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Neuromuscular Blocking Activity

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Drug Discovery and Evaluation: Pharmacological Assays

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Abstract

Neuromuscular transmission is mediated by nicotinic acetylcholine receptors for which various subtypes are described (Sargent 1993; McGehee and Role 1995; Karlin and Akabas 1995; Alexander et al. 2001).

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References and Further Reading

General Considerations

  • Alexander S, Peters J, Mathie A, MacKenzie G, Smith A (2001) TiPS nomenclature supplement 2001

    Google Scholar 

  • Allmark MG, Bachinski WM (1949) A method of assay for curare using rats. J Am Pharm Assoc 38:43–45

    Article  CAS  Google Scholar 

  • Burn JH, Finney DJ, Goodwin LG (1952) Biological standardization. Chapter XX, Curare-like compounds. Oxford University Press, London/New York/Toronto, pp 345–354

    Google Scholar 

  • Collier HOJ, Hall RA, Fieller EC (1949) Use of a rotating drum in assessing the activities of paralysant, convulsant and anaesthetic drugs. Analyst 74:592–596

    Article  CAS  PubMed  Google Scholar 

  • Fatt P, Katz B (1951) An analysis of the end-plate potential recorded with an intra-cellular electrode. J Physiol 115:320–370

    Article  PubMed Central  CAS  PubMed  Google Scholar 

  • Hoppe JO (1955) Observations on the potency of neuromuscular blocking agents with particular reference to succinylcholine. Anesthesiology 16:91–124

    Article  CAS  PubMed  Google Scholar 

  • Hunter JM (1995) New neuromuscular blocking drugs. N Engl J Med 332:1691–1699

    Article  CAS  PubMed  Google Scholar 

  • Karlin A, Akabas MH (1995) Toward a structural basis for the function of nicotinic acetylcholine receptors and their cousins. Neuron 15:1231–1244

    Article  CAS  PubMed  Google Scholar 

  • Levis S, Preat S, Dauby J (1953) Étude pharmacodynamique de deux séries de curarisants de synthèse. Arch Int Pharmacodyn Ther 93:46–54

    CAS  PubMed  Google Scholar 

  • McGehee DS, Role LW (1995) Physiological diversity of nicotinic acetylcholine receptors expressed by vertebrate neurons. Annu Rev Physiol 57:521–546

    Article  CAS  PubMed  Google Scholar 

  • Prior C, Dempster J, Marshall IG (1993) Electrophysiological analysis of transmission at the skeletal neuromuscular junction. J Pharmacol Toxicol Methods 30:1–17

    Article  CAS  PubMed  Google Scholar 

  • Sargent PB (1995) The diversity of neuronal nicotinic acetylcholine receptors. Annu Rev Neurosci 16:403–443

    Article  Google Scholar 

  • Savarese JJ, Antonio RP, Ginsburg S (1975) Potential uses of short-acting nondepolarizing neuromuscular-blocking agents as predicted from animal experiments. Anesth Analg 54:669–678

    Article  CAS  PubMed  Google Scholar 

  • Skinner HG, Young DM (1947) A mouse assay for curare. J Pharmacol Exp Ther 91:144–146

    CAS  PubMed  Google Scholar 

  • Varney RF, Linegar CR, Holaday HA (1948) The rabbit ‘head-drop’ method for the biological assay of curare and its alkaloids. Fed Proc 7:261–262

    CAS  PubMed  Google Scholar 

  • Varney RF, Linegar CR, Holaday HA (1949) The assay of curare by the rabbit ‘head-drop’ method. J Pharmacol Exp Ther 97:72–83

    CAS  PubMed  Google Scholar 

  • Zaimis E, Head S (1976) Depolarizing neuromuscular blocking drugs. In: Zaimis E (ed) Neuromuscular junction. Handbook of experimental pharmacology, vol 42. Springer, Berlin/Heidelberg/New York, pp 365–419

    Chapter  Google Scholar 

Isolated Phrenic Nerve Diaphragm Preparation of the Rat

  • Beani L, Bianchi C, Ledda F (1964) The effect of tubocurarine on acetylcholine release from motor nerve terminals. J Physiol 174:172–183

    Article  PubMed Central  CAS  PubMed  Google Scholar 

  • Birmingham AT, Hussain SZ (1980) A comparison of the skeletal neuromuscular and autonomic ganglion-blocking potencies of five non-depolarizing relaxants. Br J Pharmacol 70:501–506

    Article  PubMed Central  CAS  PubMed  Google Scholar 

  • Bülbring E (1946) Observations on the isolated phrenic nerve diaphragm preparation of the rat. Br J Pharmacol 1:38–61

    Google Scholar 

  • Bülbring E, Chou TC (1947) The relative activity of prostigmine homologues and other substances as antagonists to tubocurarine. Br J Pharmacol 2:8–22

    Google Scholar 

  • Chang CC, Chuang ST, Lee CY, Weio JW (1972) Role of cardiotoxin and phospholipase A in the blockade of nerve conduction and depolarization of skeletal muscle induced by cobra venom. Br J Pharmacol 44:752–764

    Article  PubMed Central  CAS  PubMed  Google Scholar 

  • Colbert WE, Wilson BF, Williams PD (1990) The effects of temperature on the experimental reliability of the isolated rat phrenic nerve/diaphragm preparation. J Pharmacol Meth 24:53–57

    Article  CAS  Google Scholar 

  • Hoppe JO (1955) Observations on the potency of neuromuscular blocking agents with particular reference to succinylcholine. Anesthesiology 16:91–124

    Article  CAS  PubMed  Google Scholar 

  • Jenden DJ (1955) The effect of drugs upon neuromuscular transmission in the isolated guinea pig diaphragm. J Pharmacol Exp Ther 114:398–408

    CAS  PubMed  Google Scholar 

  • Jenden DJ, Kamijo K, Taylor DB (1994) The action of decamethonium on the isolated rabbit lumbrical muscle. J Pharmacol Exp Ther 111:229–240

    Google Scholar 

  • Kojima M, Takagi H (1969) Effects of some anticholinergic drugs on antidromic activity in the rat phrenic nerve-diaphragm preparation. Eur J Pharmacol 5:161–167

    Article  CAS  PubMed  Google Scholar 

  • Long JP, Chiou CY (1970) Pharmacological testing methods for drugs acting on the peripheral nervous system. J Pharm Sci 59:133–148

    Article  CAS  PubMed  Google Scholar 

  • Muarata T, Murai T, Kanai T, Ogaki Y, Sanai K, Kanda H, Sato S, Kajikawa N, Umetsu T, Matsuura H, Fukatsu Y, Isogaya M, Yamada N, Nishio S (1989) General pharmacology of beraprost sodium. 2nd communication: effects on the autonomic, cardiovascular and gastrointestinal systems, and other effects. Arzneimittelforschung 39:867–876

    Google Scholar 

  • Muir AW, Houston J, Green KL, Marshall RJ, Bowman WC, Marshall IG (1989) Effects of a new neuromuscular blocking agent (ORG 9426) in anaesthetized cats and pigs and in isolated nerve-muscle preparations. Br J Anaesth 63:400–410

    Article  CAS  PubMed  Google Scholar 

  • Randic M, Straughan DM (1964) Antidromic activity in the rat phrenic nerve-diaphragm preparation. J Physiol 173:130–148

    Article  PubMed Central  CAS  PubMed  Google Scholar 

  • Thesleff S (1958) A study on the interaction between neuromuscular blocking agents and acetylcholine at the mammalian motor end-plate. Acta Anaesthesiol Scand 2:69–79

    Article  CAS  PubMed  Google Scholar 

  • Van Riezen H (1968a) Classification of neuromuscular blocking agents in a new neuromuscular preparation of the chick in vitro. Eur J Pharmacol 5:29–36

    Article  PubMed  Google Scholar 

  • Van Riezen H (1968b) Effect of cholinergic and anticholinergic drugs on a new neuromuscular preparation of the chick. Eur J Pharmacol 5:37–48

    Article  PubMed  Google Scholar 

  • Vizi ES, Tuba Z, Maho S, Foldes FF, Nagano O, Doda M, Takagi S, Chaudhry IA, Saubermann AJ, Nagashima H (2003) A new short-acting non-depolarizing muscle relaxant (SZ1677) without cardiovascular side effects. Acta Anaesthesiol Scand 47:291–300

    Article  CAS  PubMed  Google Scholar 

  • Wessler I, Kilbinger H (1986) Release of [3H]acetylcholine from a modified rat phrenic nerve-hemidiaphragm preparation. Naunyn Schmiedebergs Arch Pharmacol 334:357–364

    Article  CAS  PubMed  Google Scholar 

  • Wessler I, Steinlein O (1987) Differential release of [3H]acetylcholine from the rat phrenic nerve-hemidiaphragm preparation by electrical nerve stimulation and by high potassium. Neuroscience 22:289–299

    Article  CAS  PubMed  Google Scholar 

  • Wessler I, Wagner G, Walczok A (1992) Suppression by cholinesterase inhibition of a Ca2+-independent efflux of [3H]acetylcholine from the neuromuscular junction of the isolated rat diaphragm. Eur J Pharmacol 221:371–376

    Article  CAS  PubMed  Google Scholar 

  • West GB (1947) Note on the biological assay of tubocurarine. Q J Pharm Pharmacol 20:518–527

    CAS  PubMed  Google Scholar 

Sciatic Nerve-Gastrocnemius Muscle Preparation in the Rabbit

  • Benz FW, Long JP (1969) Investigations on a series of heterocyclic hemicholinium-3 analogs. J Pharmacol Exp Ther 166:225–236

    CAS  PubMed  Google Scholar 

  • Bowman WC, Goldberg AAJ, Raper C (1962) A comparison between the effects of a tetanus and the effects of sympathomimetic amines on the fast- and slow-contracting mammalian muscles. Br J Pharmacol 19:464–484

    CAS  Google Scholar 

  • Bülbring E, Chou TC (1947) The relative activity of prostigmine homologues and other substances as antagonists to tubocurarine. Br J Pharmacol 2:8–22

    Google Scholar 

  • Chiou CY, Long JP (1969) Effects of α, α′-bis-(dimethylammoniumacetaldehyde diethylacetal)-p, p′-diacetylbiphenyl bromide (DMAE) on neuromuscular transmission. J Pharmacol Exp Ther 167:344–350

    CAS  PubMed  Google Scholar 

  • Durant NN, Bowman WC, Marshall IG (1977) A comparison of the neuromuscular and autonomic blocking activities of (+)-tubocurarine and its N-methyl and O, O, N-trimethyl analogues. Eur J Pharmacol 46:297–302

    Article  CAS  PubMed  Google Scholar 

  • Levis S, Preat S, Dauby J (1953) Étude pharmacodynamique de deux séries de curarisants de synthèse. Arch Int Pharmacodyn Ther 93:46–54

    CAS  PubMed  Google Scholar 

  • Long JP, Evans CT, Wong S (1967) A pharmacological evaluation of hemicholinium analogs. J Pharmacol Exp Ther 155:223–230

    CAS  PubMed  Google Scholar 

  • MacIntosh (1938) The effect of preganglionic section on acetylcholine in the ganglion. J Physiol 92:22P

    Google Scholar 

  • Paton WDM, Zaimis EJ (1948) Clinical potentialities of certain bisquarternary salts causing neuromuscular and ganglionic block. Nature 20:810

    Article  Google Scholar 

  • Paton WDM, Zaimis EJ (1951) The action of d-tubocurarine and of decamethonium on respiratory and other muscles in the cat. J Physiol 112:311–331

    Article  PubMed Central  CAS  PubMed  Google Scholar 

  • Reitzel NL, Long JP (1959) The neuromuscular properties of α,α′-dimethylamino-4,4′-biacetophenone (hemicholinium). Arch Int Pharmacodyn Ther 119:20–30

    CAS  PubMed  Google Scholar 

  • Salafsky B (1968) The effect of succinylcholine on denervated fast and slow skeletal muscle. Arch Int Pharmacodyn Ther 174:294–303

    CAS  PubMed  Google Scholar 

  • Wilson H, Long JP (1959) Effect of hemicholinium (HC-3) at various peripheral cholinergic transmitting sites. Arch Int Pharmacodyn Ther 120:343–352

    CAS  PubMed  Google Scholar 

Evaluation of Neuromuscular Blockade in Cats, Pigs, Dogs and Monkeys

  • Bowman WC, Rodger IW, Houston J, Marshall RJ, McIndewar I (1988) Structure: action relationships among some desacetoxy analogues of pancuronium and vecuronium in the anesthetized cat. Anesthesiology 69:57–62

    Article  CAS  PubMed  Google Scholar 

  • Brown KM, Dennis JS (1972) Derivative free analogs of the Levenberg-Marquardt and Gauss algorithms for non-linear least square approximation. Numer Math 18:288–297

    Google Scholar 

  • Clutton RE, Boyd C, Flora R, Payne J, McGrath CJ (1992) Autonomic and cardiovascular effects of neuromuscular blockade antagonism in the dog. Vet Surg 21:68–75

    Article  CAS  PubMed  Google Scholar 

  • Cullen LK, Jones RS, Snowdon SL (1980) Neuromuscular activity in the intact dog: techniques for recording evoked mechanical responses. Br Vet J 136:154–159

    CAS  PubMed  Google Scholar 

  • Hoppe JO (1950) A pharmacological investigation of 2,5-bis-(3-diethylaminopropylamino)benzoquinone-bis-benzylchloride (WIN 2747) A new curarimimetic drug. J Pharmacol Exp Ther 100:333–345

    CAS  PubMed  Google Scholar 

  • Hughes R (1984) Experimental and clinical evaluation of neuromuscular blocking agents. J Pharmacol Meth 12:1–27

    Article  CAS  Google Scholar 

  • Hughes R, Chapple DJ (1976a) Effects of non-depolarizing neuromuscular blocking agents on peripheral autonomic mechanisms in cats. Br J Anaesth 48:59–68

    Article  CAS  PubMed  Google Scholar 

  • Hughes R, Chapple DJ (1976b) Cardiovascular and neuromuscular effects of dimethyl tubocurarine in anaesthetized cats and rhesus monkeys. Br J Anaesth 48:847–852

    Article  CAS  PubMed  Google Scholar 

  • Hughes R, Chapple DJ (1981) The pharmacology of atracurium: a new competitive neuromuscular blocking agent. Br J Pharmacol 53:31–44

    CAS  Google Scholar 

  • Keesey JC (1988) AAEE minimonograph33: electrodiagnostic approach to defects of neuromuscular transmission. Muscle Nerve 12:613–626

    Article  Google Scholar 

  • Khuenl-Brady K, Castagnoli KP, Canfell PC, Caldwell JE, Agoston S, Miller RD (1990) The neuromuscular blocking effects and pharmacokinetics of ORG 9426 and ORG 9616 in the cat. Anesthesiology 72:669–674

    Article  CAS  PubMed  Google Scholar 

  • Marshall RJ, Muir AW, Sleigh T, Savage DS (1994) An overview of the pharmacology of rocuronmium bromide in experimental animals. Eur J Anaesthesiol 11(Suppl 9):9–15

    Google Scholar 

  • Muir AW, Houston J, Green KL, Marshall RJ, Bowman WC, Marshall IG (1989) Effects of a new neuromuscular blocking agent (ORG 9426) in anaesthetized cats and pigs and in isolated nerve-muscle preparations. Br J Anaesth 63:400–410

    Article  CAS  PubMed  Google Scholar 

  • Muir AW, Anderson K, Marshall RJ, Booij LHDJ, Crul FJ, Prior C, Bowman WC, Marshall IG (1991) The effects of a 16-N-homopyridine analogue of vecuronium in anesthetized cats, pigs, dogs and monkeys, and in isolated preparations. Acta Anaesthesiol Scand 35:85–90

    Article  CAS  PubMed  Google Scholar 

  • Ono H, Saito KI, Kondo M, Morishita SI, Kato K, Hasebe Y, Nakayama M, Kato F, Nakamura T, Satoh M, Oka JI, Goto M, Fukuda H (1990) Effects of the new centrally acting muscle relaxant 7-chloro-N,N,3-trimethylbenzo[b]furan-2-carboxamide on motor and central nervous systems in rats. Arzneimittelforschung 40:730–735

    CAS  PubMed  Google Scholar 

  • Paton WDM (1957) Histamine release by compounds of simple chemical structure. Pharmacol Rev 9:269–328

    CAS  PubMed  Google Scholar 

  • Savarese JJ (1979) The autonomic margins of safety of metocurine and d-tubocurarine in the cat. Anesthesiology 50:40–46

    Article  CAS  PubMed  Google Scholar 

  • Walts LF (1973) The “Boomerang” – a method for recording adductor pollicis tension. Can Anaesth Soc J 20:706–708

    Article  CAS  PubMed  Google Scholar 

Evaluation of Neuromuscular Blockade in Anesthetized Mice

  • Cullen LK, Jones RS, Snowdon SL (1980) Neuromuscular activity in the intact dog: techniques for recording evoked mechanical responses. Br Vet J 136:154–159

    CAS  PubMed  Google Scholar 

  • Keesey JC (1989) AAEE Minimonograph 33: electrodiagnosis approach to defects of neuromuscular transmission. Muscle Nerve 12:613–626

    Article  CAS  PubMed  Google Scholar 

  • Lefebvre HP, Cardona A, Toutain PL, Morel E, Bach JF, Vernetder-Garabedian B (1992) A simple method for the quantitative evaluation of neuromuscular blockade in mice. J Pharmacol Toxicol Methods 27:129–133

    Article  CAS  PubMed  Google Scholar 

Safety Pharmacology

  • Vogel HG (2006) Chapter I.H. Peripheral nervous system. In: Vogel HG, Hock FJ, Maas J, Mayer D (eds) Drug discovery and evaluation safety and pharmacokinetic assays. Springer, Berlin/Heidelberg/New York, pp 195–209

    Chapter  Google Scholar 

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Authors and Affiliations

  1. Neurologische Klinik, Heinrich-Heine Universität, Moorenstrasse 5, 40225, Düsseldorf, Germany

    Hans-Peter Hartung

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  1. Hans-Peter Hartung
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Correspondence to Hans-Peter Hartung .

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Editors and Affiliations

  1. CorDynamics, Dieburg, Germany

    Franz J. Hock

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Hartung, HP. (2016). Neuromuscular Blocking Activity. In: Hock, F. (eds) Drug Discovery and Evaluation: Pharmacological Assays. Springer, Cham. https://doi.org/10.1007/978-3-319-05392-9_39

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