spasticity

Orphenadrine hydrochloride (Mephenamin) is a muscarinic antagonist used to treat drug-induced parkinsonism and to relieve pain from muscle spasm.

1-Hydroxyoctadecane (OctadecanolOctadecanol) is a fatty alcohol present in human and is normally incorporated into plasmalogen lipids. Sjogren-Larsson syndrome is defined by the triad of ichthyosis, mental retardation, and spasticity, and patients accumulate fatty alcohols such as Octadenol in the plasma and cultured fibroblasts.

Baclofen (Lioresal) is a synthetic chlorophenyl-butanoic acid derivative used to treat spasms due to spinal cord damage and multiple sclerosis, muscle-relaxing Baclofen acts as a gamma-aminobutyric acid (GABA) agonist specific for GABA-B receptors. It acts at spinal and supraspinal sites, reducing excitatory transmission.

Dantrolene sodium (Dantrolene sodium salt) is a skeletal muscle relaxant and can interfere with excitation-contraction coupling in the muscle fiber. It is used for the treatment of spasticity and other neuromuscular abnormalities. Its mechanism of action is may not central, but dantrolene is usually grouped with the central muscle relaxants.

Zolmitriptan (311C90) selectively binds to and activates serotonin (5-HT) 1B receptors expressed in intracranial arteries and 5-HT 1D receptors located on peripheral trigeminal sensory nerve terminals in the meninges and central terminals in brainstem sensory nuclei. Zolmitriptan is a member of the triptan class of agents with anti-migraine properties. Receptor binding results in constriction of cranial vessels, reduction of vessel pulsation and inhibition of nociceptive transmission, thereby providing relief of migraine headaches. Zolmitriptan may also relieve migraine headaches by inhibition of pro-inflammatory neuropeptide release.

Dantrolene is a postsynaptic muscle relaxant by inhibiting Ca2+ ions release from sarcoplasmic reticulum stores by antagonizing ryanodine receptors.

Mebeverine acid hydrochloride is an effective, oral compound to act directly on the smooth muscle of the gastrointestinal tract to relieve spasticity symptoms.

JB002, a myosin II inhibitor, exhibits potent activity with an IC50 of ≤10 μM. It holds potential for research applications in muscle spasticity, chronic musculoskeletal pain, and hypertrophic cardiomyopathy.

JB062 is a chemical compound acting as a nonmuscle myosin inhibitor, exhibiting IC50 values of 1.6, 5.4, and >100 μM against skeletal muscle myosin, cardiac muscle myosin, and smooth muscle myosin II, respectively. It selectively exhibits cytotoxicity towards human cancer cells without affecting normal cells. The compound is applicable in research fields concerning muscle spasticity, chronic musculoskeletal pain, and hypertrophic cardiomyopathy.

Baclofen hydrochloride (4-amino-3-(4-chlorophenyl)butanoic acid hydron chloride) is a GAMMA-AMINOBUTYRIC ACID derivative that is a specific GABA-B RECEPTORS agonist. It is used in the treatment of MUSCLE SPASTICITY, especially that due to SPINAL CORD INJURIES. Its therapeutic effects result from actions at spinal and supraspinal sites, generally the reduction of excitatory transmission.

Arbaclofen hydrochloride, a Gamma-Aminobutyric Acid derivative, is a specific agonist of GABA-B receptors, it is used to treat spasticity, especially that due to spinal cord damage. It acts at spinal and supraspinal sites, generally reduces excitatory tra

(R)-baclofen (STX209), a derivative of gamma-aminobutyric acid, is commonly utilized for the treatment of spasticity.

VSN-16, a cannabinoid receptor agonist, is used potentially for the treatment of spasticity in multiple sclerosis.

MPH-220 is a selective, orally active skeletal muscle myosin-2 inhibitor that facilitates muscle relaxation. As an anti-spastic agent, it holds potential for research into spasticity and muscle stiffness.

SAD-448 is a cannabinoid receptor type 1 (CB1) agonist. SAD-448 controls spasticity via action on the peripheral nerve CB1 receptor.

Tolperisone free base, a centrally acting muscle relaxant, has been used for the symptomatic treatment of spasticity and muscle spasm.

Orphenadrine Citrate (Flexon) is a skeletal muscle relaxant, it acts in the central nervous system to produce its muscle relaxant effects.