Skip to main content
. 2018 May;16(4):415–425. doi: 10.2174/1570159X15666170818102108

Table 1.

Efficacy of α7 neuronal nicotinic acetylcholine receptor ligands in various animal models of pain.

Compound Ligand Type Animal Model Animal Response Refs.
Choline Agonist Murine endotoxemia and sepsis Mice Reduced systemic TNF levels, suppressed HMGB1 release [73]
Choline Agonist Tail flick test Mice Antinociceptive [87]
Choline Agonist Incisional postoperative pain Mice Reduced thermal hyperalgesia and mechanical allodynia [97]
CDP-choline Source of choline Carrageenan Rats Reduced mechanical hyperalgesia
decreased TNF-α in the paw
[76]
CDP-choline Source of choline Oxaliplatin-induced CIPN Rats Reduced mechanical hyperalgesia [94]
CDP-choline Source of choline CCI Rats Reduced mechanical hyperalgesia [95]
JN403 Agonist CFA and partial sciatic nerve ligation models
Tail flick test
Rats Reduced mechanical hyperalgesia
Lack of effect
[86]
DMXB and
4-OH-DMXB
Partial agonist Tail flick test Mice Lack of effect by itself
blocked choline-induced antinociception
[87]
Compound-B Agonist CFA Rats, mice Reduced mechanical hyperalgesia [88]
Compound-B Agonist Carrageenan and CFA
Formalin models
Rats Reduced mechanical hyperalgesia
Attenuated pain behavior in formalin test
[104]
Nicotine Agonist CIA model Mice Ameliorated arthritis and reduced synovial inflammation [89]
AR-R17779 Agonist CIA model Mice Ameliorated arthritis and reduced synovial inflammation [89]
TC-7020 Agonist CCI Rats Reduced mechanical allodynia [91]
PHA-543613 Agonist CCI Mice Reduced mechanical allodynia [92]
PNU-282987 Agonist CCI Rats Reduced mechanical hyperalgesia [93]
NS1738 Type I PAM Carrageenan
CCI
Mice Reduced thermal hyperalgesia
Lack of effect
[92]
NS1738 Type I PAM Hot plate and tail-flick tests
Formalin model
Mice Lack of effect
Lack of effect
[103]
PNU-120596 Type II PAM Carrageenan
CCI
Mice Reduced thermal hyperalgesia
reduced thermal hyperalgesia and mechanical allodynia
potentiated effects of PHA-543613
[92]
PNU-120596 Type II PAM Carrageenan and CFA
Formalin model
Rats Reduced mechanical hyperalgesia and weight-bearing
deficit
lack of effect
[104]
PNU-120596 Type II PAM Hot plate and tail-flick tests formalin model Mice Lack of effect
Attenuated pain behavior in formalin test
[103]
2,4,2’,5’-tetrahydroxychalcone Type II PAM CFA Rats Lack of effect on thermal hyperalgesia reduced mechanical hyperalgesia [105]
3-furan-2-yl-N-p-tolyl-acrylamide Type II PAM Carrageenan
CFA
CCI
CPA
Mice Reduced mechanical allodynia by itself and potentiated antiallodynic effect of choline
Reduced thermal hyperalgesia
Reduced mechanical allodynia
Reversed negative affective behaviors
[106]
Compound Ligand Type Animal Model Animal Response Refs.
GAT107 Ago-PAM (allosteric agonist and type II PAM) Tail flick and hot plate tests
Formalin model
CFA and CCI models
LPS
Acetic acid induced visceral stretching and CPA
mice Lack of effect
antinociceptive
reduced thermal hyperalgesia and mechanical allodynia
reduced mechanical allodynia
decreased stretching behavior and reversed negative
affective behaviors
[36]
NS6740 Silent agonist Formalin model
CCI
CPA
mice Attenuated pain behavior in formalin test
reduced mechanical allodynia
reversed negative affective behaviors
[37]
PMP-072 Silent agonist CIA mice Reduced arthritis [109]

CCI—Chronic constrictive nerve injury, CFA—Complete Freund's adjuvant, CIA—collagen-induced arthritis, CIPN—chemotherapy-induced peripheral neuropathy, CPA—Conditioned place aversion, PAM—positive allosteric modulator, PSNL—Partial sciatic nerve ligation, SNL—Spinal nerve ligation.