Table 1.
Effects of mu and delta opioid receptor (MOR and DOR, respectively) agonists, and kappa opioid receptor (KOR) antagonists, in rodent models of depression a.
Target | Compound | Activity | Species | Behavioral test |
Effect |
---|---|---|---|---|---|
Opioid
receptors b |
enkephalins & endorphins [29] |
endogenous agonists |
rat | FS | antiD |
RB38A & RB38B [30] | enkephalinase inhibitors |
LH | antiD | ||
naloxone[31] | general antagonist |
depressant | |||
DOR | BUBU[46] | agonist | rat | LH | antiD |
RB101[46] | enkephalinase inhibitor |
||||
RB101[39] | enkephalinase inhibitor |
FS | |||
opiorphin[34] | endogenous enkephalinase inhibitor |
||||
SNC-80 (acute & chronic); SNC-86; SNC-162; BW363U86; DPDPE; deltorphin II; JOM-13; H-Dmt-Tic-NHCH2- Bid [32, 33, 35-38, 47] |
agonists | ||||
SNC-80[45] | agonist | olfactory bulbectomy |
|||
UFP-512[48] | agonist | rat & mouse |
FS | ||
RB101[41] | enkephalinase inhibitor |
mouse | FS, CSM | ||
opiorphin[49] | endogenous enkephalinase inhibitor |
FS | |||
SNC-80[43] | agonist | ||||
KNT-127[44] | agonist | ||||
NIH-11082[40] | agonist | ||||
MOR | morphine[31, 51] | agonist | rat | LH | antiD |
levorphanol, methadone, tramadol[53] |
agonists | ||||
opiorphin[49] | endogenous enkephalinase inhibitor |
mouse | TS | ||
codeine, tramadol[51] | agonists | FS | |||
morphine; codeine; levorphanol; methadone; tramadol[50] |
agonists | ||||
KOR | nor-BNI[57] | antagonist | rat | LH | antiD |
nor-BNI; JDTic[55, 56] | antagonist | FS | |||
U69593[56] | agonist | depressant |
Abbreviations: AntiD, antidepressant-like effect; BUBU, Tyr-D.Ser-O-tert-butyl.-Gly-Phe-Leu-ThrO-Tet-butyl-OH; BW363U86, (+)-4-[(R)-[(2S,5R)-2,5-dimethyl-4-(2-propenyl)-1-piperazinyl]-(3-hydroxyphenyl)methyl]-N,N-diethylbenzamide dihydrochloride; DPDPE, Tyr-D-Pen-Gly-Phe-D-Pen; Deltorphin II, Tyr-D-Ala-Phe-Glu-Val-Val-Gly-NH2; JDTic, (3R)-7-hydroxy-N-[(1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]-methyl]-2-methylpropyl]-1,2,3,4-tetrahydro-3isoquinolinec arboxamide; JOM-13, Tyr-c[D-Cys-Phe-DDPen]OH, a systemically active derivative of DPDPE; NIH-11082, (−)-(1R,5R,9R)-5,9-dimethyl-2′-hydroxy-2-(6-hydroxyhexyl)-6,7-benzomorphan hydrochloride; Nor-BNI, nor-binaltorphimine; RB38A, (R,S)HONH-CO-CH2-CH-(CH2CH6H5)-CONH-CH(CH2-C6H5)-COOH; RB38B, (S,S)HONH-CO-CH2-CH-(CH2C6H5)-CONH-CH-(CH2C6H5)-COOH; RB101, H3N-CH(CH2-CH2-SCH3)-CH2-S-S-CH2-CH(CH2)-CONH-CH(CH2)-COOCH2; SNC-80, ([()-4-[(R)--[(2S,5R)-2,5-dimethyl-4-(2-propenyl)-1-piperazinyl]-(3-methoxyphenyl)-methyl]-N,N-diethylbenzamide; U-69593, [5alpha,7alpha,8beta]-N-methyl-N-[7-[1-pyrrolidinyl]-1-oxaspiro[4.5]dec8-yl]-benzenacetamide; UFP-512, H-Dmt-Tic-NH-CH(CH2-COOH)-Bid.
The first row of the table shows general opioid effects, where MOR, DOR or KOR specificity was not addressed.