Table 1.
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.