Ketanserin

DuPre, Ann; Teitler, Milt

doi:10.1016/b978-008055232-3.61983-x

Cited by 3 publications

(2 citation statements)

References 42 publications

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“…Thus if fentanyl, directly or indirectly, influences the intrasynaptic levels of serotonin, it could also influence the excitability of the spinal motoneurons [43]. Ketanserin is a quinazoline derivative and acts as a selective 5HT 2A receptor antagonist [44]. Even though ketanserin administration did not reverse the increased distance moved in fentanyl-treated pigs in the current study, this does not rule out a role of serotonin in fentanyl-induced locomotor activity.…”

Section: Discussioncontrasting

confidence: 61%

“…Pigs in the fentanyl-saline group which received saline as injection 3 did not present with the transient ataxia but had a reduction in the duration of the stiff gait/posture pattern. The transient ataxia seen in pigs receiving ketanserin can possibly be explained by the blood pressure reducing capacity of the antagonist which is thought to be mediated primarily by antagonist action on the 5HT 2A receptor on arteriolar smooth muscle cells, and a possible weak α 1 -adrenergic receptor blocking effect [44,47,48]. Considering the short duration of the visible ataxia in this study, a transient drop in blood pressure seems like a plausible explanation.…”

Section: Discussionmentioning

confidence: 60%

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High and Hyper: Fentanyl Induces Psychomotor Side-Effects in Healthy Pigs

Digranes,

Haga,

Nordgreen

2023

Animals

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Analgesic effects of fentanyl have been investigated using behavior. The behavioral effects of fentanyl and possible serotonergic influence are largely unknown. We therefore investigated behavioral effects of fentanyl, with or without the serotonin antagonist ketanserin, in pigs. Fourteen mixed-breed pigs, weighing 17–25 kg were included in a randomised blinded prospective, balanced three-group study. Ten pigs received first 5 and then 10 µg/kg of fentanyl intravenously. Ketanserin at 1 mg/kg or saline was given intravenously as a third injection. Four control pigs received three injections of saline. Behavior was video-recorded. The distance moved was automatically measured by commercially available software, and behaviors manually scored in retrospect. Fentanyl inhibited resting and playing, and induced different repetitive behaviors. The mean (SD) distance moved in the control group and fentanyl group was 21.3 (13.0) and 57.8 (20.8) metres respectively (p < 0.05 for pairwise comparison). A stiff gait pattern was seen after fentanyl injection for median (range) 4.2 (2.8–5.1) minutes per 10 min, which was reduced to 0 (0–4) s after ketanserin administration. Conclusion: fentanyl-induced motor and behavioral effects, and serotonergic transmission may be involved in some of them. The psychomotor side effects of fentanyl could potentially interfere with post-operative pain evaluation in pigs.

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Section: Discussioncontrasting

confidence: 61%

Section: Discussionmentioning

confidence: 60%

High and Hyper: Fentanyl Induces Psychomotor Side-Effects in Healthy Pigs

Digranes,

Haga,

Nordgreen

2023

Animals

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Motor effects of fentanyl in isoflurane-anaesthetized pigs and the subsequent effect of ketanserin or naloxone

Digranes,

Hoeberg,

Lervik

et al. 2024

Veterinary Anaesthesia and Analgesia

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Asymmetric Synthesis of Trifluoroethyl-Based, Chiral 3-Benzyloxy-1- and -2-Phenyl-quinazolinones of Biomedicinal Interest by Radical Type Cross-Coupling to Olefins

Chen

Chang

Tseng

et al. 2022

IJMS

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Several 2-substituted (H, Ph, and S-Me) and 1-substituted (H, Ph, and Bn), 3-hydroxy-1,3-quinazolin(di)ones were utilized for the first time as radical trapping agents in asymmetric 1,2-oxytrifluoromethylation of styrenes catalyzed by chiral vanadyl methoxide complexes bearing 3,5-disubstituted-N-salicylidene-t-leucinate templates. The effects of catalysts and solvents on the asymmetric induction were systematically examined. The best and complementary scenarios involved the use of vanadyl complexes V(O)-1 and V(O)-2, which bear 3-(2,5-dimethyl)phenyl-5-bromophenyl and 3-t-butyl-5-bromophenyl groups in an i-propanol solvent at ambient temperature. The corresponding (R)-cross-coupling products by V(O)-1 were obtained in 45–71% (for 2-substituted series) and 59–93% yields (for 1-substituted series) for p-/m-methylstyrenes and m-halo/CF3/CO2Me-styrenes in 38–63% ees (the best in 2-H case) and 60–84% ees (the best in 1-benzyl cases), respectively. The corresponding (S)-cross-coupling products by V(O)-2 were obtained in 28–55% (for 2-substituted series) and 45–72% yields (for 1-substituted series) for the same substrate class in 50–91% ees (85–91% ees in 2-phenyl cases) and 64–75% ees (up to 74–75% ees for each 1-H, Ph, and Bn cases), respectively. Theoretical calculations were carried out to explain the origin and extent of enantiocontrols. They both may serve as potential inhibitors of acetohydroxyacid synthase and epidermal growth factor receptor (EGFR) kinases.

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Ketanserin

Cited by 3 publications

References 42 publications

High and Hyper: Fentanyl Induces Psychomotor Side-Effects in Healthy Pigs

High and Hyper: Fentanyl Induces Psychomotor Side-Effects in Healthy Pigs

Motor effects of fentanyl in isoflurane-anaesthetized pigs and the subsequent effect of ketanserin or naloxone

Asymmetric Synthesis of Trifluoroethyl-Based, Chiral 3-Benzyloxy-1- and -2-Phenyl-quinazolinones of Biomedicinal Interest by Radical Type Cross-Coupling to Olefins

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