Muscle Relaxant Development
Muscle relaxants are medications which help to reduce muscle tension or spasms by acting on the nervous system. Protheragen uses modern understanding of the causes and the genetic factors of rare movement and neurologic disorders to develop tailored muscle relaxants and precision animal models which speed up preclinical drug development. We aim to fully assist you and optimize your therapeutic development workflows, providing support at every step.
Introduction to Muscle Relaxants
Muscle relaxants are a class of pharmacological agents designed to alleviate muscle spasms, hypertonia, and involuntary contractions. These drugs are broadly categorized into two groups:
- Neuromuscular blocking agents (NMBAs) are indicated chiefly for surgery to induce temporary paralysis by blocking acetylcholine (ACh) action at the neuromuscular junction (NMJ).
- Spasmolytics (centrally or peripherally acting) target the central nervous system (CNS) or skeletal muscle directly to relieve spasticity and muscle rigidity associated with chronic conditions.
Fig.1 Structure of the adult neuromuscular junction (NMJ). (Martyn J A J, et al., 2023)
Mechanisms of Action of Muscle Relaxants
Neuromuscular Blocking Agents (NMBAs)
NMBAs work at the neuromuscular junction (NMJ) either through a depolarizing or non-depolarizing mechanism. Depolarizing agents attach to nicotinic acetylcholine receptors (nAChRs) resulting in sustained muscle membrane depolarization and paralysis. Non-depolarizing agents block muscular contraction by ACh competitive inhibition.
Spasmolytics
Spasmolytic drugs relieve muscle spasm either in the central nervous system or in the peripheral skeletal muscle. For instance, centrally acting drugs like baclofen augment GABA-B receptor signaling in the spinal cord, whereas peripherally acting drugs like dantrolene inhibit calcium release from the sarcoplasmic reticulum by blocking ryanodine receptors.
Development of Muscle Relaxants
| Drug Names | Indications | Targets | Mechanism of Action | Phase |
| Baclofen | Hereditary spastic paraplegia | GABA-B receptors | GABAergic inhibition in spinal cord | Approved |
| Amifampridine | Congenital myasthenic syndromes | Potassium channels | Enhances neuromuscular transmission | Approved |
| Mexiletine | Myotonic dystrophy | Voltage-gated sodium channels | Stabilizes muscle membrane excitability | Approved |
| Tizanidine | Spastic dystonias | α2-adrenergic receptors | Reduces excitatory neurotransmission | Approved |
| Ranolazine | Myotonia (DM1) | Late sodium current | Reduces muscle hyperexcitability | Phase II |
Disclaimer: Protheragen focuses on providing preclinical research services. This table is for information exchange purposes only. This table is not a treatment plan recommendation. For guidance on treatment options, please visit a regular hospital.
Our Services
Specializing in the therapeutic development of rare motor neuron diseases and rare musculoskeletal disorders, Protheragen simultaneously conducts deep mechanistic studies and translational research to muscle relaxants. Guided by our specialized skills in disease modeling and target validation alongside our extensive preclinical research experience, we assist our partners in refining drug candidates and mitigating development challenges.
Diverse Development Platforms for Muscle Relaxants
Workflow of Muscle Relaxant Development
Target Identification & Validation
- Genetic analysis
- Transcriptomics
- Proteomics
- Functional assays
- Biomarker development
Drug Screening and Optimization
- High-throughput screening
- Structure-based design
- SAR studies
- ADME profiling
In Vitro Characterization
- Cell-based models
- Organoid models
- Patch-clamp electrophysiology
- Calcium imaging
In Vivo Efficacy Testing
- Animal models
- Disease phenotype modulation
- PD/PK
- Systemic effects evaluation
Safety Assessment
- Core Safety Pharmacology
- General Toxicology
- Electrophysiology
- Biomarker analysis
Targets of Muscle Relaxant Development
Protheragen is focused on developing novel muscle relaxants for the following molecular targets, which can be selected by customers. We target key pathways involved in muscle hyperexcitability, spasticity, and contracture through precision drug design and validated translational models, developing therapies that address both peripheral and central mechanisms of muscle dysfunction.
- Nicotinic acetylcholine receptors (nAChRs)
- Voltage-gated sodium channels
- Calcium channels
- GABA-B receptors
- Glycine receptors
- Myosin ATPase
- Troponin complex
- More
At Protheragen, we seek to create a novel approach to the development of muscle relaxants for rare movement and neurological disorders. We are uniquely positioned to make progress in this important area of therapy with our record of success, an expert multidisciplinary team, and our continued focus on innovative research. If you are interested in our services, please feel free to contact us for more details and quotation information of related services.
Reference
- Martyn J A J, Sparling J L, Bittner E A. Molecular mechanisms of muscular and non-muscular actions of neuromuscular blocking agents in critical illness: a narrative review[J]. British Journal of Anaesthesia, 2023, 130(1): 39-50.