Pharmacological relevance of peripheral type benzodiazepine receptors on motor nerve and skeletal muscle

• Published in: British journal of pharmacology Vol. 112; no. 1; pp. 257 - 261
• Main Authors: Chiou, L.C., Chang, C.C.
• Format: Journal Article
• Language: English
• Published: Oxford, UK Blackwell Publishing Ltd 01.05.1994; Nature Publishing
• Subjects: Animals; benzodiazepines; Benzodiazepinones - pharmacology; Biological and medical sciences; Cell receptors; Cell structures and functions; Diaphragm - drug effects; Diaphragm - innervation; Electric Stimulation; Electrophysiology; Female; Flumazenil - pharmacology; Fundamental and applied biological sciences. Psychology; GABA-A Receptor Antagonists; gamma-Aminobutyric Acid - pharmacology; In Vitro Techniques; Male; Mice; Mice, Inbred ICR; Microelectrodes; Miscellaneous; Molecular and cellular biology; Motor Endplate - drug effects; Motor Neurons - drug effects; Muscle Contraction - drug effects; Muscles - drug effects; Muscles - innervation; Neostigmine - antagonists & inhibitors; Neostigmine - pharmacology; neuromuscular transmission; Peripheral benzodiazepine receptors; Phrenic Nerve - drug effects; PK11195; Ro5–4864; Peripheral benzodiazepine receptor; Rodentia; Electrophysiology; Benzodiazepine receptor; Striated muscle; Neuromuscular transmission; Muscle contraction; In vitro; Vertebrata; Mammalia; Mouse; Motor nerve; Mechanism of action
• ISSN: 0007-1188; 1476-5381
• DOI: 10.1111/j.1476-5381.1994.tb13060.x

1 Effects of agonists and antagonists of peripheral and central benzodiazepine receptors (pBZR and cBZR) on neuromuscular transmission were studied in mouse isolated phrenic nerve‐diaphragm preparations. 2 Ro5–4864, a pBZR agonist, had no effect on the neuromuscular transmission but increased muscle contractility and antagonized the tetanic fade induced by neostigmine. 3 Ro5–4864 inhibited the regenerative tonic endplate depolarization caused by repetitive stimulation in the presence of neostigmine without affecting the amplitude and decay time of miniature and evoked single endplate potentials. 4 All the effects of Ro5–4864 were shared by PK11195, a pBZR antagonist, but not by clonazepam and flumazenil, a cBZR agonist and antagonist, respectively. 5 It is suggested that peripheral type benzodiazepine receptors modulate presynaptic function and muscle contraction.