motor

ITI-214 is a picomolar PDE1 inhibitor with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters, and ion channels, exhibits potent PDE1 inhibitory activity (Ki = 58 pM).

Branaplam (LMI 070) is a highly potent, selective and orally active small molecule SMN2 splicing modulator.

Risdiplam (RG7916) is a centrally and peripherally distributed and orally administrable small molecule SMN2 pre-mRNA splicing modifier that increases survival motor neuron (SMN) protein levels.

Piclozotan (anhydrous), a 5-HT1A receptor agonist, demonstrated significant neuroprotective activity in a transient middle cerebral artery occlusion (t-MCAO) model, ameliorating motor complications in patients with advanced Parkinson's disease.

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.

Rovatirelin (S-0373) is a newly synthesized thyrotropin-releasing hormone (TRH) analog that ameliorates cytosine arabinoside-induced motor dysfunction in a rat model of spinal cerebellar degeneration via acetylcholine and dopamine neurotransmission.

Stemazole is a novel small molecule human stem progenitor cell proliferation activator that promotes the survival of human embryonic stem cells and maintains stemness, and promotes the survival of oligodendrocyte precursor cells in vitro. Stemazole significantly increased cell survival and clone formation in a dose-dependent manner, reduced apoptosis, and promoted recovery of motor dysfunction and myelin repair. Stemazole can be used as a therapeutic agent in demyelinating disorders, promoting OPC survival in vitro and regeneration in vivo.

Ranirestat (AS-3201) is an orally active and potent aldose reductase (AR) inhibitor with neuroprotective properties that ameliorates peripheral nerve dysfunction in rats with advanced diabetic polyneuropathy.Ranirestat inhibits the inflammatory response of high glucose-exposed endothelial cells and may be useful for the study of diabetic sensory-motor polyneuropathy.

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.

Pridopidine (FR310826), a dopamine (DA) stabilizer, acts as a low affinity dopamine D2 receptor (D2R) antagonist, improves motor performance and shows neuroprotective effects in Huntington disease R6 2 mouse model.

Phenytoin (5,5-Diphenylhydantoin) is a hydantoin derivative and a non-sedative antiepileptic agent with anticonvulsant activity. It potentially acts by promoting sodium efflux from neurons in the motor cortex, reducing post-tetanic potentiation at synapses. This prevents cortical seizure foci from spreading to adjacent areas and stabilizes the threshold against hyperexcitability. Additionally, it appears to reduce muscle spindle sensitivity to stretch, causing muscle relaxation.

Deltamethrin (RU 22974), a neurotoxic pyrethroid insecticide, produces a reversible sequence of motor symptoms in rats involving hind limb rigidity and choreoathetosis.Deltamethrin is globally used in crop protection, control of malaria and other vector-borne diseases. It is easily degradable.

Pancuronium dibromide (Pavulon), a competitive AChR antagonist (IC50 = 5.5 nM), acts as a skeletal muscle relaxant. Pancuronium dibromide(Pancuronium bromide) blocking neuromuscular transmission is achieved by competing with acetylcholine for receptor sites on the motor end-plate.

Triprolidine hydrochloride monohydrate is a histamine H1 antagonist used in allergic rhinitis, asthma.

Ciliobrevin D is a AAA+ ATPase motor cytoplasmic dynein inhibitor. Ciliobrevin D inhibits Hedgehog (Hh) signaling and primary cilia formation and it also inhibits dynein-dependent microtubule gliding and ATPase activity in vitro.

Pimozide (R6238) is a diphenylbutylpiperidine derivative and a dopamine antagonist with the antipsychotic property. Pimozide selectively inhibits type 2 dopaminergic receptors in the central nervous system (CNS), thereby decreasing dopamine neurotransmission and reducing the occurrence of the motor and vocal tics and delusions of parasitosis. In addition, this agent antagonizes alpha-adrenergic and 5-HT2 receptors.

Pyridostigmine(Regonol) is an acetylcholinesterase inhibitor that can treat myasthenia gravis by increasing acetylcholine at the postsynaptic motor endplate.

MTP 131 is a mitochondria-targeted peptide antioxidant.1,2It localizes to the mitochondria and reducestert-butyl hydroperoxide-induced lipid peroxidation and apoptosis in SH-SY5Y cells when used at concentrations ranging from 0.001 to 1 nM.1MTP 131 (2 mg kg) reduces infarct volume, hemispheric swelling, and glutathione (GSH) depletion in a mouse model of acute cerebral ischemia induced by middle cerebral artery occlusion (MCAO).2It increases survival, improves motor function, and decreases degeneration of the lumbar spinal cord in a superoxide dismutase 1 mutant (SOD1G93A) transgenic mouse model of amyotrophic lateral sclerosis (ALS) when administered at a dose of 5 mg kg. MTP 131 reduces albuminuria, urinary hydrogen peroxide levels, and mesangial matrix accumulation, as well as preserves superoxide production, in adb dbmouse model of diabetic nephropathy.3 1.Zhao, K., Luo, G., Giannelli, S., et al.Mitochondria-targeted peptide prevents mitochondrial depolarization and apoptosis induced by tert-butyl hydroperoxide in neuronal cell linesBiochem. Pharmacol.70(12)1796-1806(2005) 2.Szeto, H.H.Mitochondria-targeted peptide antioxidants: Novel neuroprotective agentsAAPS J.8(3)E521-E531(2006) 3.Miyamoto, S., Zhang, G., Hall, D., et al.Restoring mitochondrial superoxide levels with elamipretide (MTP-131) protects db db mice against progression of diabetic kidney diseaseJ. Biol. Chem.295(21)7249-7260(2020)

UCM-1306 is a potent and orally active allosteric modulator (PAM) of the human dopamine D1 receptor. It increases the maximal effect of endogenous dopamine (DA) in both human and mouse D1 receptors. UCM-1306 could improve motor symptoms and address key comorbid cognitive impairment associated with long-term Parkinson's disease (PD).

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.

Eg5-IN-1 is a potent inhibitor of the kinesin family of motor proteins (Eg5) with an IC50 value of 1.97 µM for Eg5.Eg5-IN-1 can be used in cancer research.

Ca2+ channel agonist 1 is an agonist of N-type Ca2+ channel and an inhibitor of Cdk2 (EC50s: 14.23 μM and 3.34 μM) and is used as a potential treatment for motor nerve terminal dysfunction.

Myomodulin acetate is present in two identified aplysia neurons that contain myomodulin A the ARC motor neuron B16 and the abdominal neuron L10.

Etilevodopa hydrochloride (L-DOPA ethyl ester) is a prodrug of levodopa. It also has greater gastric solubility and significant brain penetration.