Abstract:
:Antagonists of the serotonergic 5-hydroxytryptamine 3A receptor (5-HT(3A)R) and muscle nicotinic acetylcholine receptors (nAChR) are widely used in anesthesia practice. Both 5-HT(3A)R and nAChR are ligand-gated ion channels with known pharmacological overlap between some of their agonists and antagonists. We studied the actions of clinically used 5-HT(3A)R antagonist antiemetics and nondepolarizing muscle blockers on ionic currents elicited by the activation of mammalian 5-HT(3A)R and muscle nAChR, expressed in Xenopus laevis oocytes. Currents were recorded using a whole-cell two-electrode voltage clamp technique. Dolasetron, ondansetron, and granisetron reversibly inhibited 5-HT(3A)R function at nanomolar concentrations with 50% inhibitory concentrations (IC(50)) of 11.8, 6.4, and 0.2 nM; the rank order of inhibition correlated well with their clinical antiemetic potencies. The principal metabolite of dolasetron, hydrodolasetron, was 40 times more potent than the parent compound on 5-HT(3A)R (IC(50) = 0.29 nM). The potency of the nondepolarizing muscle blocker d-tubocurarine in blocking 5-HT(3A)R was similar to that of the antiemetics and significantly more than vecuronium and rapacuronium (IC(50) = 11.4 nM, 18.9 microM, 60.5 microM). Conversely, ondansetron, dolasetron, and granisetron also reversibly inhibited nAChR currents in a dose-dependent manner with IC(50)s of 14.2, 7.8, and 4.4 microM for the adult nAChR and 16.0, 18.6, and 13.9 microM for the embryonic nAChR. Again, hydrodolasetron showed significantly (10 times) more inhibitory potency on the adult nAChR than the parent compound dolasetron. These results indicate that drugs that target specific ligand-gated ion channels may also affect other ion channel types.
journal_name
Anesth Analgjournal_title
Anesthesia and analgesiaauthors
Paul M,Callahan R,Au J,Kindler CH,Yost CSdoi
10.1213/01.ANE.0000160531.65953.77subject
Has Abstractpub_date
2005-09-01 00:00:00pages
715-21, table of contentsissue
3eissn
0003-2999issn
1526-7598pii
101/3/715journal_volume
101pub_type
杂志文章abstract::A claim of superiority of one intervention over another often depends naturally on results from several outcomes of interest. For such studies the common practice of making conclusions about individual outcomes in isolation can be problematic. For example, an intervention might be shown to improve one outcome (e.g., p...
journal_title:Anesthesia and analgesia
pub_type: 杂志文章
doi:10.1213/ANE.0b013e3182504435
更新日期:2012-06-01 00:00:00
abstract:UNLABELLED:Recent reports have discussed the potential risk of transient radicular irritation (TRI) after spinal anesthesia with lidocaine. Because we have not encountered such neurologic sequelae with the high incidence reported, we prospectively examined the incidence of TRI after spinal anesthesia with lidocaine. On...
journal_title:Anesthesia and analgesia
pub_type: 杂志文章
doi:10.1097/00000539-199805000-00022
更新日期:1998-05-01 00:00:00
abstract:UNLABELLED:Capsaicin can produce a selective and long-lasting neural blockade. Resiniferatoxin (RTX) is an ultrapotent vanilloid agonist with a unique spectrum of activities different from that of capsaicin. We sought to determine whether a single application of RTX to a peripheral nerve could completely prevent the lo...
journal_title:Anesthesia and analgesia
pub_type: 杂志文章
doi:10.1097/00000539-200205000-00038
更新日期:2002-05-01 00:00:00
abstract:UNLABELLED:We compared, in a double-blinded manner, the anesthetic maintenance and recovery properties of remifentanil with a clinically comparable fentanyl-based anesthetic technique in pediatric ambulatory surgical patients. Anesthesia was induced with either halothane or sevoflurane and nitrous oxide and oxygen. Pat...
journal_title:Anesthesia and analgesia
pub_type: 临床试验,杂志文章,多中心研究,随机对照试验
doi:10.1097/00000539-200004000-00017
更新日期:2000-04-01 00:00:00
abstract::The effects of narcotic agents and two inhalation anesthetics on intrabiliary pressure (IBP) were measured before and after morphine (0.2 mg/kg), meperidine (2 mg/kg), fentanyl (0.002 mg/kg), or pentazocine (1 mg/kg) given intramuscularly to guinea pigs, and after halothane (0.5, 1.0, 1.5, or 2.0 MAC) or enflurane (sa...
journal_title:Anesthesia and analgesia
pub_type: 杂志文章
doi:
更新日期:1979-03-01 00:00:00
abstract:BACKGROUND:Respiratory variations in arterial pulse pressure (DeltaPP) are accurate predictors of fluid responsiveness in mechanically ventilated patients. The aim of our study was to assess the ability of a novel algorithm for automatic estimation of stroke volume variation (SVV) to predict fluid responsiveness in mec...
journal_title:Anesthesia and analgesia
pub_type: 杂志文章
doi:10.1213/ane.0b013e318192a36b
更新日期:2009-02-01 00:00:00
abstract::Cardioprotection by anesthetic preconditioning (APC) can be abolished by nitric oxide (NO*) synthase inhibitors or by reactive oxygen species (ROS) scavengers. We previously reported attenuated mitochondrial electron transport (ET) and increased ROS generation during preconditioning sevoflurane exposure as part of the...
journal_title:Anesthesia and analgesia
pub_type: 杂志文章
doi:10.1213/01.ANE.0000139346.76784.72
更新日期:2005-01-01 00:00:00
abstract::Common practice during local anesthetic injection is to warn the patient using words such as: "You will feel a big bee sting; this is the worst part." Our hypothesis was that using gentler words for administration of the local anesthetic improves pain perception and patient comfort. One hundred forty healthy women at ...
journal_title:Anesthesia and analgesia
pub_type: 杂志文章,随机对照试验
doi:10.1213/ANE.0b013e3181cc5727
更新日期:2010-03-01 00:00:00
abstract::A recognized side effect of chemonucleolysis is life-threatening anaphylaxis to chymopapain. In the clinical trials of chymopapain, 13 cases of anaphylaxis were reported in 1585 administrations (0.82%). Two patients died. Data from a postmarketing survey (48,239 questionnaires) were reviewed to identify factors influe...
journal_title:Anesthesia and analgesia
pub_type: 杂志文章
doi:
更新日期:1985-12-01 00:00:00
abstract:UNLABELLED:Many drugs are tested intrathecally to investigate alternatives to opioids. We aimed to explore the analgesic and possible neurotoxic effects of chronic intrathecally-administered ketorolac tromethamine in rats. Catheters were placed via atlantoaxial interval in 28 Wistar rats under anesthesia of intraperito...
journal_title:Anesthesia and analgesia
pub_type: 杂志文章
doi:10.1213/01.ane.0000093226.75543.90
更新日期:2004-01-01 00:00:00
abstract::The management of severe pain may require "balanced analgesia," involving the use of analgesics with different modes of action. Clonidine, an alpha(2)-adrenoreceptor agonist produces analgesia by itself as well as when given with morphine and local anesthetics. Ketorolac is indicated for the management of moderately s...
journal_title:Anesthesia and analgesia
pub_type: 杂志文章
doi:10.1097/00000539-200005000-00028
更新日期:2000-05-01 00:00:00
abstract::To further investigate possible prolongation of the frequency-corrected QT interval (QTc interval) after administration of droperidol (DRO), we studied 40 surgical patients who were randomly assigned to one of three groups, receiving an intravenous (IV) injection of either 0.1 mg/kg (Group 1, n = 10), 0.175 mg/kg (Gro...
journal_title:Anesthesia and analgesia
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1213/00000539-199411000-00028
更新日期:1994-11-01 00:00:00
abstract::Catecholamine-induced desensitization of beta-adrenergic receptors resulting in hyporesponsiveness to further stimulation has been frequently reported after an increase in endogenous catecholamines. To examine the possibility of beta-adrenoceptor desensitization due to intraoperative adrenergic activation (surgical st...
journal_title:Anesthesia and analgesia
pub_type: 杂志文章
doi:10.1213/00000539-199007000-00001
更新日期:1990-07-01 00:00:00
abstract::Total knee arthroplasty (TKA) may result in severe pain, and single-injection femoral nerve blocks (SFNB) have been demonstrated to have a limited duration of analgesia. Continuous femoral nerve blocks (CFNB) can prolong the analgesic duration of SFNB. We prospectively randomized 36 patients undergoing TKA to CFNB ver...
journal_title:Anesthesia and analgesia
pub_type: 杂志文章,随机对照试验
doi:10.1213/01.ane.0000198675.20279.81
更新日期:2006-04-01 00:00:00
abstract::Persistent postoperative opioid use is thought to contribute to the ongoing opioid epidemic in the United States. However, efforts to study and address the issue have been stymied by the lack of a standard definition, which has also hampered efforts to measure the incidence of and risk factors for persistent postopera...
journal_title:Anesthesia and analgesia
pub_type: 杂志文章,实务指引
doi:10.1213/ANE.0000000000003941
更新日期:2019-08-01 00:00:00
abstract:BACKGROUND:The purpose of this study was to identify optimal target propofol and remifentanil concentrations to avoid a gag reflex in response to insertion of an upper gastrointestinal endoscope. METHODS:Patients presenting for endoscopy received target-controlled infusions (TCI) of both propofol and remifentanil for ...
journal_title:Anesthesia and analgesia
pub_type: 杂志文章,随机对照试验
doi:10.1213/ANE.0000000000000756
更新日期:2015-07-01 00:00:00
abstract::Several observational and objective methods are available to assess sedation depth; however, data regarding their accuracy in differentiating deep sedation are limited. In this study we compared 3 sedation tools in children from birth to 18 yr of age and determined their relative value in detecting deep levels of seda...
journal_title:Anesthesia and analgesia
pub_type: 杂志文章
doi:10.1213/01.ANE.0000184045.01780.73
更新日期:2006-02-01 00:00:00
abstract::As of November 2016, the Florida Department of Health (FDH) and the Centers for Disease Control and Prevention have confirmed more than 4000 travel-related Zika virus (ZIKV) infections in the United States with >700 of those in Florida. There have been 139 cases of locally acquired infection, all occurring in Miami, F...
journal_title:Anesthesia and analgesia
pub_type: 杂志文章
doi:10.1213/ANE.0000000000002047
更新日期:2017-06-01 00:00:00
abstract:IMPLICATIONS:We report a unique case of acute anaphylaxis after mediastinal irrigation with a dilute bacitracin solution. ...
journal_title:Anesthesia and analgesia
pub_type: 杂志文章
doi:10.1097/00000539-200010000-00049
更新日期:2000-10-01 00:00:00
abstract:BACKGROUND:Previous studies have demonstrated that Homer 1b/c, a postsynaptic molecular scaffolding protein that binds and clusters metabotropic glutamate receptors at neuronal synapses, has an important role in the metabotropic glutamate receptor signaling process. In the current study, we investigated the possible in...
journal_title:Anesthesia and analgesia
pub_type: 杂志文章
doi:10.1213/ANE.0b013e31822c0b98
更新日期:2011-12-01 00:00:00
abstract:UNLABELLED:Prolongation of the Q-T interval may be associated with polymorphic ventricular tachycardia known as torsade de pointes, syncope and sudden death. Existing data show that isoflurane prolongs the Q-T interval, whereas halothane shortens it. The aim of this study was to determine whether sevoflurane or propofo...
journal_title:Anesthesia and analgesia
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1097/00000539-200001000-00006
更新日期:2000-01-01 00:00:00
abstract::Sufentanil is a new synthetic opiate analgesic that is 4520 times more potent than morphine in animal experiments. This study evaluated the cardiovascular effects of sufentanil, 15 micrograms/kg, and air/O2 used as a complete anesthetic with 50% inspired oxygen (air/O2 mixture) in 40 adult patients undergoing elective...
journal_title:Anesthesia and analgesia
pub_type: 杂志文章
doi:
更新日期:1982-02-01 00:00:00
abstract::The insertion of implantable cardioverter/defibrillators (ICD) requires induction of repeated episodes of ventricular fibrillation (VF). The neuropsychological repercussions associated with repeated inducement of hypotension and cerebral ischemia are unknown. In this prospective clinical trial, 1 day prior to ICD asse...
journal_title:Anesthesia and analgesia
pub_type: 临床试验,杂志文章
doi:10.1097/00000539-199706000-00003
更新日期:1997-06-01 00:00:00
abstract::In pediatric practice, complications due to the laryngeal mask airway (LMA) have been studied with size 2 LMA, but not with size 1 LMA. We, therefore, compared prospectively the complications induced by LMA size 1 and 2 in 141 children aged 21 days to 11 yr. Intraoperative and lowest SpO2 values after removal of LMA w...
journal_title:Anesthesia and analgesia
pub_type: 杂志文章
doi:10.1213/00000539-199303000-00012
更新日期:1993-03-01 00:00:00
abstract:UNLABELLED:This study was designed to determine if, and to what extent, antithrombin III (AT) levels affect the response of the activated clotting time (ACT) to heparin in concentrations used during cardiac surgery, and to characterize the relationship between AT levels and markers of activation of coagulation during c...
journal_title:Anesthesia and analgesia
pub_type: 杂志文章
doi:10.1097/00000539-199709000-00005
更新日期:1997-09-01 00:00:00
abstract::Acute angle closure glaucoma is a rare complication of general anesthesia. However, in case of delayed diagnosis, it may lead to blindness. We present a case of bilateral acute angle closure glaucoma after cervical spine surgery under general anesthesia in a hypermetropic patient. In this case, the most likely trigger...
journal_title:Anesthesia and analgesia
pub_type: 杂志文章
doi:10.1213/ANE.0b013e3182009ad6
更新日期:2011-01-01 00:00:00
abstract:BACKGROUND:Preoperative risk stratification is a critical element in assessing the risks and benefits of surgery. Prior work has demonstrated that intra-abdominal general surgery patients can be classified based on their comorbidities and risk factors using latent class analysis (LCA), a model-based clustering techniqu...
journal_title:Anesthesia and analgesia
pub_type: 杂志文章
doi:10.1213/ANE.0000000000002345
更新日期:2018-03-01 00:00:00
abstract:BACKGROUND:The bispectral index (BIS) monitor has been available for clinical use for >20 years and has had an immense impact on academic activity in Anesthesiology, with >3000 articles referencing the bispectral index. Despite attempts to infer its algorithms by external observation, its operation has nevertheless rem...
journal_title:Anesthesia and analgesia
pub_type: 杂志文章
doi:10.1213/ANE.0000000000005220
更新日期:2020-12-01 00:00:00
abstract::Cardiopulmonary bypass (CPB) impairs pulmonary endothelial injury in part by increasing expression of adhesion molecules that results in neutrophil influx. Although numerous proinflammatory cytokines up-regulate these responses, the extent to which systemic and pulmonary proinflammatory cytokines increase remains unkn...
journal_title:Anesthesia and analgesia
pub_type: 杂志文章
doi:10.1097/00000539-200005000-00008
更新日期:2000-05-01 00:00:00
abstract:BACKGROUND:The inflated costs and documented deleterious effects of excess perioperative transfusion have led to the investigation of targeted coagulation factor replacement strategies. One particular coagulation factor of interest is factor I (fibrinogen). Hypofibrinogenemia is typically tested for using time-consumin...
journal_title:Anesthesia and analgesia
pub_type: 临床试验,杂志文章
doi:10.1213/ANE.0000000000001465
更新日期:2016-09-01 00:00:00