locomotor activity

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.

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.

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

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].

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

RO-5328673 is a dual NK2 NK3 antagonist. O5328673. [(3)H]RO5328673 bound to a single saturable site on hNK2, hNK3 and gpNK3 with high-affinity. RO5328673 acted as an insurmountable antagonist at both human and guinea-pig NK3 receptors in the [(3)H]IP accumulation assay. In binding kinetic analyses, [(3)H]RO5328673 had fast association and dissociation rates at hNK2 while it had a fast association rate and a remarkably slow dissociation rate at gp and hNK3. In electrophysiological recordings of gp SNpc, RO5328673 inhibited the senktide-induced potentiation of spontaneous activity of dopaminergic neurons with an insurmountable mechanism of action. RO5328673 exhibited in-vivo activity in gerbils, robustly reversing the senktide-induced locomotor activity.

Paraxanthine-d6 is intended for use as an internal standard for the quantification of paraxanthine by GC- or LC-MS. Paraxanthine is an active metabolite of caffeine. It is formed via N3-demethylation of caffeine by the cytochrome P450 (CYP) isoform CYP1A2. Paraxanthine is an adenosine A1 and A2 receptor antagonist. In vivo, paraxanthine increases striatal cGMP and extracellular striatal dopamine levels and locomotor activity, as well as inhibits motor depression induced by the adenosine A1 agonist CPA or the adenosine A2 receptor agonist CGS 21680 in rats not habituated to caffeine. It also promotes wakefulness and increases locomotor activity and core temperature in narcoleptic transgenic mice without increasing behavioral anxiety.

CTOP TFA, a potent and highly selective μ-opioid receptor antagonist, antagonizes acute analgesic effects and hypermotility, while enhancing extracellular dopamine levels in the nucleus accumbens. It also dose-dependently increases locomotor activity [1] [2].

Neuropeptide S(Mouse) TFA, an endogenous agonist for the neuropeptide S receptor (NPSR) with an EC50 value of 3 nM, plays a significant role in physiological processes by inducing the mobilization of intracellular Ca2+. This compound elevates locomotor activity and wakefulness, and simultaneously decreases anxiety-like behavior in mice.

Neuropeptide S(Rat) TFA, a robust endogenous agonist for the neuropeptide S receptor (NSPR) with an EC50 of 3.2 nM, enhances locomotor activity and promotes wakefulness while concurrently diminishing anxiety-like behavior in mice.

NocII TFA, an orphan neuropeptide, stimulates locomotor activity in mice [1].

Delta (Phospho) Sleep Inducing Peptide (DSIP-P), a peptide that promotes sustained sleep, induces changes in circadian locomotor activity in rats [1][2][3].

Adipokinetic hormone Gryllus bimaculatus (Grybi-AKH), an adipokinetic hormone, mobilizes lipids and carbohydrates from the insect fat body, regulating energy homeostasis. It also enhances the locomotor activity of the two-spotted cricket and has potential applications in human medical studies for body weight regulation, weight loss induction, and alleviation of glycogen storage disorders [1] [2] [3].