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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Synthesis and Structure-Activity Relationships of Neuromuscular Blocking Agents

Author(s): Zoltan Tuba, Sandor Maho and E. Sylvester Vizi

Volume 9 , Issue 16 , 2002

Page: [1507 - 1536] Pages: 30

DOI: 10.2174/0929867023369466

Price: $65


The first use of neuromuscular blocking agents (muscle relaxants) in clinical practice (1942) revolutionised the practice of anaesthesia and started the modern era of surgery. Since 1942 introduction of tubocurarine (18) neuromuscular blocking agents have been used routinely to provide skeletal muscle relaxation during surgical procedures allowing access to body cavities without hindrance from voluntary or reflex muscle movement. After the introduction of tubocurarine and the depolarizing suxamethonium chloride (4) (1949) several nondepolarizing steroidal and nonsteroidal neuromuscular blocking agents with different onset time and duration of effect were introduced e.g. gallamine triethiodide (1) (1949), methocurine (2) (1949), alcuronium chloride (3) (1963), pancuronium bromide (9) (1968), vecuronium bromide (11) (1982), pipecuronium bromide (10) (1982), atracurium besylate (5) (1982), doxacurium chloride (6) (1991), mivacurium chloride (8) (1992), rocuronium bromide (12) (1994) cisatracurium besyla te (7) (1996), and rapacuronium bromide (13) (2000) (Fig. (1)). SZ-1677 (14) a steroid type nondepolarizing neuromuscular blocking agent under development (preclinical phase) (Fig. (2)). This review article deals with a comprehensive survey of the progress in chemical, pharmacological and, in some respects, of clinical studies of neuromuscular blocking agents used in the clinical practice and under development, including the synthesis, structure elucidation, pharmacological actions, structure-activity relationships studies of steroidal and nonsteroidal derivatives.

Keywords: neuromuscular blocking agents, (muscle relaxants), neuromuscular blocking drugs

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