Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UNIPROT:Q9UIJ5 (Rec)
 58,342 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

After opening, Na(+) channels may enter several kinetically distinct inactivated states. Whereas fast inactivation occurs by occlusion of the inner channel pore by the fast inactivation gate, the mechanistic basis of slower inactivated states is much less clear. We have recently suggested that the inner pore of the voltage-gated Na(+) channel may be involved in the process of ultra-slow inactivation (I(US)). The local anesthetic drug lidocaine is known to bind to the inner vestibule of the channel and to interact with slow inactivated states. We therefore sought to explore the effect of lidocaine binding on I(US). rNa(V) 1.4 channels carrying the mutation K1237E in the selectivity filter were driven into I(US) by long depolarizing pulses (-20 mV, 300 s). After repolarization to -120 mV, 53 +/- 5% of the channels recovered with a very slow time constant (tau(rec) = 171 +/- 19 s), typical for recovery from I(US). After exposure to 300 microM lidocaine, the fraction of channels recovering from I(US) was reduced to 13 +/- 4% (P < 0.01, n = 6). An additional mutation in the binding site of lidocaine (K1237E + F1579A) substantially reduced the effect of lidocaine on I(US), indicating that lidocaine has to bind to the inner vestibule of the channel to modulate I(US). We propose that I(US) involves a closure of the inner vestibule of the channel. Lidocaine may interfere with this pore motion by acting as a "foot in the door" in the inner vestibule.
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PMID:Lidocaine: a foot in the door of the inner vestibule prevents ultra-slow inactivation of a voltage-gated sodium channel. 1532 57

Lidocaine intrathecal anaesthesia was used to perform phallectomies in 15 hybrid Galapagos tortoises (Geochelone nigra) in a field setting as part of a conservation and ecosystem restoration project in the Galapagos Islands. The intrathecal injection was performed in the dorsal intercoccygeal region of the tail. Once the tail and hindlimbs were relaxed and the phallus was easily exteriorised, phallectomy was performed in a routine manner. All the animals recovered well from the procedure and were walking 30 to 60 minutes after surgery. No adverse effects were noted as a result of lidocaine intrathecal anaesthesia. One of the larger animals had evidence of haemorrhage from the surgical site 48 hours postoperatively. All tortoises continued to make full recoveries and were released on to the island of Pinta in May 2010.
Vet Rec 2011 Jan 22
PMID:Sterilisation of hybrid Galapagos tortoises (Geochelone nigra) for island restoration. Part 2: phallectomy of males under intrathecal anaesthesia with lidocaine. 2125 86