Abstract:
BACKGROUND AND OBJECTIVES:In addition to their blockade of voltage-dependent sodium channels, the action of local anesthetics at 5-hydroxytryptamine-3 (5-HT3) receptors may be clinically relevant. Because local anesthetics have different clinical properties, we have tested the hypothesis that differences in interactions at the 5-HT3 receptor may be clinically relevant by investigating the effects of 4 local anesthetics on recombinant wild-type and 4 mutant 5-HT3A receptors. METHODS:The cRNAs from human wild-type and 4 mutant 5-HT3A subunit clones were synthesized in vitro and expressed in Xenopus oocytes. Four mutant receptors were obtained by site-directed mutagenesis in the N-terminal extracellular region, which contains the agonist binding domain. Tryptophan (W) at positions 62 and 155 were replaced by tyrosine (Y) and glutamate (E) at position 101 by aspartate (D) or asparagine (N). The 2-electrode voltage clamp technique was used to measure peak currents induced by 5-HT in these receptors in the presence and absence of local anesthetics. RESULTS:All local anesthetics inhibited 5-HT-induced currents in a dose-dependent manner in the wild-type receptor. Inhibition by procaine and tetracaine were competitive whereas those of bupivacaine and lidocaine were both noncompetitive and competitive. The 4 mutants (W62Y, W155Y, E101D, E101N) could all form functional receptors. All mutant receptors exhibited a major increase (> 10-fold) in the half-maximum inhibitory concentration for procaine. The half-maximum inhibitory concentrations of tetracaine, bupivacaine, and lidocaine in mutant receptors were increased 2- to 3-fold except that of tetracaine in W62Y receptor (6-fold). CONCLUSIONS:The ester type local anesthetics, procaine and tetracaine, may act at a different site on the 5-HT(3A) receptor and with a different mechanism than the amide-type local anesthetics. Clinical differences between local anesthetics may be at least partially due to differences in interactions at the 5-HT3A receptor.
journal_name
Reg Anesth Pain Medjournal_title
Regional anesthesia and pain medicineauthors
Ueta K,Suzuki T,Sugimoto M,Uchida I,Mashimo Tdoi
10.1016/j.rapm.2007.06.391subject
Has Abstractpub_date
2007-11-01 00:00:00pages
462-70issue
6eissn
1098-7339issn
1532-8651pii
S1098-7339(07)00604-9journal_volume
32pub_type
杂志文章abstract::Perioperative outcomes research has gained widespread interest and is viewed as increasingly important among different specialties, including anesthesiology. Outcomes research studies serve to help in the adjustment of risk, allocation of resources, and formulation of hypotheses to guide future research. Pursuing high...
journal_title:Regional anesthesia and pain medicine
pub_type: 杂志文章,评审
doi:10.1097/AAP.0000000000000110
更新日期:2014-09-01 00:00:00
abstract:BACKGROUND AND OBJECTIVES:Peripheral nerve and spinal cord stimulation techniques have been used for many years. However, electrical stimulation methods rarely have been used to confirm epidural catheter placement. This study examines the practicality of this technique to confirm epidural catheter placement in obstetri...
journal_title:Regional anesthesia and pain medicine
pub_type: 临床试验,杂志文章
doi:10.1016/s1098-7339(99)90160-8
更新日期:1999-01-01 00:00:00
abstract:OBJECTIVE:This report describes the effects of ganglionic local opioid application (GLOA) in patients with chronic headache and persistent idiopathic facial pain. CASE REPORT:We present 2 patients with chronic headaches and 1 patient with persistent idiopathic facial pain who were refractory to medical treatment. Thes...
journal_title:Regional anesthesia and pain medicine
pub_type: 杂志文章
doi:10.1016/j.rapm.2006.03.011
更新日期:2006-09-01 00:00:00
abstract:BACKGROUND AND OBJECTIVES:Morphine may elicit potent antinociceptive effects by binding and activating peripheral opioid receptors. However, the results in clinical studies have varied. We examined the postoperative analgesic effects of incisional morphine in patients undergoing lumpectomies and axillary node dissectio...
journal_title:Regional anesthesia and pain medicine
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1016/s1098-7339(99)90075-5
更新日期:1999-03-01 00:00:00
abstract:BACKGROUND:Amitriptyline (AMI) is a lipophilic, tricyclic antidepressant with analgesic properties that could potentially be used for epidural (EPI) analgesia. However, no pharmacokinetic data are available for AMI in spinal spaces. The objective of this study was to evaluate the spinal disposition and intrathecal (IT)...
journal_title:Regional anesthesia and pain medicine
pub_type: 杂志文章
doi:10.1097/AAP.0000000000000322
更新日期:2015-11-01 00:00:00
abstract:BACKGROUND AND OBJECTIVES:The effect of intravenous dexamethasone on the duration of axillary plexus block performed using ropivacaine is not described. The aim of this study is to assess the effect of intravenous dexamethasone on the duration of axillary plexus block analgesia after distal upper arm surgery. METHODS:...
journal_title:Regional anesthesia and pain medicine
pub_type: 杂志文章,随机对照试验
doi:10.1136/rapm-2018-100035
更新日期:2019-03-01 00:00:00
abstract:BACKGROUND AND OBJECTIVES:Spontaneous intracranial hypotension is a postural headache syndrome unrelated to dural puncture. Due to the apparent failure of epidural blood patch to relieve headache in spontaneous intracranial hypotension, we investigated the epidemiologic features and treatment outcomes of this condition...
journal_title:Regional anesthesia and pain medicine
pub_type: 杂志文章
doi:10.1053/rapm.2001.28275
更新日期:2001-11-01 00:00:00
abstract::As anesthesiologists and acute pain medicine specialists, we will care for patients in the perioperative period who use cannabinoids for chronic pain and/or marijuana recreationally. We will have to address difficult questions from patients regarding the potential applications for cannabinoids in acute pain management...
journal_title:Regional anesthesia and pain medicine
pub_type: 杂志文章
doi:10.1136/rapm-2020-101475
更新日期:2020-07-01 00:00:00
abstract::Conventional opioids are widely used for acute pain management in the postoperative setting. However, a primary concern with conventional opioids is their therapeutic window-the range between doses that produce the desired therapeutic effect (analgesia) and doses that produce unwanted opioid-related adverse events (OR...
journal_title:Regional anesthesia and pain medicine
pub_type: 杂志文章,评审
doi:10.1136/rapm-2018-000010
更新日期:2019-01-01 00:00:00
abstract:OBJECTIVE:Although uncommon, residual effects from contrast agents used more than 2 decades ago are possible. This case report is to alert clinicians to the implications of residual oil-based ionic contrast agents in the intrathecal space. CASE REPORT:A 70-year-old female with evidence of degenerative disc disease und...
journal_title:Regional anesthesia and pain medicine
pub_type: 杂志文章
doi:10.1016/j.rapm.2005.07.193
更新日期:2006-01-01 00:00:00
abstract:BACKGROUND AND OBJECTIVES:The duration of nerve block is longer in streptozotocin (STZ)-induced diabetic rats for all local anesthetics (with and without adjuvants) compared with normal rats. Perioperative glycemic control is currently practiced to reduce adverse events in many at-risk patients, especially in diabetic ...
journal_title:Regional anesthesia and pain medicine
pub_type: 杂志文章
doi:10.1097/AAP.0b013e31826742fd
更新日期:2012-11-01 00:00:00
abstract::As the epidemics of obesity and diabetes expand, there are more patients with these disorders requiring elective surgery. For surgery on the extremities, peripheral nerve blocks have become a highly favorable anesthetic option when compared with general anesthesia. Peripheral blocks reduce respiratory and cardiac stre...
journal_title:Regional anesthesia and pain medicine
pub_type: 杂志文章,评审
doi:10.1097/AAP.0b013e3181ac9e42
更新日期:2009-09-01 00:00:00
abstract:BACKGROUND AND OBJECTIVE:The study goal was to compare the effect of epinephrine in different doses on pulmonary gas exchange in a rat model of bupivacaine-induced cardiac depression. METHODS:Twenty-four adult male Sprague-Dawley rats were divided into 4 groups (n = 6), and each group received a bupivacaine infusion (...
journal_title:Regional anesthesia and pain medicine
pub_type: 杂志文章
doi:10.1097/AAP.0000000000000541
更新日期:2017-05-01 00:00:00
abstract:BACKGROUND AND OBJECTIVES:Epidural anesthesia is a technically challenging regional anesthetic technique that can be difficult to teach to novices. Epidural simulators are now available to allow realistic training within a safe and controlled environment before attempting the procedure on patients. Potentially, this ma...
journal_title:Regional anesthesia and pain medicine
pub_type: 杂志文章,随机对照试验
doi:10.1097/AAP.0b013e3181a34345
更新日期:2009-05-01 00:00:00
abstract::The use of ultrasound to facilitate regional anesthesia is an evolving area of clinical, education, and research interests. As our community's experience grows, it has become evident that anesthesiologists performing "routine" ultrasound-guided blocks may very well be confronted with atypical or even pathologic anatom...
journal_title:Regional anesthesia and pain medicine
pub_type: 杂志文章,评审
doi:10.1097/AAP.0b013e3181ddd21f
更新日期:2010-05-01 00:00:00
abstract:BACKGROUND AND OBJECTIVES:Perioperative systemic lidocaine provides postoperative analgesia, decreases opioid consumption, and facilitates rehabilitation in abdominal surgery. We hypothesized that systemic lidocaine has analgesic effects in women undergoing day-case laparoscopic sterilization. METHODS:Eighty women wer...
journal_title:Regional anesthesia and pain medicine
pub_type: 杂志文章,随机对照试验
doi:10.1097/AAP.0000000000000398
更新日期:2016-05-01 00:00:00
abstract::This study aimed to describe the anatomical distribution of dye injected in the erector spinae plane (ESP) in a porcine living model, which could aid to reveal factors potentially relevant to the unexplained clinical effects of the ESP block. Six pigs received 0.6 mL/kg of 0.25% new methylene blue at the level of the ...
journal_title:Regional anesthesia and pain medicine
pub_type: 杂志文章
doi:10.1136/rapm-2019-100964
更新日期:2020-03-01 00:00:00
abstract:BACKGROUND AND OBJECTIVES:We present 2 case reports that illustrate that chronic intrathecal (IT) baclofen administration may be efficacious in treating patients with long-standing complex regional pain syndrome, type I (CRPS I) who have failed treatment with multiple drugs and procedures. CASE REPORTS:Both cases pres...
journal_title:Regional anesthesia and pain medicine
pub_type: 杂志文章
doi:10.1053/rapm.2002.29244
更新日期:2002-01-01 00:00:00
abstract:BACKGROUND AND OBJECTIVES:Mexiletine is an oral sodium channel antagonist that has been reported to be effective in a variety of neuropathic pain syndromes. However, recent reports question the efficacy of oral mexiletine in neuropathic pain. The objectives of this study were to examine the effect of oral mexiletine on...
journal_title:Regional anesthesia and pain medicine
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1053/rapm.2000.8583
更新日期:2000-09-01 00:00:00
abstract:BACKGROUND AND OBJECTIVES:Peripheral nerve blocks reduce postoperative pain and enhance recovery after total knee arthroplasty (TKA). This study aims to assess the benefits of addition of intravenous dexmedetomidine (DexM) to intravenous dexamethasone on the analgesic duration of quadruple nerve blocks. METHODS:This d...
journal_title:Regional anesthesia and pain medicine
pub_type: 杂志文章
doi:10.1136/rapm-2020-101749
更新日期:2021-02-01 00:00:00
abstract:BACKGROUND AND OBJECTIVES:Continuous spinal anesthesia via a spinal catheter allows adjusting the duration and extent of anesthesia to surgical needs, maintenance of hemodynamic stability, and good postoperative analgesia. This study was designed to determine the median effective local anesthetic dose of plain ropivaca...
journal_title:Regional anesthesia and pain medicine
pub_type: 杂志文章,随机对照试验
doi:10.1016/j.rapm.2007.06.396
更新日期:2008-01-01 00:00:00
abstract:BACKGROUND AND OBJECTIVES:We describe a new therapeutic modality for sacroiliac joint syndrome that represents an alternative to other treatment modalities. We report on four cases of sacroiliac joint syndrome with severe pain. METHODS:Three patients had undergone operative treatment of the lumbar spine and one patien...
journal_title:Regional anesthesia and pain medicine
pub_type: 杂志文章
doi:10.1016/s1098-7339(99)90170-0
更新日期:1999-01-01 00:00:00
abstract:BACKGROUND:The underlying mechanisms of neuropathic pain remain unclear. This work aimed to investigate the role of Sirtuin3 (SIRT3), an nicotinamide adenosine dinucleotide+-dependent histone deacetylase, in the development of neuropathic pain induced by type 2 diabetes mellitus (T2DM) and to explore the associated mec...
journal_title:Regional anesthesia and pain medicine
pub_type: 杂志文章
doi:10.1136/rapm-2020-101918
更新日期:2021-01-01 00:00:00
abstract:BACKGROUND AND OBJECTIVES:In this study, we examined the consistency, rapidity, and reproducibility of the ABCDE technique for diaphragm identification. Operators using this method place the probe at the Anterior axillary line, watch for Breathing (lung sliding), and then move the probe Caudally to identify the Diaphra...
journal_title:Regional anesthesia and pain medicine
pub_type: 杂志文章
doi:10.1097/AAP.0000000000000718
更新日期:2018-02-01 00:00:00
abstract::The progression of sensory blockade in the hand following a forearm Bier block with ropivacaine is currently unknown. The hands of 10 healthy adult human subjects were anesthetized with ropivacaine, and their sensitivities to cold and touch were tested until the completion of anesthesia. On average, insensitivity to c...
journal_title:Regional anesthesia and pain medicine
pub_type: 杂志文章
doi:10.1097/AAP.0b013e31820d42ed
更新日期:2011-03-01 00:00:00
abstract:BACKGROUND AND OBJECTIVES:We wished to determine which long-acting local anesthetic would produce the least pain on injection for treatment of myofascial pain disorders. We compared the pain on intramuscular injection of bupivacaine, ropivacaine, bupivacaine with dexamethasone, ropivacaine with dexamethasone, and needl...
journal_title:Regional anesthesia and pain medicine
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1053/rapm.2000.8933
更新日期:2000-11-01 00:00:00
abstract:BACKGROUND AND OBJECTIVES:Shortening the onset time of sensory block is a practical goal to improve the quality of epidural anesthesia. The addition of fentanyl to a local anesthetic solution is widely used during epidural anesthesia. This randomized double-blind study examined the onset time of sensory block during ep...
journal_title:Regional anesthesia and pain medicine
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1053/rapm.2001.27852
更新日期:2001-11-01 00:00:00
abstract:OBJECTIVE:Sacroiliac joint injections are frequently performed procedures in the management of acute and chronic low-back pain, including patients with various immunocompromised states. Infectious complications following these procedures along with other spinal injections are rarely reported, but the true incidence is ...
journal_title:Regional anesthesia and pain medicine
pub_type: 杂志文章
doi:10.1097/AAP.0000000000000608
更新日期:2017-07-01 00:00:00
abstract:BACKGROUND AND OBJECTIVES:Peripherally administered opioids, e.g., intra-articular morphine, exert their analgesic action on local opioid receptors. The present study investigated the safety and efficacy of intrabursal oxycodone and bupivacaine in comparison with bupivacaine infiltration and interscalene brachial plexu...
journal_title:Regional anesthesia and pain medicine
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1016/s1098-7339(98)90030-x
更新日期:1998-09-01 00:00:00
abstract:BACKGROUND AND OBJECTIVES:The purpose of this randomized, double-blind study was to evaluate if use of an asymmetric spinal block affects the incidence of hypotension during spinal anesthesia. METHODS:With Ethical Committee approval and patient consent, 120 patients undergoing lower limb surgery were placed in the lat...
journal_title:Regional anesthesia and pain medicine
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1016/s1098-7339(99)90130-x
更新日期:1999-05-01 00:00:00