 |Schwartz et al (2017) Trace amine-associated receptor 1 regulates wakefulness and EEG spectral composition. Neuropsychopharmacology. 42 1305 PMID:27658486

N,N-Dipropyldopamine is a dopamine receptor agonist.1,2,3 It decreases dihydrophenylalanine (DOPA) levels in the limbic forebrain and striatum of reserpinized rats (ED50s = 25 and 20 μmol/kg, respectively), as well as reduces homovanillic acid levels in rat striatum when administered at a dose of 80 μmol/kg.1 N,N-Dipropyldopamine (0.5-16 mg/kg) reduces spontaneous locomotor activity in mice, an effect that can be reversed by the antipsychotic spiroperidol.2,3

(R)-Preclamol, a dopamine (DA) agonist, exhibits both autoreceptor and postsynaptic receptor stimulatory effects. It effectively reduces the locomotor activity in mice and rats at low doses [1].