A solid state device for measuring sensitivity to thermal pain

Walker, J. Michael; Dixon, William C.

doi:10.1016/0031-9384(83)90155-5

Cited by 19 publications

(8 citation statements)

References 12 publications

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“…In all treated groups, no effect on nociception (Walker & Dixon 1985) was observed in the tail immersion test (Cowan 1990) and the hot plate method (Kitchen & Crowder 1985) up to 10 mg kg −1 . An impairment of motor activity could not be observed in all tested models up to a dose of 10 mg kg −1 in the wire mesh grasping and the rota-rod test.…”

Section: Nociception and Motor Activity Testsmentioning

confidence: 89%

Synthesis and evaluation of N-(3-oxo-2,3-dihydro-1H-pyrazol-4-yl)-1H-indole-carboxamides as cholecystokinin antagonists

Lattmann

Singh

Boonprakob

et al. 2006

Journal of Pharmacy and Pharmacology

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The structure-activity relationship optimization of the pyrazoline template 3a resulted in novel 3-oxo-1,2-diphenyl-2,3-dihydro-1H-pyrazol-4-yl)-indole carboxamides 4a-4e. These non-peptidal CCK ligands have been shown to act as potent CCK1 ligands in a [125]I-CCK-8 receptor binding assay. The best amides (4c and 4d) of this series displayed an IC50 of 20/25 nM for the CCK1 receptor. In a subsequent in-vivo evaluation using various behaviour pharmacological assays, an anxiolytic effect of these novel 3-oxo-1,2-diphenyl-2,3-dihydro-1H-pyrazol-4-yl)-indole carboxamides was found at high doses in the elevated plus-maze. In the despair swimming test, a model for testing antidepressants, an ED50 of 0.33/0.41 mg kg(-1) was determined for amide 4c/4d and the antidepressant effect had a magnitude comparable to desimipramine.

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Section: Nociception and Motor Activity Testsmentioning

confidence: 89%

Synthesis and evaluation of N-(3-oxo-2,3-dihydro-1H-pyrazol-4-yl)-1H-indole-carboxamides as cholecystokinin antagonists

Lattmann

Singh

Boonprakob

et al. 2006

Journal of Pharmacy and Pharmacology

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“…Finger flick task A modified tail flick apparatus similar to that described by Walker and Dixon (1983) was used as a finger flick apparatus. In brief, the finger flick device consists of a radiant heat source, photocell, timer, and power source.…”

Section: Methodsmentioning

confidence: 99%

“…Our radiant heat methodology is practical to implement. The finger flick device was inexpensive to build based on the design described by Walker and Dixon (1983). As mentioned earlier, laser pulse methodologies produce reliable pain threshold responses, yet the high cost of the equipment makes them impractical to most laboratories (Chery- Croze, 1983).…”

Section: Methodsmentioning

confidence: 99%

A novel radiant heat test for assessing pain threshold in human subjects: Measurement stability

Lee

Stitzer

1995

Behavior Research Methods, Instruments, & Computers

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New methodologies to assess analgesic response in humans are needed to better integrate preclinical and clinical data. In the present study we examined the test-retest stability of an innovative radiant heat methodology compared with an electrical stimulation methodology. For the radiant heat task, a modified rodent tail flick apparatus was used, The latency for fmger withdrawal was recorded. For the electrical stimulation tasks, subjects placed two fingers on two electrodes from which they received a brief series of increasingly intense electrical stimulations. Maximumstimulus intensity (in milliamps) delivered was recorded. On each of 4 test days, the subjects received five test trials with a lO-min interval between trials. Allthe subjects were tested twice on each apparatus in a counterbalanced design. Finger withdrawal latencies for the radiant heat task did not differ significantly across test trials or test days. Finger withdrawal scores for electrical stimulation increased significantly across test trials as well as test days. These data show that the radiant heat method generates consistent latencies across trials and days, whereas shock produces trends over time. The radiant heat task, which is convenient to operate and inexpensive to build, appears promising as a reliable test of pain threshold in humans.

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“…In all treated groups, no effect on nociception for doses of up to 5 mg/kg was observed for the furanone 18 in the tail immersion test as a single agent. Administered in conjunction with tramadol/morphine and desimipramine at 0.05 mg/kg showed no potentiation of analgesia and a clinically relevant significant effect was observed at 0.5 mg/kg.…”

Section: Resultsmentioning

confidence: 85%

“…The effects of CCK on the modulation of pain transmission and the opioid effects are well established , and typically a low dose of morphine or a high dose of a weak opiate agonist will result in a good potentiation of analgesia in the tail immersion test .…”

Section: Resultsmentioning

confidence: 99%

Analgesic Effects of 5‐Alkyloxy‐4‐amino‐2(5H)‐furanones as Cholecystokinin‐2 Antagonists

Lattmann

Sattayasai

Schwalbe

et al. 2016

Archiv der Pharmazie

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4-Amino-2(5H)-furanones were synthesized in high yields over two synthetic steps from readily available mucochloric acid. These 5-alkyloxy-4-amino-2(5H)-furanones were screened in a ([125]) I-CCK-8 radioligand receptor binding assay for CCK2 affinity and novel active ligands in the nanomolar range were identified. SAR was optimized leading to the cyclohexyl derivative 25 with an IC50 of 27 nM. Furanone 18 was obtained as a stable crystalline material with an IC50 of 85 nM, but had a higher CCK2 selectivity. It was subsequently tested in the isolated guinea pig ileum assay with sulfated CCK8 , and the CCK antagonizing properties of the ligand were confirmed. The CCK2 selective antagonist 18 was found to potentiate analgesia in the tail flick assay in mice, for the strong opiate morphine, the partial opiate agonist tramadol and the tricyclic antidepressant desimipramine.

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A solid state device for measuring sensitivity to thermal pain

Cited by 19 publications

References 12 publications

Synthesis and evaluation of N-(3-oxo-2,3-dihydro-1H-pyrazol-4-yl)-1H-indole-carboxamides as cholecystokinin antagonists

Synthesis and evaluation of N-(3-oxo-2,3-dihydro-1H-pyrazol-4-yl)-1H-indole-carboxamides as cholecystokinin antagonists

A novel radiant heat test for assessing pain threshold in human subjects: Measurement stability

Analgesic Effects of 5‐Alkyloxy‐4‐amino‐2(5H)‐furanones as Cholecystokinin‐2 Antagonists

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