Abstract:
BACKGROUND AND OBJECTIVE:Long-acting nociceptive-selective regional anesthesia has remained an elusive clinical goal. We aspired to identify a novel compound that would produce nociceptive-selective regional anesthesia through the transient receptor potential vanilloid 1 (TRPV1) channels. METHODS:We designed and synthesized a novel compound (LL-a) that penetrates the cell membrane through TRPV1 channels and binds to voltage-gated sodium channels. The regional anesthetic effect of LL-a was evaluated in a rodent sciatic nerve block model. Electrophysiological recording was applied to test the inhibition of LL-a on voltage-gated sodium channel currents. RESULTS:LL-a inhibited sodium channel currents on the dorsal root ganglion neurons of mice and this action was diminished by TRPV1 channel knockout. In a sciatic nerve block model of a rat, 0.2% and 0.4% (w/v) LL-a produced selective sensory block with median (IQR) durations of 42.0 (24.0, 48.0) and 72.0 (69.0, 78.0) hours, respectively. No motor block was found for 0.2% LL-a. 0.4% LL-a produced a motor block with a median (IQR) duration of 3.0 (0.0, 6.0) hours. This selective sensory block was not observed on TRPV1 knockout mice. As a positive control, 0.5% and 0.75% levobupivacaine produced a non-selective sciatic nerve block with median (IQR) durations of 2.8 (2.6, 2.8) and 3.8 (3.8, 4.8) hours, respectively. No systemic or local irritation was observed during injection of LL-a and sensory and motor function completely recovered for all the animals. CONCLUSIONS:LL-a is a potential novel local anesthetic for long-lasting nociceptive-selective analgesia.
journal_name
Reg Anesth Pain Medjournal_title
Regional anesthesia and pain medicineauthors
Zhou C,Tang L,Yin Q,Yang L,Gong D,Kang Y,Cao H,Fan J,Zhang Y,Qian D,Zhang Q,Ke B,Liu J,Zhang W,Yang Jdoi
10.1136/rapm-2019-101057subject
Has Abstractpub_date
2020-06-01 00:00:00pages
412-418issue
6eissn
1098-7339issn
1532-8651pii
rapm-2019-101057journal_volume
45pub_type
杂志文章abstract:BACKGROUND AND OBJECTIVES:Amputations of the lower extremity remain a common procedure in a high-risk population. Perioperative morbidity and mortality reach as high as 14.1% in below-knee amputations. We aimed to determine whether regional, or neuraxial, anesthesia, when compared with general anesthesia (GA), would be...
journal_title:Regional anesthesia and pain medicine
pub_type: 杂志文章
doi:10.1097/AAP.0000000000000687
更新日期:2018-01-01 00:00:00
abstract:BACKGROUND AND OBJECTIVES:The aim of this study was to compare the potency of bupivacaine, ropivacaine, and levobupivacaine in an equal dose and concentration for sympathetic block. METHODS:We measured mean arterial pressure, heart rate (HR), and right and left brachial artery blood flow (BABF) before and after cervic...
journal_title:Regional anesthesia and pain medicine
pub_type: 杂志文章
doi:10.1097/AAP.0b013e3181e6acf1
更新日期:2010-09-01 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:This case series assesses the in vivo spread of contrast within the adductor canal in subjects who recently underwent a total knee arthroplasty. A previous analysis of profound leg weakness with a continuous adductor canal revealed contrast spread from the adductor canal to the femoral triangl...
journal_title:Regional anesthesia and pain medicine
pub_type: 杂志文章
doi:10.1097/AAP.0000000000000216
更新日期:2015-03-01 00:00:00
abstract::Potassium (K+) channels form the largest family of ion channels with more than 70 such genes identified in the human genome. They are organized in 3 superfamilies according to their predicted membrane topology: (1) subunits with 6 membrane-spanning segments and 1-pore domain, (2) subunits with 2 membrane-spanning segm...
journal_title:Regional anesthesia and pain medicine
pub_type: 杂志文章,评审
doi:10.1016/j.rapm.2004.12.001
更新日期:2005-05-01 00:00:00
abstract:BACKGROUND AND OBJECTIVES:Anesthesia and analgesia with paravertebral block are reportedly variable. Existence of an endothoracic fascia has been proposed as one of the possible mechanisms leading to variability. We undertook an electron-microscopy imaging study to investigate the endothoracic fascia in the thoracic pa...
journal_title:Regional anesthesia and pain medicine
pub_type: 杂志文章
doi:10.1097/AAP.0b013e31824451cb
更新日期:2012-03-01 00:00:00
abstract:BACKGROUND AND OBJECTIVES:Ultrasound-guided infiltration of the interspace between the popliteal artery and capsule of the knee (iPACK) block, a new regional analgesic technique, is believed to relieve posterior knee pain, after total knee arthroplasty, by targeting the articular branches innervating posterior aspect o...
journal_title:Regional anesthesia and pain medicine
pub_type: 杂志文章
doi:10.1136/rapm-2018-100355
更新日期:2019-05-06 00:00:00
abstract:OBJECTIVE:Local anesthetic-induced cardiotoxicity remains a complication of regional anesthesia, with the potential to result in cardiac arrest refractory to resuscitation. Successful resuscitation using Intralipid (Baxter Pharmaceuticals by Fresenius Kabi, Uppsala, Sweden), has been reported in 2 patients with bupivac...
journal_title:Regional anesthesia and pain medicine
pub_type: 杂志文章
doi:10.1016/j.rapm.2007.09.006
更新日期:2008-03-01 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
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journal_title:Regional anesthesia and pain medicine
pub_type: 杂志文章
doi:10.1097/AAP.0b013e318228d1c0
更新日期:2011-09-01 00:00:00
abstract:BACKGROUND:Ultrasound (US) guidance, in some instances, can increase the success rate and reduce the onset and procedure times for peripheral nerve blockade compared with traditional nerve localization techniques. The presumptive mechanism for these benefits is the ability to accurately inject local anesthetic circumfe...
journal_title:Regional anesthesia and pain medicine
pub_type: 杂志文章,随机对照试验
doi:10.1097/AAP.0b013e318217a6a1
更新日期:2011-05-01 00:00:00
abstract:BACKGROUND AND OBJECTIVES:Ropivacaine is a potent local anesthetic that, experimentally at low concentrations, produces an effective block of pain conducting nerve fibers. Therefore, it was hypothesized that 0.1% and 0.2% ropivacaine would provide clinically adequate postoperative analgesia in continuous axillary 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(00)80010-3
更新日期:2000-01-01 00:00:00
abstract:BACKGROUND AND OBJECTIVES:Continuous brachial plexus blocks at the interscalene level are associated with known diaphragm dysfunction from phrenic nerve paresis. More distal blocks along the brachial plexus may provide postsurgical analgesia while potentially having less effect on diaphragm function. Continuous intersc...
journal_title:Regional anesthesia and pain medicine
pub_type: 杂志文章,随机对照试验
doi:10.1097/AAP.0000000000000578
更新日期:2017-05-01 00:00:00
abstract:BACKGROUND AND OBJECTIVES:Prior to this investigation, there was no approach to compare both the potency of local anesthetics and their time course of action in a reproducible nociceptive system in humans. We tested whether the vascularly isolated vein segment is appropriate for such an approach. METHODS:In six health...
journal_title:Regional anesthesia and pain medicine
pub_type: 杂志文章
doi:10.1016/s1098-7339(99)90105-0
更新日期:1999-07-01 00:00:00
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journal_title:Regional anesthesia and pain medicine
pub_type: 杂志文章,随机对照试验
doi:10.1097/AAP.0000000000000496
更新日期:2016-11-01 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: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:Concern for block-related injury and liability has dissuaded many anesthesiologists from using regional anesthesia for eye and extremity surgery, despite many studies demonstrating the benefits of regional over general anesthesia. To determine injury patterns and liability associated with eye ...
journal_title:Regional anesthesia and pain medicine
pub_type: 杂志文章,多中心研究
doi:10.1016/j.rapm.2008.01.016
更新日期:2008-09-01 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
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journal_title:Regional anesthesia and pain medicine
pub_type: 杂志文章
doi:10.1136/rapm-2019-100859
更新日期:2020-01-12 00:00:00
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journal_title:Regional anesthesia and pain medicine
pub_type: 杂志文章
doi:10.1097/AAP.0b013e31820d4334
更新日期:2011-05-01 00:00:00
abstract:BACKGROUND AND OBJECTIVES:Whether patients titrate themselves to an individualized blood or plasma opioid concentration (the so-called minimum effective concentration or [MEC]) has been debated extensively. Nevertheless, there is consistent opinion that during patient controlled analgesia (PCA) patients balance accepta...
journal_title:Regional anesthesia and pain medicine
pub_type: 临床试验,杂志文章
doi:10.1016/s1098-7339(00)90008-7
更新日期:2000-05-01 00:00:00
abstract:BACKGROUND AND OBJECTIVES:The benefit of adding sciatic nerve block (SNB) to femoral nerve block to improve analgesia after total knee arthroplasty (TKA) is uncertain. We hypothesized that the effective duration of single-injection SNB is too short to improve postoperative analgesia and that this contributes to conflic...
journal_title:Regional anesthesia and pain medicine
pub_type: 杂志文章,随机对照试验
doi:10.1097/AAP.0000000000000076
更新日期:2014-05-01 00:00:00
abstract:BACKGROUND AND OBJECTIVES:The incidence of postdural puncture headache (PDPH) after epidural wet tap for obstetric patients may be as high as 75%. We have studied how subsequent placement of a subarachnoid catheter immediately after confirmation of a wet tap, and leaving the catheter in place for 24 hours affects the i...
journal_title:Regional anesthesia and pain medicine
pub_type: 杂志文章
doi:10.1016/s1098-7339(03)00393-6
更新日期:2003-11-01 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: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:OBJECTIVE:To describe a late neurologic complication of intrathecal pump implantation and show the methods used for the diagnosis and successful treatment of transverse myelitis in this setting. CASE REPORT:A 32-year-old man with a chronic abdominal pain syndrome presented with right lower-extremity numbness 2 months ...
journal_title:Regional anesthesia and pain medicine
pub_type: 杂志文章
doi:10.1016/s1098-7339(03)00222-0
更新日期:2003-09-01 00:00:00
abstract:BACKGROUND:Third occipital nerve block (TONB) is commonly used in the diagnosis and treatment of upper neck pain and cervicogenic headaches. Although fluoroscopy is the current imaging standard for TONB, ultrasound (US) guidance offers a promising, radiation-free alternative. In this randomized, observer-blinded trial,...
journal_title:Regional anesthesia and pain medicine
pub_type: 杂志文章,随机对照试验
doi:10.1097/AAP.0b013e31828b25bc
更新日期:2013-05-01 00:00:00
abstract:OBJECTIVE:We present an occurrence of a severe but transient neurologic complication after intraneural injection during an ultrasound-guided interscalene block. CASE REPORT:A 36-year-old man underwent ultrasound-guided interscalene nerve blockade before shoulder incision and drainage. On postoperative day 1, he exhibi...
journal_title:Regional anesthesia and pain medicine
pub_type: 杂志文章
doi:10.1097/aap.0b013e3181e8a35f
更新日期:2010-07-01 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