motor function

UK-240455 is a potent and selective N-methyl-D-aspartic acid (NMDA) glycine receptor antagonist with neuroprotective effects and improvements in motor function in Parkinson's disease models, making it a potential candidate for Parkinson's disease treatment.

Golexanolone (Golexanolona) is a novel GABA-A receptor-modulating steroid antagonist that reduces peripheral inflammation and neuroinflammation and improves cognitive and motor function in rats with chronic hyperammonemia, and may be used to study hepatic encephalopathy.

Gastrin-Releasing Peptide, human(TFA) is a regulatory human peptide that elicits gastrin release and regulates gastric acid secretion and enteric motor function. The post-ganglionic fibers of the vagus nerve that innervate the G cells of the stomach release GRP, which stimulates the G cells to release gastrin.

exo-Tetrahydrocannabivarin (Compound 12) is an analog of Δ9,11-THC. It weakly binds to cannabinoid receptors (CB) with an IC50 of 1.4 μM. In mice, exo-Tetrahydrocannabivarin exhibits activity related to both motor function and analgesia.

Nrf2 activator 19 is a compound capable of crossing the blood-brain barrier and acts as an NRF2/HO-1 activator, offering potent antioxidant and neuroprotective effects. It effectively reduces brain damage and minimizes the accumulation of Reactive Oxygen Species (ROS). Additionally, Nrf2 activator 19 inhibits neuronal apoptosis, aiding in the recovery of neural function and motor skills. It has demonstrated significant potential in ischemic stroke research.

A-86929 is a potent and selective dopamine D1 receptor agonist with a pKi of 7.3. It significantly induces rotational behavior in a 6-OHDA-induced unilateral nigral lesion rat model and improves motor function in an MPTP-induced Parkinson's disease marmoset model. Furthermore, A-86929 shows potential value in reducing cocaine-induced craving behavior in rats and reversing Haloperidol-induced cognitive deficits in rhesus monkeys. The compound is useful for researching neurological disorders.

MCOPPB is a potent and selective agonist for the nociceptin receptor with a pKi of 10.07, much weaker activity at other opioid receptors. In animal studies, MCOPPB produces potent anxiolytic effects, with no inhibition of motor or memory function, and onl

SKF 81297 hydrobromide is a selective agonist of the dopamine D1-like receptor, with a high affinity for both D1 and D5 subtypes (Ki = 1.9 nM). SKF 81297 hydrochloride exhibits central activity in vivo and is widely used to study the neuromodulatory effects of the dopamine system, particularly in studies related to cognitive function and motor activity, such as Parkinson's disease.

Crisdesalazine (AAD 2004) is an inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES-1). Crisdesalazine reduces autophagosome formation, axonopathy, and motor neuron degeneration, improving motor function and increasing life span.

Rg3039 (PF-06687859) is a potent DcpS inhibitor. DcpS is a therapeutic target for spinal muscular atrophy. Spinal muscular atrophy (SMA) is caused by deletion or mutation of both copies of the SMN1 gene which produces an essential protein known as SMN. RG3039 improves motor function in SMA mice. RG3039 also showed activity to improve survival, function and motor unit pathologies in two SMA mouse models.

Urocortin II is a neuropeptide hormone and member of the corticotropin-releasing factor (CRF) family which includes mammalian CRF , urocortin , urocortin III , frog sauvagine, and piscine urotensin I.1 Mouse urocortin II shares 34 and 42% sequence homology with rat CRF and urocortin . It is expressed in mouse paraventricular, supraoptic, and arcuate nuclei of the hypothalamus, the locus coeruleus, and in motor nuclei of the brainstem and spinal ventral horn. Urocortin II selectively binds to CRF1 over CRF2 receptors (Kis = 0.66 and >100 nM, respectively) and induces cAMP production in CHO cells expressing CRF2 (EC50 = 0.14 nM). In vivo, urocortin II suppresses nighttime food intake by 35% in rats when administered intracerebroventricularly at a dose of 1 μg. Urocortin II (0.1 and 0.5 μg, i.c.v) stimulates fecal pellet output, increases distal colonic transit, and inhibits gastric emptying in mice.2References1. Reyes, T.M., Lewis, K., Perrin, M.H., et al. Urocortin II: A member of the corticotropin-releasing factor (CRF) neuropeptide family that is selectively bound by type 2 CRF receptors. Proc. Natl. Acad. Sci. U.S.A. 98(5), 2843-2848 (2001).2. Martinez, V., Wang, L., Million, M., et al. Urocortins and the regulation of gastrointestinal motor function and visceral pain. Peptides 25(10), 1733-1744 (2004). Urocortin II is a neuropeptide hormone and member of the corticotropin-releasing factor (CRF) family which includes mammalian CRF , urocortin , urocortin III , frog sauvagine, and piscine urotensin I.1 Mouse urocortin II shares 34 and 42% sequence homology with rat CRF and urocortin . It is expressed in mouse paraventricular, supraoptic, and arcuate nuclei of the hypothalamus, the locus coeruleus, and in motor nuclei of the brainstem and spinal ventral horn. Urocortin II selectively binds to CRF1 over CRF2 receptors (Kis = 0.66 and >100 nM, respectively) and induces cAMP production in CHO cells expressing CRF2 (EC50 = 0.14 nM). In vivo, urocortin II suppresses nighttime food intake by 35% in rats when administered intracerebroventricularly at a dose of 1 μg. Urocortin II (0.1 and 0.5 μg, i.c.v) stimulates fecal pellet output, increases distal colonic transit, and inhibits gastric emptying in mice.2 References1. Reyes, T.M., Lewis, K., Perrin, M.H., et al. Urocortin II: A member of the corticotropin-releasing factor (CRF) neuropeptide family that is selectively bound by type 2 CRF receptors. Proc. Natl. Acad. Sci. U.S.A. 98(5), 2843-2848 (2001).2. Martinez, V., Wang, L., Million, M., et al. Urocortins and the regulation of gastrointestinal motor function and visceral pain. Peptides 25(10), 1733-1744 (2004).

Domperidone (R33812) monomaleate is a selective, orally active dopamine-2 receptor antagonist that affects the chemoreceptor trigger zone and motor function in the stomach and small intestine, and has antiemetic and prokinetic effects. Domperidone monomaleate is an antiemetic and prokinetic agent.

PBT434 is a novel, brain-penetrant, small molecule inhibitor of α-synuclein aggregation. In transgenic animal models of Parkinson disease (A53T) and MSA (PLP-α-Syn), PBT434 reduced α-synuclein aggregation, preserved neurons and improved motor function. Glial cell inclusions were also reduced in a murine MSA model. PBT434 is thought to act by redistributing reactive iron across membranes, thereby blocking intracellular protein aggregation and oxidative stress. The affinity of PBT434 for iron is greater than that of α-synuclein but lower than that of iron trafficking proteins, e.g., ferritin.

NNZ 2591, a synthetic analogue of cyclic glycine-proline (cGP), exhibits oral activity and the ability to cross the blood-brain barrier. This compound demonstrates neuroprotective properties following ischemic brain injury and improves motor function in a rat model of Parkinson's disease. NNZ 2591 holds research potential for ischemic brain injury and Angelman syndrome [1] [2] [3].

Compound 10, an hNTS1R agonist-1, acts as a full agonist with a strong affinity for hNTS1R (K i: 6.9 nM), showing the ability to cross the blood-brain barrier (BBB). It not only enhances motor function but also improves memory in a mouse model of Parkinson's disease (PD). Additionally, this compound is an analog of Neurotensin(8-13) and demonstrates neuroprotective properties [1].

Tat-CIRP, a peptide inhibitor, impedes the protein-protein interaction between myeloid differentiation 2 (MD-2), also known as lymphocyte antigen 96 (LY96), and cold-inducible RNA binding protein (CIRP) by binding to MD-2. This disrupts the MD-2 and CIRP interaction as confirmed in co-immunoprecipitation assays. Notably, in vivo studies reveal that Tat-CIRP, at dosages of 10 and 20 mg/kg, significantly reduces infarct volume in both a mouse model of middle cerebral artery occlusion (MCAO) and a rhesus monkey model of thrombosis-induced stroke. Additionally, it improves motor function, evidenced by decreased time to manipulate and withdraw food with the affected arm in the primate model.

Gastrin-Releasing Peptide, human is a regulatory human peptide that elicits gastrin release and regulates gastric acid secretion and enteric motor function. The post-ganglionic fibers of the vagus nerve that innervate the G cells of the stomach release GRP, which stimulates the G cells to release gastrin.

Sumanirole maleate (PNU-95666E) is a D2 receptor full agonist with high selectivity (ED50 = 46 nM) that improves motor function in patients with Parkinson's disease and plays an important role in the study of restless legs syndrome.