3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer: A non-peptide, kappa-opioid receptor agonist which has also been found to stimulate the release of adrenocorticotropin (ADRENOCORTICOTROPIC HORMONE) via the release of hypothalamic arginine vasopressin (ARGININE VASOPRESSIN) and CORTICOTROPIN-RELEASING HORMONE. (From J Pharmacol Exp Ther 1997;280(1):416-21) [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
U50488 : A monocarboxylic acid amide obtained by formal condensation between the carboxy group of 3,4-dichlorophenylacetic acid and the secondary amino group of (1R,2R)-N-methyl-2-(pyrrolidin-1-yl)cyclohexanamine [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]
| ID Source | ID |
|---|---|
| PubMed CID | 3036289 |
| CHEMBL ID | 441765 |
| CHEBI ID | 73358 |
| SCHEMBL ID | 332193 |
| MeSH ID | M0369892 |
| Synonym |
|---|
| gtpl1652 |
| LOPAC0_001256 |
| u-50488h |
| u-50,488 |
| u 50488 |
| u 50,488 |
| benzeneacetamide, 3,4-dichloro-n-methyl-n-(2-(1-pyrrolidinyl)cyclohexyl)-, trans- |
| u50488h |
| NCGC00016071-02 |
| lopac-u-111 |
| lopac-u-110 |
| NCGC00016071-01 |
| u50,488 |
| u-50488 |
| 67198-13-4 |
| u50488 |
| trans-3,4-dichloro-n-methyl-n-[2-(1-pyrrolidinyl)cyclohexyl]-benzeneacetamide |
| NCGC00163181-01 |
| 3,4-dichloro-n-methyl-n-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-isomer |
| 2-(3,4-dichlorophenyl)-n-methyl-n-[(1r,2r)-2-pyrrolidin-1-ylcyclohexyl]acetamide |
| bdbm50000296 |
| chembl441765 , |
| 2-(3,4-dichlorophenyl)-n-methyl-n-(2-pyrrolidin-1-ylcyclohexyl)acetamide |
| A843453 |
| 2-(3,4-dichlorophenyl)-n-methyl-n-[(1r,2r)-2-pyrrolidin-1-ylcyclohexyl]ethanamide |
| 2-(3,4-dichlorophenyl)-n-methyl-n-[(1r,2r)-2-(1-pyrrolidinyl)cyclohexyl]acetamide |
| chebi:73358 , |
| unii-39k8jhe8xn |
| um 1382 |
| nih 10533 |
| 39k8jhe8xn , |
| CCG-205330 |
| 2-(3,4-dichlorophenyl)-n-methyl-n-[(1r,2r)-2-(pyrrolidin-1-yl)cyclohexyl]acetamide |
| SCHEMBL332193 |
| DTXSID50849401 |
| rel-3,4-dichloro-n-methyl-n-[(1r,2r)-2-(1-pyrrolidinyl)cyclohexyl]benzeneacetamide |
| trans-3,4-dichloro-n-methyl-n-[2-(1-pyrrolidinyl)-cyclohexyl]-benzeneacetamide |
| trans-(+/-)-3,4-dichloro-n-methyl-n-(2-[1-pyrrolidinyl]cyclohexyl)benzeneacetamide |
| Q7862881 |
| benzeneacetamide, 3,4-dichloro-n-methyl-n-[(1r,2r)-2-(1-pyrrolidinyl)cyclohexyl]- |
| Excerpt | Reference | Relevance |
|---|---|---|
| " In contrast, mu-opioids are highly active as analgesics against a range of nociceptive stimuli, but also concomitantly elicit strongly adverse effects." | ( Antinociceptive and adverse effects of mu- and kappa-opioid receptor agonists: a comparison of morphine and U50488-H. Gallantine, EL; Meert, TF, 2008) | 0.35 |
| " One study compared inhibition of (-)-U-50488 toxicity injected ip at the estimated LD50 into male ICR mice, treated with a potency chord of the same stereoisomer, with control ('isopathic' study)." | ( Isopathic versus enantiomeric inhibition of U-50488 HCl toxicity--experimental studies. Kuzeff, RM; Metcheva, R; Topashka-Ancheva, M, 2009) | 0.89 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " In a search for KOR antagonists that do not accumulate in the brain, we compared single doses of five methylated JDTic analogs (RTI-97, -194, -212, -240, and -241) for reversal of U50,488 diuresis and pharmacokinetic (PK) properties." | ( Pharmacodynamic Relationships between Duration of Action of JDTic-like Kappa-Opioid Receptor Antagonists and Their Brain and Plasma Pharmacokinetics in Rats. Carroll, FI; Fennell, TR; Howard, JL; Owens, SM; Pollard, GT; Snyder, RW, 2016) | 0.43 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " The ability of intrathecally administered clonidine alone or in combination with morphine, DPDPE, or U50,488H to alter thresholds for the production of the visceromotor response was examined." | ( Visceral antinociceptive effects of spinal clonidine combined with morphine, [D-Pen2, D-Pen5] enkephalin, or U50,488H. Collins, JG; Harada, Y; Kishikawa, K; Kitahata, LM; Nishioka, K, 1995) | 0.29 |
| " The STR was mimicked in mice treated with BD 1047 (a putative σ(1) receptor antagonist), but not SM-21, a putative σ(2) receptor antagonist, in combination with METH." | ( Straub tail reaction in mice treated with σ(1) receptor antagonist in combination with methamphetamine. Hall, FS; Kitanaka, J; Kitanaka, N; Nishiyama, N; Takemura, M; Tanaka, K; Uhl, GR, 2012) | 0.38 |
A morphometric study of kainic acid- (KA) induced lesions was designed for the study of the interaction of the diamines U-5449A and U-50488H with excitatory amino acids. Animals treated with U- 50488H on a similar dosing schedule showed significant neuroprotection.
| Excerpt | Relevance | Reference |
|---|---|---|
| "A morphometric study of kainic acid- (KA) induced lesions was designed for the study of the interaction of the diamines U-5449A and U-50488H with excitatory amino acids, and the dose-response relationship thereof." | ( Antagonism of kainic acid lesions in the mouse hippocampus by U-54494A and U-50488H. Aaron, CS; Camacho Ochoa, M; Jackson, TA; Lahti, RA; Strain, GM; Von Voigtlander, PF, 1992) | 0.72 |
| " Animals treated with U-50488H on a similar dosing schedule showed significant neuroprotection at all doses tested, with peak protection observed at 30 mg/kg (51." | ( The kappa opioid-related anticonvulsants U-50488H and U-54494A attenuate N-methyl-D-aspartate induced brain injury in the neonatal rat. Althaus, JS; Hudson, CJ; Means, ED; Scherch, HM; Von Voigtlander, PF, 1991) | 0.86 |
| " On the basis of our dose-response data, we suggest that, in mice, kappa and mu, but not delta, opioid receptors modulate tonic pain perception at both spinal and supraspinal loci." | ( Tonic pain perception in the mouse: differential modulation by three receptor-selective opioid agonists. Cowan, A; Murray, CW, 1991) | 0.28 |
| " A dose-response study demonstrated that the maximum growth hormone release was obtained with 10 micrograms/kg while higher doses were less or not effective." | ( The growth hormone secretory response to fentanyl in rat: an involvement of mu type receptors. Buydens, P; Finné, E; Govaerts, J; Matton, A; Vanhaelst, L, 1990) | 0.28 |
| " In Long-Evans rats, BW942C produced a biphasic dose-response curve for urine output with lower doses increasing and higher doses suppressing output." | ( Kappa opioid partial agonist activity of the enkephalin-like pentapeptide BW942C based on urination and in vitro studies in humans and animals. Cone, EJ; Johnson, RE; Su, TP; Vaupel, DB, 1990) | 0.28 |
| " However, when the dose-response curves for both U50, 488H and DPDPE in the presence of a low-analgesic dose of the other agent were compared with the dose-response curves for the respective agonist administered alone, the curves for the combination regimens were shifted to the left." | ( Kappa- and delta-opioid agonists synergize to produce potent analgesia. Levine, JD; Miaskowski, C; Taiwo, YO, 1990) | 0.28 |
| ") against chemically induced cutaneous pain in rats, was assessed from cumulative dose-response experiments and the formalin test." | ( Analgesia produced by intrathecal administration of the kappa opioid agonist, U-50,488H, on formalin-evoked cutaneous pain in the rat. Hernández, A; Paeile, C; Pelissier, T; Saavedra, H; Soto-Moyano, R, 1990) | 0.28 |
| " In order to investigate the possible actions of peripheral, endogenous kappa agonists, a dose-response curve was generated in the place conditioning paradigm from separate groups of naive rats injected with various intraperitoneal doses of the specific kappa antagonist Mr2266 (0." | ( Kappa receptors mediate the peripheral aversive effects of opiates. Bechara, A; van der Kooy, D, 1987) | 0.27 |
| " After 1 week of treatment and after pump removal, dose-response curves for the induction of antinociception by morphine against noxious heat, pressure and electrical stimulation were shifted to the left across the entire time course of action: this supersensitivity subsided over a period of 1 week postremoval." | ( Antagonist-induced opioid receptor up-regulation. I. Characterization of supersensitivity to selective mu and kappa agonists. Herz, A; Millan, MJ; Morris, BJ, 1988) | 0.27 |
| " Similar blockade was observed for EKC and U 50488 at doses of 10 and/or 20 ng/kg, but DAGO was unable to affect the AS-induced gastric inhibition at any dosage tested (20-200 ng/kg icv)." | ( CNS blockade of acoustic stress-induced gastric motor inhibition by kappa-opiate agonists in dogs. Alvinerie, M; Bueno, L; Gue, M; Honde, C; Junien, JL; Pascaud, X, 1988) | 0.27 |
| " The kappa-selective antagonist, norbinaltorphimine, also failed to shift the dose-response curve to U50488H in this test, despite producing considerable antagonism of the U50488H effect in the rotarod test and of U69593 in both experimental situations." | ( Evidence that the kappa agonist U50488H has non-opioid actions. Birch, PP; Cavicchini, E; Hayes, AG, 1988) | 0.27 |
| " But a number of kappa agonists, including bremazocine, tifluadom, ethylketocyclazocine, ketocyclazocine, U-50,488 and Win 42,610 all depressed contractions, producing parallel dose-response curves." | ( Profile of activity of kappa receptor agonists in the rabbit vas deferens. Hayes, A; Kelly, A, 1985) | 0.27 |
| "Systemic administration of beta-funaltrexamine (beta-FNA) 24 hr before analgesic testing produced approximately a 10-fold parallel shift in the dose-response curves of the prototypic mu agonists morphine, I-methadone, fentanyl and etorphine in the mouse abdominal constriction test." | ( Use of beta-funaltrexamine to determine mu opioid receptor involvement in the analgesic activity of various opioid ligands. Hynes, MD; Leander, JD; Reel, JK; Zimmerman, DM, 1987) | 0.27 |
| " A U-shaped dose-response relationship was observed for the ability of CCK-8-S to attenuate (by approximately 50%, at most) morphine-induced tail flick analgesia." | ( Antagonism of morphine analgesia by CCK-8-S does not extend to all assays nor all opiate analgesics. Barbaz, BS; Hall, NR; Liebman, JM, ) | 0.13 |
| " After 12 generations of selective breeding, the high antinociceptive response line exhibited about 7 times steeper dose-response curve than did the low antinociceptive response line whereas only small differences were seen with saline alone." | ( Selective breeding for levorphanol-induced antinociception on the hot-plate assay: commonalities in mechanism of action with morphine, pentazocine, ethylketocyclazocine, U-50488H and clonidine in mice. Belknap, JK; Danielson, PW; Laursen, SE; Noordewier, B, 1987) | 0.47 |
| " administration of 5 mg/kg morphine, a mu-opioid agonist, or U50488H (U50), a kappa 1-opioid agonist, for 5 days in male CD-1 mice results in a 2-3-fold shift to the right of the respective analgesic (tail flick) dose-response curves, indicating the development of tolerance." | ( The NMDA receptor antagonists, LY274614 and MK-801, and the nitric oxide synthase inhibitor, NG-nitro-L-arginine, attenuate analgesic tolerance to the mu-opioid morphine but not to kappa opioids. Elliott, K; Inturrisi, CE; Kolesnikov, YA; Minami, N; Pasternak, GW, 1994) | 0.29 |
| " Administration of U50,488H (3 mg/kg), in conjunction with several doses of cocaine, did not shift the cocaine dose-response curve." | ( Assessment of the discriminative stimulus effects of cocaine in the rat: lack of interaction with opioids. Broadbent, J; Dworkin, SI; Gaspard, TM, ) | 0.13 |
| " The effect was statistically significant at a dosage of 30 mg/kg, but not at lower doses (0." | ( Potential protection by a specific kappa-opiate agonist U-50488H against membrane failure in acute ischemic brain. Furui, T, 1993) | 0.53 |
| " A single NO2Arg dose retards morphine tolerance for several days, and dosing every 4 days is almost as effective as daily NO2Arg." | ( Blockade of tolerance to morphine but not to kappa opioids by a nitric oxide synthase inhibitor. Ciszewska, G; Kolesnikov, YA; Pasternak, GW; Pick, CG, 1993) | 0.29 |
| " Continuous ICV infusion with butorphanol produced a marked rightward shift of the antinociceptive dose-response curve resulting from U-50,488 challenge." | ( Crosstolerance between butorphanol and morphine in rats. Feng, YZ; Ho, IK; Hoskins, B; Narita, M; Tseng, YT, 1994) | 0.29 |
| " Dose-response curves were generated for both delta 9-THC (i." | ( Interactions between delta 9-tetrahydrocannabinol and kappa opioids in mice. Martin, BR; Smith, PB; Welch, SP, 1994) | 0.29 |
| "1 mg/kg) which does not affect morphine analgesia acutely prevents tolerance following chronic morphine dosing for 10 days." | ( Modulation of opioid analgesia by agmatine. Jain, S; Kolesnikov, Y; Pasternak, GW, 1996) | 0.29 |
| "0 mg/kg) if the dosing interval was 10 min, whereas 30." | ( Opioid antagonist profile of SC nor-binaltorphimine in the formalin paw assay. Grouhel, A; Wettstein, JG, 1996) | 0.29 |
| " Buprenorphine, when injected systemically, revealed a potent analgesic effect by tailflick assay, with a biphasic dose-response curve, which was reversed by naloxone." | ( Pharmacological characterization of buprenorphine, a mixed agonist-antagonist with kappa 3 analgesia. Peter, Y; Pick, CG; Schreiber, S; Weizman, R, 1997) | 0.3 |
| " Pairing Delt II (5 microg) with low (100-200 mg/kg) 2DG doses significantly enhanced intake, producing a leftward (3-fold) shift in 2DG's hyperphagic dose-response curve." | ( Delta and kappa opioid receptor subtypes and ingestion: antagonist and glucoprivic effects. Bodnar, RJ; Ruegg, H; Yu, WZ, 1997) | 0.3 |
| " Self-administration of cocaine (by rats) and morphine (by mice) was readily initiated and showed an inverted U-shaped unit dose-response curve." | ( Kappa-opioid receptor agonist U50,488H modulates cocaine and morphine self-administration in drug-naive rats and mice. Gerrits, MA; Kuzmin, AV; Semenova, S; Van Ree, JM; Zvartau, EE, 1997) | 0.3 |
| " Naloxone (1 microM) or norbinaltorphimine (10 nM) shifted the dose-response curve of (-)-U50,488H to the right by 100-fold." | ( Activation of the cloned human kappa opioid receptor by agonists enhances [35S]GTPgammaS binding to membranes: determination of potencies and efficacies of ligands. Chen, C; Li, JG; Liu-Chen, LY; Luo, LY; Zhu, J, 1997) | 0.3 |
| " Administration of morphine, DPDPE, or U50,488H three times daily for 3 days according to an escalating dosing schedule resulted in analgesic tolerance as indicated by an increase in analgesic ED50 values using the tail-flick test in mice." | ( The competitive alpha-amino-3-hydroxy-5-methylisoxazole-4-propionate receptor antagonist LY293558 attenuates and reverses analgesic tolerance to morphine but not to delta or kappa opioids. Inturrisi, CE; Kao, B; Kest, B; McLemore, G, 1997) | 0.3 |
| " Similarly, the progressive and complete loss of analgesia in CD-1 mice seen with repeated dosing of the delta ligand [D-Pen2, D-Pen5]enkephalin is not observed in 129/SvEv mice." | ( Lack of morphine and enkephalin tolerance in 129/SvEv mice: evidence for a NMDA receptor defect. Jain, S; Kolesnikov, Y; Pasternak, GW; Wilson, R, 1998) | 0.3 |
| " In dose-response tests, subjects rarely responded on the U-50,488H-appropriate key when morphine was administered or on the morphine-appropriate key when they received U-50,488H." | ( Establishing morphine and U-50,488H as discriminative stimuli in a three-choice assay with pigeons. Makhay, MM; Poling, A; Young, AM, 1998) | 0.3 |
| " Slopes for dose-response curves were determined." | ( Effects of nalbuphine, pentazocine and U50488H on gastric emptying and gastrointestinal transit in the rat. Asai, T; Mapleson, WW; Power, I, 1998) | 0.3 |
| " Diazoxide (2 microg/mouse) shifted morphine's dose-response curve 47-fold, while levcromakalim (0." | ( ATP-gated K(+) channel openers enhance opioid antinociception: indirect evidence for the release of endogenous opioid peptides. Lohmann, AB; Welch, SP, 1999) | 0.3 |
| " In the first study, U50,488H was administered in a cumulative dosing procedure (5." | ( Long-term voluntary access to running wheels decreases kappa-opioid antinociception. D'Anci, KE; Gerstein, AV; Kanarek, RB, 2000) | 0.31 |
| " Subjects were then tested for tolerance in the distinctive context using the tail-flick procedure and dose-response curve methodology." | ( Associative and non-associative fentanyl tolerance in the rat: evaluation of cross tolerance with mu-and kappa-specific opioids. Carter, BL; Conklin, CA; Tiffany, ST, 2000) | 0.31 |
| " The Ca(2+) response occurred in all-or-none fashion and the half-maximal dosage of U50488H (812." | ( Cyclic AMP regulates the calcium transients released from IP(3)-sensitive stores by activation of rat kappa-opioid receptors expressed in CHO cells. Allen, CN; Grandy, DK; Ikeda, M; Nelson, CS; Shinagawa, H; Shinoe, T; Sugiyama, T; Yoshioka, T, 2001) | 0.31 |
| " Reflex contraction of the rectus abdominis in response to distension was recorded before and after cumulative dosing with the mu-opioid agonist morphine and the kappa-opioid agonist (-)U50488." | ( Estrogen reduces efficacy of mu- but Not kappa-opioid agonist inhibition in response to uterine cervical distension. Eisenach, JC; Sandner-Kiesling, A, 2002) | 0.31 |
| " The dose-response curve to U50-induced analgesia in U50-tolerant mice was shifted rightward (2." | ( Ginseng total saponin potentiates acute U-50,488H-induced analgesia and inhibits tolerance to U-50,488H-induced analgesia in mice. Nemmani, KV; Ramarao, P, 2002) | 0.31 |
| " Using a mouse hot-plate test, dose-response relationships were first determined for all compounds individually and then for opioids co-administered with fixed doses of ketamine or dextromethorphan." | ( Dextromethorphan and ketamine potentiate the antinociceptive effects of mu- but not delta- or kappa-opioid agonists in a mouse model of acute pain. Baker, AK; Hoffmann, VL; Meert, TF, 2002) | 0.31 |
| " Using a mouse hot-plate test, dose-response relationships were first determined for all compounds individually and then for opioids co-administered with fixed doses of clonidine, ketamine or dextromethorphan." | ( Interactions of NMDA antagonists and an alpha 2 agonist with mu, delta and kappa opioids in an acute nociception assay. Baker, AK; Hoffmann, VL; Meert, TF, 2002) | 0.31 |
| " However, heroin, but not SNC-80 or U50488, significantly shifted the dose-response curve for THC discrimination to the left." | ( Involvement of mu-, delta- and kappa-opioid receptor subtypes in the discriminative-stimulus effects of delta-9-tetrahydrocannabinol (THC) in rats. Goldberg, SR; Solinas, M, 2005) | 0.33 |
| " A separate group of animals was used to investigate the dose-response effect on this motor dysfunction." | ( Mu and delta, but not kappa, opioid agonists induce spastic paraparesis after a short period of spinal cord ischaemia in rats. Davison, KJ; Fuchigami, T; Kakinohana, M; Marsala, M; Nakamura, S; Sugahara, K, 2006) | 0.33 |
| " A dose-response was constructed by administering the delta-receptor opioid methionine-enkephalin-arginine-phenylalanine (MEAP) by microdialysis into the interstitium of the canine sinoatrial node during vagal and sympathetic stimulation." | ( Vagotonic effects of enkephalin are not mediated by sympatholytic mechanisms. Barlow, MA; Caffrey, JL; Deo, S; Johnson, S, 2006) | 0.33 |
| " None of the drugs affected the residual volume, micturition threshold pressure or bladder contraction pressure at any dosage examined." | ( Effects of opioid subtypes on detrusor overactivity in rats with cerebral infarction. Ishiura, Y; Komatsu, K; Nagasaka, Y; Nakamura, Y; Namiki, M; Yokoyama, O, 2007) | 0.34 |
| " Subclinical MOR activation (10 nM DAMGO) produced a leftward shift in (D-Ala2)-Deltorphin II dose-response curve in non-ligated rats (IC50 16." | ( Depression of C fibre-evoked spinal field potentials by the spinal delta opioid receptor is enhanced in the spinal nerve ligation model of neuropathic pain: involvement of the mu-subtype. Aguilera, L; Aira, Z; Azkue, JJ; Bilbao, J; Buesa, I; Mozas, M; Salgueiro, M; Urrutia, A; Zimmermann, M, 2008) | 0.35 |
| " Dose-response curves were generally quantal under the FR and graded under the FI schedules, but highly variable among subjects under the FI." | ( Drug discrimination in pigeons trained to discriminate among morphine, U50488, a combination of these drugs, and saline. Li, M; McMillan, DE; Wessinger, WD, 2011) | 0.37 |
| " To test this hypothesis, separate cohorts of male Wistar rats were trained in one of the two animal models of impulsivity: delay-discounting (DD) or stop-signal reaction time (SSRT) tasks, and once stable responding was observed, received intracerebroventricular (ICV) infusions of the KOR agonist U50,488 (0-50 μg) according to a within-subject dosing regimen." | ( Dissociable effects of kappa-opioid receptor activation on impulsive phenotypes in wistar rats. Kissler, JL; Walker, BM, 2013) | 0.39 |
| " We have previously shown that the antinociception dose-response curve for peripherally restricted doses of the KOR agonist (-)-(trans)-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl]benzeneacetamide (U50488) has an inverted U shape." | ( Functional selectivity of kappa opioid receptor agonists in peripheral sensory neurons. Berg, KA; Chavera, TA; Clarke, WP; Jacobs, BA; Jamshidi, RJ; Prisinzano, TE; Saylor, RM; Sullivan, LC, 2015) | 0.42 |
| Role | Description |
|---|---|
| kappa-opioid receptor agonist | A compound that exhibits agonist activity at the kappa-opioid receptor. |
| diuretic | An agent that promotes the excretion of urine through its effects on kidney function. |
| analgesic | An agent capable of relieving pain without the loss of consciousness or without producing anaesthesia. In addition, analgesic is a role played by a compound which is exhibited by a capability to cause a reduction of pain symptoms. |
| antitussive | An agent that suppresses cough. Antitussives have a central or a peripheral action on the cough reflex, or a combination of both. Compare with expectorants, which are considered to increase the volume of secretions in the respiratory tract, so facilitating their removal by ciliary action and coughing, and mucolytics, which decrease the viscosity of mucus, facilitating its removal by ciliary action and expectoration. |
| calcium channel blocker | One of a class of drugs that acts by selective inhibition of calcium influx through cell membranes or on the release and binding of calcium in intracellular pools. |
| [role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Class | Description |
|---|---|
| N-alkylpyrrolidine | |
| monocarboxylic acid amide | A carboxamide derived from a monocarboxylic acid. |
| dichlorobenzene | Any member of the class of chlorobenzenes carrying two chloro groups at unspecified positions. |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| TDP1 protein | Homo sapiens (human) | Potency | 29.0929 | 0.0008 | 11.3822 | 44.6684 | AID686979 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 10.8573 | 0.0013 | 18.0743 | 39.8107 | AID926; AID938 |
| 67.9K protein | Vaccinia virus | Potency | 8.9125 | 0.0001 | 8.4406 | 100.0000 | AID720579 |
| cytochrome P450 2D6 isoform 1 | Homo sapiens (human) | Potency | 2.6200 | 0.0020 | 7.5337 | 39.8107 | AID891 |
| cellular tumor antigen p53 isoform a | Homo sapiens (human) | Potency | 16.1862 | 0.3162 | 12.4435 | 31.6228 | AID902; AID924 |
| cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 5.0119 | 0.0316 | 10.2792 | 39.8107 | AID884; AID885 |
| muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 0.0010 | 6.0009 | 35.4813 | AID943; AID944 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Integrin beta-3 | Homo sapiens (human) | Potency | 12.5893 | 0.3162 | 11.4157 | 31.6228 | AID924 |
| Integrin alpha-IIb | Homo sapiens (human) | Potency | 12.5893 | 0.3162 | 11.4157 | 31.6228 | AID924 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Inositol monophosphatase 1 | Rattus norvegicus (Norway rat) | Potency | 5.6113 | 1.0000 | 10.4756 | 28.1838 | AID1457; AID901 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Aldo-keto reductase family 1 member B1 | Rattus norvegicus (Norway rat) | Ki | 0.2900 | 0.0032 | 2.2887 | 9.3160 | AID709667 |
| Delta-type opioid receptor | Mus musculus (house mouse) | Ki | 3.2500 | 0.0000 | 0.5393 | 9.4000 | AID1188907; AID149188; AID321652; AID369071 |
| Delta-type opioid receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 8.7167 | 0.0003 | 0.3887 | 7.0000 | AID149041; AID150392 |
| Delta-type opioid receptor | Rattus norvegicus (Norway rat) | Ki | 5.0000 | 0.0000 | 0.6068 | 9.2330 | AID514360 |
| Kappa-type opioid receptor | Mus musculus (house mouse) | IC50 (µMol) | 0.0027 | 0.0013 | 1.5380 | 10.0000 | AID148304; AID1755978 |
| Kappa-type opioid receptor | Mus musculus (house mouse) | Ki | 0.0081 | 0.0003 | 0.3594 | 2.7500 | AID1773094 |
| Mu-type opioid receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 8.7167 | 0.0001 | 0.8874 | 10.0000 | AID149041; AID150392 |
| Mu-type opioid receptor | Rattus norvegicus (Norway rat) | Ki | 1.6012 | 0.0000 | 0.3845 | 8.6000 | AID224586; AID321651; AID369070; AID514359 |
| Kappa-type opioid receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 5.2303 | 0.0005 | 0.3698 | 7.0000 | AID1285646; AID1433979; AID149041; AID150392 |
| Kappa-type opioid receptor | Rattus norvegicus (Norway rat) | Ki | 0.0005 | 0.0000 | 0.1868 | 3.9500 | AID1433979; AID1630711 |
| Mu-type opioid receptor | Homo sapiens (human) | Ki | 0.2900 | 0.0000 | 0.4197 | 10.0000 | AID709667 |
| Delta-type opioid receptor | Homo sapiens (human) | Ki | 6.5800 | 0.0000 | 0.5978 | 9.9300 | AID147910; AID149188; AID149189; AID149194; AID709666 |
| Kappa-type opioid receptor | Cavia porcellus (domestic guinea pig) | IC50 (µMol) | 0.0958 | 0.0003 | 0.7123 | 7.0700 | AID147956; AID147959 |
| Kappa-type opioid receptor | Cavia porcellus (domestic guinea pig) | Ki | 0.0191 | 0.0000 | 0.2018 | 6.4240 | AID147976; AID147981; AID147982; AID148262; AID149128; AID149129; AID149130; AID149131; AID149844; AID1877935; AID1901076; AID223595; AID514361 |
| Kappa-type opioid receptor | Homo sapiens (human) | IC50 (µMol) | 0.0537 | 0.0000 | 1.2011 | 10.0000 | AID1186507; AID1336343; AID1355423; AID1425958; AID1458124; AID147856; AID148434; AID223600; AID340258; AID346441; AID450521; AID751865; AID752228 |
| Kappa-type opioid receptor | Homo sapiens (human) | Ki | 0.0083 | 0.0000 | 0.3624 | 10.0000 | AID1185267; AID1303901; AID1355420; AID1581726; AID1604693; AID1630479; AID1633369; AID1655379; AID1689585; AID1755975; AID1861728; AID239298; AID254480; AID270608; AID276331; AID321650; AID346441; AID369067; AID481097; AID488649; AID516776; AID640425; AID707252; AID709669; AID751865 |
| Mu-type opioid receptor | Mus musculus (house mouse) | Ki | 0.5050 | 0.0000 | 0.1228 | 1.3000 | AID1188906; AID149131; AID151152 |
| Mu-type opioid receptor | Cavia porcellus (domestic guinea pig) | Ki | 0.5226 | 0.0000 | 0.2786 | 9.0000 | AID147910; AID149008; AID149009; AID149014; AID149017; AID149131 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Kappa-type opioid receptor | Mus musculus (house mouse) | EC50 (µMol) | 1.6365 | 0.0008 | 0.8056 | 4.8860 | AID1773102; AID1773118; AID776681 |
| Mu-type opioid receptor | Homo sapiens (human) | EC50 (µMol) | 4.8400 | 0.0000 | 0.3263 | 9.4000 | AID329904 |
| Kappa-type opioid receptor | Homo sapiens (human) | EC50 (µMol) | 0.0416 | 0.0000 | 0.2244 | 8.9900 | AID1299242; AID1398500; AID149991; AID149994; AID1528099; AID1604703; AID1633373; AID1655385; AID1689596; AID1755981; AID240367; AID255651; AID270239; AID270609; AID276332; AID286308; AID290262; AID296058; AID310357; AID321653; AID329906; AID369068; AID385261; AID392477; AID410731; AID417160; AID516775; AID640424; AID670123; AID709664; AID719290; AID739874 |
| Mitogen-activated protein kinase 8 | Homo sapiens (human) | EC50 (µMol) | 1.2400 | 0.0100 | 0.3738 | 1.2400 | AID381427 |
| Mitogen-activated protein kinase 9 | Homo sapiens (human) | EC50 (µMol) | 1.2400 | 0.0100 | 0.3738 | 1.2400 | AID381427 |
| Mitogen-activated protein kinase 10 | Homo sapiens (human) | EC50 (µMol) | 1.2400 | 0.0870 | 0.4950 | 1.2400 | AID381427 |
| Mu-type opioid receptor | Cavia porcellus (domestic guinea pig) | EC50 (µMol) | 0.0460 | 0.0000 | 0.0493 | 0.9320 | AID149994 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Delta-type opioid receptor | Mus musculus (house mouse) | Ke | 0.0412 | 0.0001 | 0.1472 | 6.1080 | AID389661 |
| Delta-type opioid receptor | Rattus norvegicus (Norway rat) | Activity | 25.0000 | 0.0000 | 0.1193 | 1.2200 | AID149372 |
| Kappa-type opioid receptor | Mus musculus (house mouse) | Ke | 0.0078 | 0.0000 | 0.3225 | 1.5510 | AID224414; AID389675 |
| Kappa-type opioid receptor | Homo sapiens (human) | ED50 | 0.0270 | 0.0007 | 1.4569 | 8.9400 | AID1197359 |
| Mu-type opioid receptor | Mus musculus (house mouse) | Ke | 0.0315 | 0.0002 | 0.0233 | 0.0554 | AID389660 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1755978 | Agonist activity at mouse FLAG-tagged kappa opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP production preincubated for 20 mins followed by forskolin stimulation and measured after 15 mins by Glo-sensor reagent b | 2021 | Journal of natural products, 01-22, Volume: 84, Issue:1 | Isolation and Pharmacological Characterization of Six Opioidergic |
| AID149286 | Compound was evaluated for binding affinity towards kappa opioid receptor using [3H](-)-U-69,593 in guinea pig ileum | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8 | Alterations in the stereochemistry of the kappa-selective opioid agonist U50,488 result in high-affinity sigma ligands. |
| AID1528099 | Agonist activity at human KOR expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting | |||
| AID1689596 | Agonist activity at human kappa opioid receptor expressed in CHO cells incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting method | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Discovery of 3-((dimethylamino)methyl)-4-hydroxy-4-(3-methoxyphenyl)-N-phenylpiperidine-1-carboxamide as novel potent analgesic. |
| AID385262 | Activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding relative to basal level | 2008 | Bioorganic & medicinal chemistry, May-15, Volume: 16, Issue:10 | Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 6: Opioid receptor binding properties of cyclic variants of 8-carboxamidocyclazocine. |
| AID739874 | Agonist activity at human kappa opioid receptor expressed in CHO cell membrane assessed as stimulation of [35S]GTPgammaS binding after 60 mins by liquid scintillation counting | 2013 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 23, Issue:7 | Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 9: Synthesis, characterization and molecular modeling of pyridinyl isosteres of N-BPE-8-CAC (1), a high affinity ligand for opioid receptors. |
| AID185358 | Dose required to produce 50% of the maximum possible analgesic effect evaluated through rat paw pressure assay with the compound being administered through intravenous route; Not tested | 1991 | Journal of medicinal chemistry, Jan, Volume: 34, Issue:1 | Highly selective kappa opioid analgesics. 4. Synthesis of some conformationally restricted naphthalene derivatives with high receptor affinity and selectivity. |
| AID640395 | Agonist activity at human KOPR expressed in U2OS cells assessed as beta-arrestin2 recruitment after 90 mins by DiscoveRx PathHunter assay | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2 | Differential signaling properties at the kappa opioid receptor of 12-epi-salvinorin A and its analogues. |
| AID1197359 | Agonist activity against human recombinant opioid kappa receptor expressed in CHO cell membranes after 3 hrs by [35S]GTP-gamma-S binding assay | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Probes for narcotic receptor mediated phenomena 49. N-substituted rac-cis-4a-arylalkyl-1,2,3,4,4a,9a-hexahydrobenzofuro[2,3-c]pyridin-6-ols. |
| AID135536 | Molar potency ratio relative to the standard agonist EKC on field-stimulated mouse vas deferens | 1991 | Journal of medicinal chemistry, Jan, Volume: 34, Issue:1 | 2-(3,4-Dichlorophenyl)-N-methyl-N-[2-(1-pyrrolidinyl)-1-substituted- ethyl]-acetamides: the use of conformational analysis in the development of a novel series of potent opioid kappa agonists. |
| AID410731 | Activity at human cloned kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay | 2009 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 19, Issue:1 | Syntheses and opioid receptor binding properties of carboxamido-substituted opioids. |
| AID1689594 | Agonist activity at rat mu opioid receptor expressed in CHO cells incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting method | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Discovery of 3-((dimethylamino)methyl)-4-hydroxy-4-(3-methoxyphenyl)-N-phenylpiperidine-1-carboxamide as novel potent analgesic. |
| AID149904 | Binding affinity towards Opioid receptor delta 1 in guinea pig brain membranes using [3H]naltrindole as radioligand | 2001 | Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20 | Mixed kappa agonists and mu agonists/antagonists as potential pharmacotherapeutics for cocaine abuse: synthesis and opioid receptor binding affinity of N-substituted derivatives of morphinan. |
| AID1901076 | Displacement of [3H]-U69593 from KOR in guinea pig brain membranes measured by competitive radioligand receptor binding assay | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Synthesis of 8-aminomorphans with high KOR affinity. |
| AID134208 | Antagonist Ke values of approximately 15 nM which are indicative of k receptor antagonism on field-stimulated mouse vas deferens. | 1991 | Journal of medicinal chemistry, Jan, Volume: 34, Issue:1 | 2-(3,4-Dichlorophenyl)-N-methyl-N-[2-(1-pyrrolidinyl)-1-substituted- ethyl]-acetamides: the use of conformational analysis in the development of a novel series of potent opioid kappa agonists. |
| AID1755981 | Agonist activity at human kappa opioid receptor expressed in U2OS cells assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assay | 2021 | Journal of natural products, 01-22, Volume: 84, Issue:1 | Isolation and Pharmacological Characterization of Six Opioidergic |
| AID1528105 | Antinociceptive activity in ip dosed Kunming mouse assessed as reduction in nociceptive response after 2 hrs by hot plate test | |||
| AID148034 | Binding affinity towards Opioid receptor mu 1 by displacing the radioligand [3H]DAMGO from guinea pig brain membrane | 2000 | Journal of medicinal chemistry, Jan-13, Volume: 43, Issue:1 | Synthesis and opioid receptor affinity of morphinan and benzomorphan derivatives: mixed kappa agonists and mu agonists/antagonists as potential pharmacotherapeutics for cocaine dependence. |
| AID1630712 | Displacement of [3H]DPDPE from human DOR expressed in CHO cells | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21 | An LP1 analogue, selective MOR agonist with a peculiar pharmacological profile, used to scrutiny the ligand binding domain. |
| AID389655 | Antinociceptive activity in po dosed mouse by tail flick test | 2008 | Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20 | Design, synthesis, and structure-activity relationship of novel opioid kappa-agonists. |
| AID165733 | Percent change of volume in the respiratory activity was measured in rabbit at 0.1 mg/kg dose given intravenously | 1989 | Journal of medicinal chemistry, Feb, Volume: 32, Issue:2 | Synthesis and biological evaluation of 14-alkoxymorphinans. 2. (-)-N-(cyclopropylmethyl)-4,14-dimethoxymorphinan-6-one, a selective mu opioid receptor antagonist. |
| AID148036 | Binding affinity towards Opioid receptor mu 1 in guinea pig brain membranes using [3H]DAMGO as radioligand | 2001 | Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20 | Mixed kappa agonists and mu agonists/antagonists as potential pharmacotherapeutics for cocaine abuse: synthesis and opioid receptor binding affinity of N-substituted derivatives of morphinan. |
| AID151152 | Binding affinity against Opioid receptor mu 1 using [3H]etorphine as a radioligand | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6 | Naphtho and benzo analogues of the kappa opioid agonist trans-(+/-)-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl] benzeneacetamide. |
| AID1604693 | Displacement of [3H]-diprenorphine from human KOR expressed in CHO cell membranes incubated for 1 hr by scintillation counting method | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5 | Potent, Efficacious, and Stable Cyclic Opioid Peptides with Long Lasting Antinociceptive Effect after Peripheral Administration. |
| AID239298 | Inhibition of [3H]diprenorphine binding to human Opioid receptor kappa 1 expressed in chinese hamster ovary cells | 2005 | Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11 | Synthesis and in vitro pharmacological evaluation of salvinorin A analogues modified at C(2). |
| AID1233270 | Ratio of ED50 for antinociceptive effect in C57BL/6 mouse by 55 degC Warm water tail withdrawal assay to ED50 for analgesic activity in C57BL/6 mouse by acetic acid writhing assay | 2015 | Journal of medicinal chemistry, Jun-25, Volume: 58, Issue:12 | Parallel Synthesis of Hexahydrodiimidazodiazepines Heterocyclic Peptidomimetics and Their in Vitro and in Vivo Activities at μ (MOR), δ (DOR), and κ (KOR) Opioid Receptors. |
| AID1233290 | Antinociceptive effect in icv dosed C57BL/6 mouse assessed as tail withdrawal latency measured up to 2 hrs by 55 degC Warm water tail withdrawal assay | 2015 | Journal of medicinal chemistry, Jun-25, Volume: 58, Issue:12 | Parallel Synthesis of Hexahydrodiimidazodiazepines Heterocyclic Peptidomimetics and Their in Vitro and in Vivo Activities at μ (MOR), δ (DOR), and κ (KOR) Opioid Receptors. |
| AID221724 | Antinociceptive activity determined in vivo in tail flick assay in male Swiss mice with saline | 1993 | Journal of medicinal chemistry, Jun-25, Volume: 36, Issue:13 | Non-peptide ligands for opioid receptors. Design of kappa-specific agonists. |
| AID232473 | Selectivity ratio for affinities determined by using [3H]BREM and [3H]-(+)-3-PPP in guinea pig ileum | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8 | Alterations in the stereochemistry of the kappa-selective opioid agonist U50,488 result in high-affinity sigma ligands. |
| AID670123 | Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [33S]GTPgammaS binding after 60 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8 | Synthesis, binding affinity, and functional in vitro activity of 3-benzylaminomorphinan and 3-benzylaminomorphine ligands at opioid receptors. |
| AID369067 | Displacement of [3H]diprenorphine from human KOPR expressed in CHO cells | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3 | Modification of the furan ring of salvinorin A: identification of a selective partial agonist at the kappa opioid receptor. |
| AID229800 | Ratio of Ki at mu-opioid receptor to Ki at kappa oioid receptor | 1988 | Journal of medicinal chemistry, Apr, Volume: 31, Issue:4 | Highly selective kappa opioid analgesics. Synthesis and structure-activity relationships of novel N-[(2-aminocyclohexyl)aryl]acetamide and N-[(2-aminocyclohexyl)aryloxy]acetamide derivatives. |
| AID1633369 | Displacement of [3H]-diprenorphine from human kappa opioid receptor expressed in CHO cell membranes incubated for 1 hr by micro beta2 scintillation counting method | 2019 | ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4 | Novel Cyclic Biphalin Analogues by Ruthenium-Catalyzed Ring Closing Metathesis: |
| AID381427 | Increase of JNK phosphorylation in U50488 treated HEK293 cells expressing GFP tagged kappa opioid receptor | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41 | Long-acting kappa opioid antagonists disrupt receptor signaling and produce noncompetitive effects by activating c-Jun N-terminal kinase. |
| AID295930 | Displacement of [3H]U-69593 from kappa opioid receptor in guinea pig brain membrane | 2007 | European journal of medicinal chemistry, Oct, Volume: 42, Issue:10 | Synthesis of bridged piperazines with sigma receptor affinity. |
| AID1655385 | Agonist activity at human KOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 | Developing Cyclic Opioid Analogues: Fluorescently Labeled Bioconjugates of Biphalin. |
| AID392476 | Antagonist activity at human kappa opioid receptor expressed in CHO cells assessed as inhibition of U50,488-induced [35S]GTPgammaS binding | 2009 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2 | Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 7: syntheses and opioid receptor properties of cyclic variants of cyclazocine. |
| AID254480 | Binding affinity for 1 uM [3H]diprenorphine against human Opioid receptor kappa expressed in chinese hamster ovary cells (CHO cells) | 2005 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 15, Issue:19 | Synthesis and in vitro pharmacological studies of C(4) modified salvinorin A analogues. |
| AID389660 | Equilibrium constant, ratio of IC50 for mu opioid receptor in ddy mouse vas deferens in presence of 100 nM naloxone to IC50 for mu opioid receptor in ddy mouse vas deferens | 2008 | Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20 | Design, synthesis, and structure-activity relationship of novel opioid kappa-agonists. |
| AID392475 | Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding relative to basal [35S]GTPgammaS binding | 2009 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2 | Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 7: syntheses and opioid receptor properties of cyclic variants of cyclazocine. |
| AID148884 | Irreversible inhibition of [3H][3H]ethylketocyclazocine binding to mu opioid receptors of guinea pig brain membranes on pre-incubation with 10E-6 M of the compound. | 1992 | Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12 | Selective reversible and irreversible ligands for the kappa opioid receptor. |
| AID228935 | Tested for maximum agonist response at concentration 10 uM, relative to that obtained with standard agonist U50,488. | 2000 | Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14 | [Pro(3)]Dyn A(1-11)-NH(2): a dynorphin analogue with high selectivity for the kappa opioid receptor. |
| AID709664 | Agonist activity at human kappa opioid receptor expressed in CHO cell membranes incubated for 60 mins by [35S]GTPgammaS binding assay | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 | Discovery and pharmacological evaluation of a diphenethylamine derivative (HS665), a highly potent and selective κ opioid receptor agonist. |
| AID1398501 | Agonist activity at human KOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding based liquid scintillation counting analysis relative to control | 2018 | Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14 | 7β-Methyl substituent is a structural locus associated with activity cliff for nepenthone analogues. |
| AID149367 | Evaluation for the ability of delta opioid to protect the [3H]-DAMGO binding site from alkylation | 1994 | Journal of medicinal chemistry, May-27, Volume: 37, Issue:11 | 14 alpha,14' beta-[Dithiobis[(2-oxo-2,1-ethanediyl)imino]]bis (7,8-dihydromorphinone) and 14 alpha,14' beta-[dithiobis[(2-oxo-2,1- ethanediyl)imino]]bis[7,8-dihydro-N-(cyclopropylmethyl)normorphinone]: chemistry and opioid binding properties. |
| AID149285 | Compound was evaluated for binding affinity towards Opioid receptor kappa 1 using [3H]BREM in guinea pig ileum | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8 | Alterations in the stereochemistry of the kappa-selective opioid agonist U50,488 result in high-affinity sigma ligands. |
| AID1721998 | Analgesic activity in mouse assessed as increase in wheel running activity | 2020 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 30, Issue:17 | Discovery of attenuation effect of orexin 1 receptor to aversion of nalfurafine: Synthesis and evaluation of D-nor-nalfurafine derivatives and analyses of the three active conformations of nalfurafine. |
| AID276331 | Displacement of [3H]diprenorphine binding from human kappa opioid receptor expressed in CHO cells | 2006 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21 | Synthesis and in vitro pharmacological studies of new C(4)-modified salvinorin A analogues. |
| AID340258 | Inhibition of human kappa opioid receptor | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14 | Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity. |
| AID1722002 | Toxicity in mouse assessed as increase in conditioned place aversion at 1 to 4 mg/kg, sc | 2020 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 30, Issue:17 | Discovery of attenuation effect of orexin 1 receptor to aversion of nalfurafine: Synthesis and evaluation of D-nor-nalfurafine derivatives and analyses of the three active conformations of nalfurafine. |
| AID757453 | Neurotoxicity in C57BL/6J mouse assessed as sedative effect at 10 mg/kg, ip after 60 mins by rotarod test | 2013 | Journal of natural products, Mar-22, Volume: 76, Issue:3 | The macrocyclic peptide natural product CJ-15,208 is orally active and prevents reinstatement of extinguished cocaine-seeking behavior. |
| AID251605 | Ratio of effective dose of compound producing agonistic activity in presence and absence of benzylidenenaltrexone (25 pmol) upon intrathecal administration in mouse tail flick assay | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | A bivalent ligand (KDAN-18) containing delta-antagonist and kappa-agonist pharmacophores bridges delta2 and kappa1 opioid receptor phenotypes. |
| AID389661 | Equilibrium constant, ratio of IC50 for delta opioid receptor in ddy mouse vas deferens in presence of 10 nM Naltrindole to IC50 for delta opioid receptor in ddy mouse vas deferens | 2008 | Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20 | Design, synthesis, and structure-activity relationship of novel opioid kappa-agonists. |
| AID235718 | Selectivity Ratio is the ratio of opioid receptor kappa (Ki(nM)) to the opioid receptor mu (Ki(nM)) | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16 | Substituted 1-(aminomethyl)-2-(arylacetyl)-1,2,3,4-tetrahydroisoquinolines: a novel class of very potent antinociceptive agents with varying degrees of selectivity for kappa and mu opioid receptors. |
| AID640394 | Agonist activity at human KOPR expressed in U2OS cells assessed as beta-arrestin2 recruitment after 90 mins by DiscoveRx PathHunter assay relative to salvA | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2 | Differential signaling properties at the kappa opioid receptor of 12-epi-salvinorin A and its analogues. |
| AID149019 | Tested for inhibitory effect on binding of [3H]DAMGO to opioid receptor mu in guinea pig cerebellum membranes | 1992 | Journal of medicinal chemistry, Nov-27, Volume: 35, Issue:24 | N-terminal alkylated derivatives of [D-Pro10]dynorphin A-(1-11) are highly selective for kappa-opioid receptors. |
| AID149902 | Binding affinity towards Opioid receptor delta 1 by displacing the radioligand [3H]naltrindole from guinea pig brain membrane | 2000 | Journal of medicinal chemistry, Jan-13, Volume: 43, Issue:1 | Synthesis and opioid receptor affinity of morphinan and benzomorphan derivatives: mixed kappa agonists and mu agonists/antagonists as potential pharmacotherapeutics for cocaine dependence. |
| AID132775 | In vivo antinociceptive activity in mouse tail flick test following p.o. administration. | 1991 | Journal of medicinal chemistry, Aug, Volume: 34, Issue:8 | (1S)-1-(aminomethyl)-2-(arylacetyl)-1,2,3,4-tetrahydroisoquinoline and heterocycle-condensed tetrahydropyridine derivatives: members of a novel class of very potent kappa opioid analgesics. |
| AID1604703 | Agonist activity at human KOR expressed in CHO cell membranes incubated for 1 hr by [35S]-GTPgammaS coupling assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5 | Potent, Efficacious, and Stable Cyclic Opioid Peptides with Long Lasting Antinociceptive Effect after Peripheral Administration. |
| AID1303902 | Antinociceptive activity in ip dosed mouse assessed as acetic acid induced writhing administered 30 mins prior to acetic acid challenge measured for 20 mins | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13 | Design, synthesis and biological evaluation of novel tetrahydroisoquinoline quaternary derivatives as peripheral κ-opioid receptor agonists. |
| AID286307 | Agonist activity at human opioid kappa receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S binding | 2007 | Journal of medicinal chemistry, May-03, Volume: 50, Issue:9 | Pharmacological properties of bivalent ligands containing butorphan linked to nalbuphine, naltrexone, and naloxone at mu, delta, and kappa opioid receptors. |
| AID149179 | Irreversible inhibition of [3H]-DADLE binding to delta opioid receptors of guinea pig brain membranes on preincubation with 10E-4 M of the compound. | 1992 | Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12 | Selective reversible and irreversible ligands for the kappa opioid receptor. |
| AID321653 | Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3 | Standard protecting groups create potent and selective kappa opioids: salvinorin B alkoxymethyl ethers. |
| AID1336343 | Displacement of [3H]U 69593 from human recombinant kappa-opioid receptor expressed in CHO cells measured after 60 mins by scintillation counting method | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2 | Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH |
| AID1755975 | Displacement of [3H]-U69593 from human kappa opioid receptor expressed in U2OS cells by radioligand binding assay | 2021 | Journal of natural products, 01-22, Volume: 84, Issue:1 | Isolation and Pharmacological Characterization of Six Opioidergic |
| AID392477 | Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding | 2009 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2 | Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 7: syntheses and opioid receptor properties of cyclic variants of cyclazocine. |
| AID149194 | Receptor binding affinity towards opioid receptor delta | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16 | Substituted 1-(aminomethyl)-2-(arylacetyl)-1,2,3,4-tetrahydroisoquinolines: a novel class of very potent antinociceptive agents with varying degrees of selectivity for kappa and mu opioid receptors. |
| AID221723 | Antinociceptive activity determined in vivo in tail flick assay in male Swiss mice with 2.0 mg/kg Naloxone | 1993 | Journal of medicinal chemistry, Jun-25, Volume: 36, Issue:13 | Non-peptide ligands for opioid receptors. Design of kappa-specific agonists. |
| AID1458133 | Analgesic activity in C57BL/6J mouse assessed as tail withdrawal latency at 5 mg/kg measured after 30 mins in presence of KOR antagonist norBNI by tail flick test | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15 | Opioid Receptor Modulators with a Cinnamyl Group. |
| AID1185267 | Displacement of [3H]U69593 from human kappa opioid receptor expressed in HEK293 cells by scintillation counting | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | Synthesis of tripeptides containing D-Trp substituted at the indole ring, assessment of opioid receptor binding and in vivo central antinociception. |
| AID346441 | Displacement of radiolabeled U50488 from human kappa-type opioid receptor | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia. |
| AID130114 | Antinociceptive activity in mouse tail flick test following s.c. administration. | 1991 | Journal of medicinal chemistry, Jan, Volume: 34, Issue:1 | (2S)-1-(arylacetyl)-2-(aminomethyl)piperidine derivatives: novel, highly selective kappa opioid analgesics. |
| AID233907 | Selectivity, ratio of affinity towards delta to kappa opioid receptor | 2000 | Journal of medicinal chemistry, Aug-10, Volume: 43, Issue:16 | Nonpeptide analogues of dynorphin A(1-8): design, synthesis, and pharmacological evaluation of kappa-selective agonists. |
| AID383161 | Displacement of [3H]DAMGO from mu opioid receptor in ICR mouse whole brain | 2008 | Bioorganic & medicinal chemistry, Apr-15, Volume: 16, Issue:8 | Syntheses of 4,6'-epoxymorphinan derivatives and their pharmacologies. |
| AID131416 | Phenyl-p-benzoquinone-induced abdominal constriction after subcutaneous administration in mouse (in vivo) | 1991 | Journal of medicinal chemistry, Aug, Volume: 34, Issue:8 | (1S)-1-(aminomethyl)-2-(arylacetyl)-1,2,3,4-tetrahydroisoquinoline and heterocycle-condensed tetrahydropyridine derivatives: members of a novel class of very potent kappa opioid analgesics. |
| AID296059 | Antagonist activity at human kappa opioid receptor expressed in CHO cells assessed as inhibition of U69,593-induced stimulation of [35S]GTP-gamma-S binding after 60 mins | 2007 | Bioorganic & medicinal chemistry, Jun-15, Volume: 15, Issue:12 | In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors. |
| AID270609 | Enhancement of [35S]GTP-gamma-S binding to human KOR expressed in CHO cells | 2006 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17 | Synthesis and in vitro evaluation of salvinorin A analogues: effect of configuration at C(2) and substitution at C(18). |
| AID1630711 | Displacement of [3H]U69593 from rat KOR expressed in CHO cells | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21 | An LP1 analogue, selective MOR agonist with a peculiar pharmacological profile, used to scrutiny the ligand binding domain. |
| AID1197360 | Agonist activity against human recombinant opioid kappa receptor expressed in CHO cell membranes after 3 hrs by [35S]GTP-gamma-S binding assay relative to 500 nM (-)-U50,488 | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Probes for narcotic receptor mediated phenomena 49. N-substituted rac-cis-4a-arylalkyl-1,2,3,4,4a,9a-hexahydrobenzofuro[2,3-c]pyridin-6-ols. |
| AID148101 | Tested for inhibitory effect on binding of [3H]bremazocine to opioid receptor kappa in guinea pig cerebellum membranes | 1992 | Journal of medicinal chemistry, Nov-27, Volume: 35, Issue:24 | N-terminal alkylated derivatives of [D-Pro10]dynorphin A-(1-11) are highly selective for kappa-opioid receptors. |
| AID296057 | Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding relative to basal level after 60 mins | 2007 | Bioorganic & medicinal chemistry, Jun-15, Volume: 15, Issue:12 | In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors. |
| AID1528100 | Agonist activity at human KOR expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting relative to control | |||
| AID223595 | Binding affinity against opioid receptor kappa from guinea pig brain membranes using [3H]ethylketocyclazocine as radioligand | 1992 | Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12 | Selective reversible and irreversible ligands for the kappa opioid receptor. |
| AID1451337 | Toxicity in CD-1 mouse assessed as motor impairment at 5 to 10 mg/kg, sc treated 30 mins prior to test by rotarod test | 2017 | Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17 | Highly Potent and Selective New Diphenethylamines Interacting with the κ-Opioid Receptor: Synthesis, Pharmacology, and Structure-Activity Relationships. |
| AID1433979 | Displacement of [3H]U 69593 from rat recombinant kappa opioid receptor expressed in CHO cells after 60 mins by scintillation counting | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1 | Pyrimidine-Based Inhibitors of Dynamin I GTPase Activity: Competitive Inhibition at the Pleckstrin Homology Domain. |
| AID516776 | Displacement of [3H]diprenorphine from human kappa opioid receptor expressed in CHO cells | 2010 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 20, Issue:19 | Synthesis and biological evaluation of C-2 halogenated analogs of salvinorin A. |
| AID225536 | In vivo antinociceptive activity was determined using mouse hot plate test following subcutaneous administration | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16 | Substituted 1-(aminomethyl)-2-(arylacetyl)-1,2,3,4-tetrahydroisoquinolines: a novel class of very potent antinociceptive agents with varying degrees of selectivity for kappa and mu opioid receptors. |
| AID225656 | In vivo antinociceptive activity was determined using mouse tail-flick test following subcutaneous administration | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16 | Substituted 1-(aminomethyl)-2-(arylacetyl)-1,2,3,4-tetrahydroisoquinolines: a novel class of very potent antinociceptive agents with varying degrees of selectivity for kappa and mu opioid receptors. |
| AID65265 | Compound was evaluated for binding affinity towards Dopamine receptor D2 using [3H]SULP in rat; No inhibition at 10000 nM | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8 | Alterations in the stereochemistry of the kappa-selective opioid agonist U50,488 result in high-affinity sigma ligands. |
| AID149017 | Compound was evaluated for the opioid receptor mu affinity determined with [3H][D-Ala2-MePhe4-Gly-ol5]-enkephalin (DAGOL) in the presence of excess unlabeled DAGOL to suppress mu binding. | 1991 | Journal of medicinal chemistry, Jan, Volume: 34, Issue:1 | Highly selective kappa opioid analgesics. 4. Synthesis of some conformationally restricted naphthalene derivatives with high receptor affinity and selectivity. |
| AID321652 | Displacement of [3H]diprenorphine from mouse delta opioid receptor expressed in CHO cells | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3 | Standard protecting groups create potent and selective kappa opioids: salvinorin B alkoxymethyl ethers. |
| AID369069 | Agonist activity at human KOPR expressed in CHO cells assessed as enhancement of [35S]GTPgammaS binding at 10 uM relative to U50488 | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3 | Modification of the furan ring of salvinorin A: identification of a selective partial agonist at the kappa opioid receptor. |
| AID1877935 | Displacement of [3H]-U69593 from Dunkin-Hartley guinea pig brain membrane kappa opioid receptor incubated for 30 mins by liquid scintillation counting analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Dual Sigma-1 receptor antagonists and hydrogen sulfide-releasing compounds for pain treatment: Design, synthesis, and pharmacological evaluation. |
| AID225351 | Antinociceptive activity determined in mouse tail flick assay 30 min after sc injection (peak effect) | 1993 | Journal of medicinal chemistry, Jun-25, Volume: 36, Issue:13 | Non-peptide ligands for opioid receptors. Design of kappa-specific agonists. |
| AID1861726 | Binding affinity to MOR (unknown origin) assessed as inhibition constant by radioligand binding assay | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Design, synthesis and biological evaluation of novel aminopropylcarboxamide derivatives as sigma ligands. |
| AID270239 | Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18 | Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. 4. Opioid receptor binding properties of 8-[N-(4'-phenyl)-phenethyl)carboxamido] analogues of cyclazocine and ethylketocycalzocine. |
| AID1358126 | Displacement of [3H]diprenorphine from human KOR expressed in African green monkey COS1 cell membranes at 10 uM incubated for 1 hr by scintillation counting method | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Synthesis of 7β-hydroxy-8-ketone opioid derivatives with antagonist activity at mu- and delta-opioid receptors. |
| AID256205 | Percent maximal response in enhanced [35S]GTP-gamma-S, binding to human Opioid receptor kappa expressed in CHO cells relative to U50,488H | 2005 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 15, Issue:19 | Synthesis and in vitro pharmacological studies of C(4) modified salvinorin A analogues. |
| AID221210 | Sedative activity after sc administration in female mice (Alderley Park strain) | 1991 | Journal of medicinal chemistry, Nov, Volume: 34, Issue:11 | Structure/activity studies related to 2-(3,4-dichlorophenyl)-N-methyl-N-[2-(1-pyrrolidinyl)-1-substituted- ethyl]acetamides: a novel series of potent and selective kappa-opioid agonists. |
| AID151898 | Tested for binding affinity by [3H]diprenorphine displacement for Opioid receptor mu 1 was carried on crude membrane fractions obtained from the whole rat brain minus cerebellum.. | 2000 | Journal of medicinal chemistry, Aug-10, Volume: 43, Issue:16 | Nonpeptide analogues of dynorphin A(1-8): design, synthesis, and pharmacological evaluation of kappa-selective agonists. |
| AID1355423 | Agonist activity at human kappa opioid receptor expressed in HEK293 assessed as inhibition forskolin-induced cAMP accumulation after 15 mins by EIA | 2018 | Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13 | Constraining Endomorphin-1 by β,α-Hybrid Dipeptide/Heterocycle Scaffolds: Identification of a Novel κ-Opioid Receptor Selective Partial Agonist. |
| AID223113 | Antinociceptive activity in acetic acid induced abdominal constriction assay after sc administration and abolished by naloxone administered at 3 mg/kg sc in mice | 1991 | Journal of medicinal chemistry, Nov, Volume: 34, Issue:11 | Structure/activity studies related to 2-(3,4-dichlorophenyl)-N-methyl-N-[2-(1-pyrrolidinyl)-1-substituted- ethyl]acetamides: a novel series of potent and selective kappa-opioid agonists. |
| AID147852 | Percent maximal stimulation in [35S]-GTP-gamma S binding assay mediated by the Opioid receptor kappa 1 in chinese Hamster Ovary (CHO)membranes | 2003 | Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24 | Design and synthesis of novel dimeric morphinan ligands for kappa and micro opioid receptors. |
| AID1185653 | Displacement of [3H]U-69593 from kappa opioid receptor in guinea pig brain membranes after 2 hrs by scintillation counting analysis | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | Synthesis and pharmacological evaluation of 5-pyrrolidinylquinoxalines as a novel class of peripherally restricted κ-opioid receptor agonists. |
| AID709669 | Displacement of [3H]U69,593 from human kappa opioid receptor expressed in CHO cell membranes incubated for 60 mins by liquid scintillation counting | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 | Discovery and pharmacological evaluation of a diphenethylamine derivative (HS665), a highly potent and selective κ opioid receptor agonist. |
| AID640427 | Displacement of [3H]diprenorphine from rat MOPR expressed in CHO cells at 3 uM | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2 | Differential signaling properties at the kappa opioid receptor of 12-epi-salvinorin A and its analogues. |
| AID751865 | Binding affinity to human kappa-type opioid receptor by radioligand displacement assay | 2013 | European journal of medicinal chemistry, May, Volume: 63 | Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds. |
| AID226067 | Tested for opioid receptor agonistic activity in guinea pig ileum | 1992 | Journal of medicinal chemistry, Nov-27, Volume: 35, Issue:24 | N-terminal alkylated derivatives of [D-Pro10]dynorphin A-(1-11) are highly selective for kappa-opioid receptors. |
| AID148724 | Compound was tested for the change in the Opioid receptor kappa 1 binding affinity (Ki(mut)/Ki(wild) for D138A point mutations; No binding | 1998 | Journal of medicinal chemistry, Nov-19, Volume: 41, Issue:24 | Conformational analysis and automated receptor docking of selective arylacetamide-based kappa-opioid agonists. |
| AID132777 | In vivo antinociceptive activity using mouse tail flick test, subcutaneous administration | 1991 | Journal of medicinal chemistry, Aug, Volume: 34, Issue:8 | (1S)-1-(aminomethyl)-2-(arylacetyl)-1,2,3,4-tetrahydroisoquinoline and heterocycle-condensed tetrahydropyridine derivatives: members of a novel class of very potent kappa opioid analgesics. |
| AID1425958 | Agonist activity at human KOR expressed in HEK293 cells assessed as inhibition of forskolin-induced adenylyl cyclase-mediated cAMP accumulation after 30 mins by HTRF assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Discovery, structure-activity relationship studies, and anti-nociceptive effects of N-(1,2,3,4-tetrahydro-1-isoquinolinylmethyl)benzamides as novel opioid receptor agonists. |
| AID1458134 | Agonist activity at dopamine D2 receptor (unknown origin) at 10 uM | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15 | Opioid Receptor Modulators with a Cinnamyl Group. |
| AID776680 | Agonist activity at mouse cloned delta opioid receptor expressed in CHO cells after 60 mins by [35S]GTPgammaS binding assay | 2013 | European journal of medicinal chemistry, Nov, Volume: 69 | Novel 6β-acylaminomorphinans with analgesic activity. |
| AID1188907 | Displacement of [3H]DPDPE from delta opioid receptor in mouse whole brain without cerebellum | 2014 | ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8 | Synthesis and Pharmacology of a Novel κ Opioid Receptor (KOR) Agonist with a 1,3,5-Trioxazatriquinane Skeleton. |
| AID148434 | In vitro agonist activity at kappa opioid receptor in rabbit vas deferens. | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | A potent new class of kappa-receptor agonist: 4-substituted 1-(arylacetyl)-2-[(dialkylamino)methyl]piperazines. |
| AID1458124 | Agonist activity at recombinant human KOR expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP level preincubated for 15 to 20 mins followed by forskolin addition by GloSensor assay | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15 | Opioid Receptor Modulators with a Cinnamyl Group. |
| AID1689599 | Agonist activity at human kappa opioid receptor expressed in CHO cells incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting method relative to control | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Discovery of 3-((dimethylamino)methyl)-4-hydroxy-4-(3-methoxyphenyl)-N-phenylpiperidine-1-carboxamide as novel potent analgesic. |
| AID1714338 | Agonist activity at human KOR expressed in CHO cell membranes at 10 uM incubated for 1 hr by liquid scintillation counting based [35S]GTP-gamma-S assay | 2016 | Journal of medicinal chemistry, 11-23, Volume: 59, Issue:22 | Structure-Activity Relationships of [des-Arg |
| AID1458128 | Agonist activity at recombinant human DOR expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP level at 10 uM preincubated for 15 to 20 mins followed by forskolin addition by GloSensor assay relative to control | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15 | Opioid Receptor Modulators with a Cinnamyl Group. |
| AID1528106 | Antinociceptive activity in ip dosed Kunming mouse assessed as reduction in nociceptive response after 2 hrs by acetic acid-induced abdominal constriction test | |||
| AID601795 | Displacement of [3H]U69593 from kappa opioid receptor in guinea pig brain membranes after 150 mins by scintillation counting | 2011 | European journal of medicinal chemistry, Jun, Volume: 46, Issue:6 | Synthesis of 7,9-diazabicyclo[4.2.2]decanes as conformationally restricted κ receptor agonists: fine tuning of the dihedral angle of the ethylenediamine pharmacophore. |
| AID752228 | Binding affinity to kappa opioid receptor (unknown origin) by radioligand displacement assay | 2013 | Bioorganic & medicinal chemistry, May-15, Volume: 21, Issue:10 | Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor. |
| AID1458123 | Agonist activity at recombinant human KOR expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP level at 10 uM preincubated for 15 to 20 mins followed by forskolin addition by GloSensor assay relative to control | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15 | Opioid Receptor Modulators with a Cinnamyl Group. |
| AID149012 | Displacement of [3H]DAGO from mu opioid receptors in guinea pig brain (minus cerebellum). | 1991 | Journal of medicinal chemistry, Jan, Volume: 34, Issue:1 | (2S)-1-(arylacetyl)-2-(aminomethyl)piperidine derivatives: novel, highly selective kappa opioid analgesics. |
| AID149272 | Binding affinity towards Opioid receptor kappa 1 in guinea pig brain membranes using [3H]U-69593 as radioligand | 2001 | Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20 | Mixed kappa agonists and mu agonists/antagonists as potential pharmacotherapeutics for cocaine abuse: synthesis and opioid receptor binding affinity of N-substituted derivatives of morphinan. |
| AID224414 | In vitro efficacy against naloxone, in mouse vas deferens, activity expressed as Ke values. | 1991 | Journal of medicinal chemistry, Nov, Volume: 34, Issue:11 | Structure/activity studies related to 2-(3,4-dichlorophenyl)-N-methyl-N-[2-(1-pyrrolidinyl)-1-substituted- ethyl]acetamides: a novel series of potent and selective kappa-opioid agonists. |
| AID246977 | Effective dose required for agonistic activity upon intrathecal administration in mouse (n=10) tail flick assay | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | A bivalent ligand (KDAN-18) containing delta-antagonist and kappa-agonist pharmacophores bridges delta2 and kappa1 opioid receptor phenotypes. |
| AID147856 | Binding activity against human Opioid receptor kappa 1 using [3H]-U 50488 as a radioligand | 2002 | Journal of medicinal chemistry, Mar-28, Volume: 45, Issue:7 | Design, synthesis, and evaluation of opioid analogues with non-peptidic beta-turn scaffold: enkephalin and endomorphin mimetics. |
| AID1581725 | Displacement of [3H]DADLE from human recombinant delta opioid receptor expressed in rat Chem-1 (RBL) cell membranes incubated for 60 mins | 2020 | Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1 | Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids. |
| AID149994 | Inhibitory activity in stimulating [35S]-GTP-gamma S binding mediated by the Opioid receptor kappa 1 in chinese Hamster Ovary (CHO) cell membranes was determined | 2003 | Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24 | Design and synthesis of novel dimeric morphinan ligands for kappa and micro opioid receptors. |
| AID1398500 | Agonist activity at human KOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding based liquid scintillation counting analysis | 2018 | Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14 | 7β-Methyl substituent is a structural locus associated with activity cliff for nepenthone analogues. |
| AID112521 | In vivo analgesic activity for heat stimulus modality using tail flick test in female CF-1 mice administered subcutaneously | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6 | Naphtho and benzo analogues of the kappa opioid agonist trans-(+/-)-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl] benzeneacetamide. |
| AID1875776 | Antinociceptive activity in CD-1 mouse assessed as maximum possible effect at 20 umol/kg, iv measured after 15 to 120 mins by tail-flick test | 2022 | ACS medicinal chemistry letters, Nov-10, Volume: 13, Issue:11 | Discovery of κ Opioid Receptor (KOR)-Selective d-Tetrapeptides with Improved |
| AID321650 | Displacement of [3H]diprenorphine from human kappa opioid receptor expressed in CHO cells | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3 | Standard protecting groups create potent and selective kappa opioids: salvinorin B alkoxymethyl ethers. |
| AID410732 | Activity at human cloned kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay relative to basal GTPgammaS binding | 2009 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 19, Issue:1 | Syntheses and opioid receptor binding properties of carboxamido-substituted opioids. |
| AID1861728 | Binding affinity to KOR (unknown origin) assessed as inhibition constant by radioligand binding assay | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Design, synthesis and biological evaluation of novel aminopropylcarboxamide derivatives as sigma ligands. |
| AID601796 | Displacement of [3H]DAMGO from mu opioid receptor in guinea pig brain membranes | 2011 | European journal of medicinal chemistry, Jun, Volume: 46, Issue:6 | Synthesis of 7,9-diazabicyclo[4.2.2]decanes as conformationally restricted κ receptor agonists: fine tuning of the dihedral angle of the ethylenediamine pharmacophore. |
| AID152407 | Inhibition of [3H]fluadom binding to opioid receptor | 1989 | Journal of medicinal chemistry, Feb, Volume: 32, Issue:2 | Synthesis and biological evaluation of 14-alkoxymorphinans. 2. (-)-N-(cyclopropylmethyl)-4,14-dimethoxymorphinan-6-one, a selective mu opioid receptor antagonist. |
| AID417165 | Antagonist activity against human kappa opioid receptor expressed in CHO cells assessed as inhibition of U50488-stimulated [35S]GTPgammaS binding | 2009 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8 | Syntheses of novel high affinity ligands for opioid receptors. |
| AID670124 | Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [33S]GTPgammaS binding after 60 mins by scintillation counting relative to control | 2012 | Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8 | Synthesis, binding affinity, and functional in vitro activity of 3-benzylaminomorphinan and 3-benzylaminomorphine ligands at opioid receptors. |
| AID203996 | Compound was evaluated for binding affinity towards sigma opioid receptor using [3H](+)-3-PPP in guinea pig ileum | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8 | Alterations in the stereochemistry of the kappa-selective opioid agonist U50,488 result in high-affinity sigma ligands. |
| AID383162 | Displacement of [3H]DPDPE from delta opioid receptor in ICR mouse whole brain | 2008 | Bioorganic & medicinal chemistry, Apr-15, Volume: 16, Issue:8 | Syntheses of 4,6'-epoxymorphinan derivatives and their pharmacologies. |
| AID251604 | Ratio of effective dose of compound producing agonistic activity in presence and absence of norbinaltorphimine (2.5 pmol) upon intrathecal administration in mouse tail flick assay | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | A bivalent ligand (KDAN-18) containing delta-antagonist and kappa-agonist pharmacophores bridges delta2 and kappa1 opioid receptor phenotypes. |
| AID132052 | Effective dose of the compounds at 10 mg/kg of nor-BNI was administered subcutaneously 10 min before agonist were administered in mice for rotarod test. | 2000 | Journal of medicinal chemistry, Aug-10, Volume: 43, Issue:16 | Nonpeptide analogues of dynorphin A(1-8): design, synthesis, and pharmacological evaluation of kappa-selective agonists. |
| AID389678 | Selectivity ratio of Ke for mu opioid receptor in ddy mouse vas deferens to Ke for kappa opioid receptor in ddy mouse vas deferens | 2008 | Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20 | Design, synthesis, and structure-activity relationship of novel opioid kappa-agonists. |
| AID147981 | Opioid receptor kappa affinity, determined with [3H]etorphine in the presence of excess unlabeled [D-Ala2-MePhe4-Glyol5]-enkephalin | 1991 | Journal of medicinal chemistry, Jan, Volume: 34, Issue:1 | Highly selective kappa opioid analgesics. 4. Synthesis of some conformationally restricted naphthalene derivatives with high receptor affinity and selectivity. |
| AID149372 | Binding affinity for rat delta opioid receptor was evaluated by displacing [3H]- diprenorphine | 1993 | Journal of medicinal chemistry, Jun-25, Volume: 36, Issue:13 | Non-peptide ligands for opioid receptors. Design of kappa-specific agonists. |
| AID149188 | Binding affinity against opioid receptor delta from guinea pig brain membranes using [3H]DADLE as radioligand | 1992 | Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12 | Selective reversible and irreversible ligands for the kappa opioid receptor. |
| AID310357 | Agonist activity at human kappa opioid receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay | 2007 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 17, Issue:23 | Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. 5. Opioid receptor binding properties of N-((4'-phenyl)-phenethyl) analogues of 8-CAC. |
| AID389657 | Agonist activity at kappa opioid receptor in ddy mouse vas deferens assessed as inhibition of electric stimulation-induced contraction | 2008 | Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20 | Design, synthesis, and structure-activity relationship of novel opioid kappa-agonists. |
| AID1861727 | Binding affinity to DOR (unknown origin) assessed as inhibition constant by radioligand binding assay | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Design, synthesis and biological evaluation of novel aminopropylcarboxamide derivatives as sigma ligands. |
| AID1528092 | Agonist activity at rat MOR expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting relative to control | |||
| AID410733 | Activity at human cloned kappa opioid receptor expressed in CHO cells assessed as inhibition of U50488-induced [35S]GTPgammaS binding | 2009 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 19, Issue:1 | Syntheses and opioid receptor binding properties of carboxamido-substituted opioids. |
| AID149008 | Binding affinity against opioid receptor mu from guinea pig brain membranes using [3H]naloxone as radioligand | 1992 | Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12 | Selective reversible and irreversible ligands for the kappa opioid receptor. |
| AID1458126 | Agonist activity at recombinant human MOR expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP level at 10 uM preincubated for 15 to 20 mins followed by forskolin addition by GloSensor assay relative to control | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15 | Opioid Receptor Modulators with a Cinnamyl Group. |
| AID148262 | Displacement of [3H]-U-69,593 from Opioid receptor kappa 1 in guinea pig cerebellar. | 2000 | Journal of medicinal chemistry, Aug-10, Volume: 43, Issue:16 | Nonpeptide analogues of dynorphin A(1-8): design, synthesis, and pharmacological evaluation of kappa-selective agonists. |
| AID251603 | Ratio of effective dose of compound producing agonistic activity in presence and absence of naltriben (50 pmol) upon intrathecal administration in mouse tail flick assay | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | A bivalent ligand (KDAN-18) containing delta-antagonist and kappa-agonist pharmacophores bridges delta2 and kappa1 opioid receptor phenotypes. |
| AID167701 | Percent change of rate in the respiratory activity was measured in rabbit at 0.1 mg/kg dose given intravenously | 1989 | Journal of medicinal chemistry, Feb, Volume: 32, Issue:2 | Synthesis and biological evaluation of 14-alkoxymorphinans. 2. (-)-N-(cyclopropylmethyl)-4,14-dimethoxymorphinan-6-one, a selective mu opioid receptor antagonist. |
| AID225535 | In vivo antinociceptive activity was determined using mouse abdominal constriction test following subcutaneous administration | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16 | Substituted 1-(aminomethyl)-2-(arylacetyl)-1,2,3,4-tetrahydroisoquinolines: a novel class of very potent antinociceptive agents with varying degrees of selectivity for kappa and mu opioid receptors. |
| AID157446 | Compound was evaluated for binding affinity towards Phencyclidine receptor using [3H]TCP in guinea pig ileum; No inhibition at 10000 nM | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8 | Alterations in the stereochemistry of the kappa-selective opioid agonist U50,488 result in high-affinity sigma ligands. |
| AID149844 | Binding affinity against Opioid receptor kappa 1 in guinea pig. | 1996 | Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4 | Synthesis, biological evaluation, and quantitative receptor docking simulations of 2-[(acylamino)ethyl]-1,4-benzodiazepines as novel tifluadom-like ligands with high affinity and selectivity for kappa-opioid receptors. |
| AID235330 | Selectivity ratio of kappa opioid receptor to that of mu opioid receptor in guinea pig brain membranes | 2001 | Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20 | Mixed kappa agonists and mu agonists/antagonists as potential pharmacotherapeutics for cocaine abuse: synthesis and opioid receptor binding affinity of N-substituted derivatives of morphinan. |
| AID1689598 | Agonist activity at rat delta opioid receptor expressed in CHO cells incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting method relative to control | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Discovery of 3-((dimethylamino)methyl)-4-hydroxy-4-(3-methoxyphenyl)-N-phenylpiperidine-1-carboxamide as novel potent analgesic. |
| AID131759 | Tested for effective dose required to produce antinociceptive activity in mice by tail flick method | 1982 | Journal of medicinal chemistry, Oct, Volume: 25, Issue:10 | Benzeneacetamide amines: structurally novel non-m mu opioids. |
| AID149287 | Compound was evaluated for binding affinity towards kappa opioid receptor using [3H]-BREM in guinea pig ileum | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8 | Alterations in the stereochemistry of the kappa-selective opioid agonist U50,488 result in high-affinity sigma ligands. |
| AID719289 | Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation counting relative to untreated-control | 2012 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24 | Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 8. High affinity ligands for opioid receptors in the picomolar Ki range: oxygenated N-(2-[1,1'-biphenyl]-4-ylethyl) analogues of 8-CAC. |
| AID1630718 | Selectivity ratio of Ki for displacement of [3H]DPDPE from human DOR expressed in CHO cells to Ki for displacement of [3H]DAMGO from MOR in HEK293 cells | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21 | An LP1 analogue, selective MOR agonist with a peculiar pharmacological profile, used to scrutiny the ligand binding domain. |
| AID417160 | Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding | 2009 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8 | Syntheses of novel high affinity ligands for opioid receptors. |
| AID152406 | Inhibition of [3H]DADLE binding to opioid receptor | 1989 | Journal of medicinal chemistry, Feb, Volume: 32, Issue:2 | Synthesis and biological evaluation of 14-alkoxymorphinans. 2. (-)-N-(cyclopropylmethyl)-4,14-dimethoxymorphinan-6-one, a selective mu opioid receptor antagonist. |
| AID147840 | Irreversible inhibition of [3H]naloxone binding to kopioid receptor kappa of guinea pig brain membranes on preincubation with 10E-4 M of the compound | 1992 | Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12 | Selective reversible and irreversible ligands for the kappa opioid receptor. |
| AID125471 | Percent activity against delta selective antinociception when given icv injection at a dose of 30 nmol 20 min before mouse tail flick test | 1996 | Journal of medicinal chemistry, May-10, Volume: 39, Issue:10 | Asymmetric syntheses, opioid receptor affinities, and antinociceptive effects of 8-amino-5,9-methanobenzocyclooctenes, a new class of structural analogues of the morphine alkaloids. |
| AID1722001 | Analgesic activity in OX1R knock out mouse assessed as increase in wheel running activity | 2020 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 30, Issue:17 | Discovery of attenuation effect of orexin 1 receptor to aversion of nalfurafine: Synthesis and evaluation of D-nor-nalfurafine derivatives and analyses of the three active conformations of nalfurafine. |
| AID135326 | BBB penetration classification | 2000 | Journal of medicinal chemistry, Jun-01, Volume: 43, Issue:11 | Predicting blood-brain barrier permeation from three-dimensional molecular structure. |
| AID1299242 | Agonist activity at human KOR expressed in EE-HEK293 cells | 2016 | Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12 | Evaluation of N-substituent structural variations in opioid receptor profile of LP1. |
| AID776681 | Agonist activity at mouse cloned kappa opioid receptor expressed in CHO cells after 60 mins by [35S]GTPgammaS binding assay | 2013 | European journal of medicinal chemistry, Nov, Volume: 69 | Novel 6β-acylaminomorphinans with analgesic activity. |
| AID147976 | Displacement of [3H]-BRL 52537 from opioid receptor kappa site in guinea pig | 1991 | Journal of medicinal chemistry, Aug, Volume: 34, Issue:8 | (1S)-1-(aminomethyl)-2-(arylacetyl)-1,2,3,4-tetrahydroisoquinoline and heterocycle-condensed tetrahydropyridine derivatives: members of a novel class of very potent kappa opioid analgesics. |
| AID1303904 | Peripheral restriction index, ratio of sedative ED50 in sc dosed Kunming mouse to antinociceptive ED50 in ip dosed mouse | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13 | Design, synthesis and biological evaluation of novel tetrahydroisoquinoline quaternary derivatives as peripheral κ-opioid receptor agonists. |
| AID1528110 | Induction of sedation in Kunming mouse assessed as inhibition of novelty-induced locomotor activity at 5 mg/kg, ip treated for 30 mins before placing animal into locomotor chambers and monitored for 30 mins | |||
| AID131758 | Tested for effective dose required to produce antinociceptive activity in mice by HCl writhing method | 1982 | Journal of medicinal chemistry, Oct, Volume: 25, Issue:10 | Benzeneacetamide amines: structurally novel non-m mu opioids. |
| AID149189 | Affinity for opioid receptor delta sites | 1991 | Journal of medicinal chemistry, Aug, Volume: 34, Issue:8 | (1S)-1-(aminomethyl)-2-(arylacetyl)-1,2,3,4-tetrahydroisoquinoline and heterocycle-condensed tetrahydropyridine derivatives: members of a novel class of very potent kappa opioid analgesics. |
| AID74457 | Tested for naloxone pA2 activity in guinea pig ileum | 1992 | Journal of medicinal chemistry, Nov-27, Volume: 35, Issue:24 | N-terminal alkylated derivatives of [D-Pro10]dynorphin A-(1-11) are highly selective for kappa-opioid receptors. |
| AID514359 | Displacement of [3H]DAMGO from Sprague-Dawley rat mu opioid receptor by liquid scintillation counting | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14 | Evaluation of N-substitution in 6,7-benzomorphan compounds. |
| AID149014 | Receptor binding affinity towards opioid receptor mu | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16 | Substituted 1-(aminomethyl)-2-(arylacetyl)-1,2,3,4-tetrahydroisoquinolines: a novel class of very potent antinociceptive agents with varying degrees of selectivity for kappa and mu opioid receptors. |
| AID1458129 | Antagonist activity at recombinant human DOR expressed in HEK293T cells assessed as reduction in DADLE-induced inhibition of forskolin-stimulated cAMP level at 10 uM preincubated for 15 to 20 mins followed by DADLE and forskolin addition by GloSensor assa | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15 | Opioid Receptor Modulators with a Cinnamyl Group. |
| AID149991 | Human Opioid receptor kappa 1 mediated stimulation of [35S]- GTPgammaS binding in CHO cells (Agonist potency). | 2000 | Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14 | [Pro(3)]Dyn A(1-11)-NH(2): a dynorphin analogue with high selectivity for the kappa opioid receptor. |
| AID1581726 | Displacement of [3H]U69,593 from human recombinant kappa opioid receptor expressed in rat RBL cell membranes incubated for 60 mins | 2020 | Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1 | Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids. |
| AID243417 | Activation of human Opioid receptor kappa 1 expressed in chinese hamster ovary cells to enhance [35S]GTP-gamma-S, binding compared to U50,488H | 2005 | Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11 | Synthesis and in vitro pharmacological evaluation of salvinorin A analogues modified at C(2). |
| AID149131 | Binding affinity for the Opioid receptor kappa 1 | 1988 | Journal of medicinal chemistry, Apr, Volume: 31, Issue:4 | Highly selective kappa opioid analgesics. Synthesis and structure-activity relationships of novel N-[(2-aminocyclohexyl)aryl]acetamide and N-[(2-aminocyclohexyl)aryloxy]acetamide derivatives. |
| AID389673 | Equilibrium constant, ratio of IC50 for mu opioid receptor in guinea pig ileum in presence of 100 nM Naloxone to IC50 for mu opioid receptor in guinea pig ileum | 2008 | Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20 | Design, synthesis, and structure-activity relationship of novel opioid kappa-agonists. |
| AID389670 | Agonist activity at kappa opioid receptor in guinea pig ileum assessed as inhibition of electric stimulation-induced contraction | 2008 | Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20 | Design, synthesis, and structure-activity relationship of novel opioid kappa-agonists. |
| AID138825 | Evaluation for the ability of mu opioid to protect the [3H]DAMGO binding site from alkylation | 1994 | Journal of medicinal chemistry, May-27, Volume: 37, Issue:11 | 14 alpha,14' beta-[Dithiobis[(2-oxo-2,1-ethanediyl)imino]]bis (7,8-dihydromorphinone) and 14 alpha,14' beta-[dithiobis[(2-oxo-2,1- ethanediyl)imino]]bis[7,8-dihydro-N-(cyclopropylmethyl)normorphinone]: chemistry and opioid binding properties. |
| AID148304 | Binding affinity against Opioid receptor kappa 1 using [3H]U-69593 as a radioligand | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6 | Naphtho and benzo analogues of the kappa opioid agonist trans-(+/-)-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl] benzeneacetamide. |
| AID235329 | Selectivity ratio of kappa opioid receptor to that of delta opioid receptor in guinea pig brain membranes | 2001 | Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20 | Mixed kappa agonists and mu agonists/antagonists as potential pharmacotherapeutics for cocaine abuse: synthesis and opioid receptor binding affinity of N-substituted derivatives of morphinan. |
| AID131761 | Tested for effective dose required to produce morphine antagonist activity in mice | 1982 | Journal of medicinal chemistry, Oct, Volume: 25, Issue:10 | Benzeneacetamide amines: structurally novel non-m mu opioids. |
| AID488650 | Selectivity ratio of Ki for mu opioid receptor to kappa opioid receptor | 2010 | Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12 | Identification of the three-dimensional pharmacophore of kappa-opioid receptor agonists. |
| AID76238 | Opioid agonist activity was measured by Anti-Straub tail (AST) test after subcutaneous administration in guinea pig ilium | 1994 | Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19 | Synthesis and opioid activity of 7-oxygenated 2,3,4,4a,5,6,7,7a-octahydro-1H-benzofuro[3,2-e]isoquinolin-9-ols. |
| AID329905 | Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay relative to DAMGO | 2008 | Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8 | Herkinorin analogues with differential beta-arrestin-2 interactions. |
| AID147979 | Displacement of [3H]U-69593 from kappa opioid receptors in guine pig brain (minus cerebellum). | 1991 | Journal of medicinal chemistry, Jan, Volume: 34, Issue:1 | (2S)-1-(arylacetyl)-2-(aminomethyl)piperidine derivatives: novel, highly selective kappa opioid analgesics. |
| AID1633373 | Agonist activity at human kappa opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay | 2019 | ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4 | Novel Cyclic Biphalin Analogues by Ruthenium-Catalyzed Ring Closing Metathesis: |
| AID185352 | Dose (po) required to produce 50% of the maximum possible analgesic effect, evaluated by rat-paw pressure assay | 1988 | Journal of medicinal chemistry, Apr, Volume: 31, Issue:4 | Highly selective kappa opioid analgesics. Synthesis and structure-activity relationships of novel N-[(2-aminocyclohexyl)aryl]acetamide and N-[(2-aminocyclohexyl)aryloxy]acetamide derivatives. |
| AID488649 | Binding affinity to kappa opioid receptor | 2010 | Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12 | Identification of the three-dimensional pharmacophore of kappa-opioid receptor agonists. |
| AID1188906 | Displacement of [3H]DAMGO from mu opioid receptor in mouse whole brain without cerebellum | 2014 | ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8 | Synthesis and Pharmacology of a Novel κ Opioid Receptor (KOR) Agonist with a 1,3,5-Trioxazatriquinane Skeleton. |
| AID224426 | Molar potency ratio relative to the standard agonist EKC assayed in mouse vas deferens. | 1991 | Journal of medicinal chemistry, Nov, Volume: 34, Issue:11 | Structure/activity studies related to 2-(3,4-dichlorophenyl)-N-methyl-N-[2-(1-pyrrolidinyl)-1-substituted- ethyl]acetamides: a novel series of potent and selective kappa-opioid agonists. |
| AID406411 | Protection against Bacillus anthracis lethal toxin-mediated cytotoxicity in mouse RAW264.7 cells assessed as change in viability at 0.125 to 12.5 uM relative to toxin-treated control | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Amiodarone and bepridil inhibit anthrax toxin entry into host cells. |
| AID709666 | Displacement of [3H]pCl-DPDPE from human delta opioid receptor expressed in CHO cell membranes incubated for 60 mins by liquid scintillation counting | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 | Discovery and pharmacological evaluation of a diphenethylamine derivative (HS665), a highly potent and selective κ opioid receptor agonist. |
| AID148254 | Evaluation for the ability of kappa opioid to protect the [3H]-DAMGO binding site from alkylation | 1994 | Journal of medicinal chemistry, May-27, Volume: 37, Issue:11 | 14 alpha,14' beta-[Dithiobis[(2-oxo-2,1-ethanediyl)imino]]bis (7,8-dihydromorphinone) and 14 alpha,14' beta-[dithiobis[(2-oxo-2,1- ethanediyl)imino]]bis[7,8-dihydro-N-(cyclopropylmethyl)normorphinone]: chemistry and opioid binding properties. |
| AID383163 | Displacement of [3H]U69593 from kappa opioid receptor in guinea pig cerebellum | 2008 | Bioorganic & medicinal chemistry, Apr-15, Volume: 16, Issue:8 | Syntheses of 4,6'-epoxymorphinan derivatives and their pharmacologies. |
| AID131764 | Tested for effective dose required to produce sedative activity in mice by inclined screen method | 1982 | Journal of medicinal chemistry, Oct, Volume: 25, Issue:10 | Benzeneacetamide amines: structurally novel non-m mu opioids. |
| AID1655289 | Displacement of [3H]-U69,593 from KOR in guinea pig brain membranes incubated for 30 mins by liquid scintillation counting | |||
| AID1581727 | Displacement of [3H]DAMGO from human recombinant mu opioid receptor expressed in HEK293 cell membranes incubated for 60 mins | 2020 | Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1 | Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids. |
| AID112522 | In vivo analgesic activity for pressure stimulus modality using tail pinch test in female CF-1 mice administered subcutaneously | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6 | Naphtho and benzo analogues of the kappa opioid agonist trans-(+/-)-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl] benzeneacetamide. |
| AID1861724 | Binding affinity to sigma 2 receptor (unknown origin) assessed as inhibition constant by radioligand binding assay | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Design, synthesis and biological evaluation of novel aminopropylcarboxamide derivatives as sigma ligands. |
| AID1188908 | Displacement of [3H]U69593 from kappa opioid receptor in guinea pig cerebellum | 2014 | ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8 | Synthesis and Pharmacology of a Novel κ Opioid Receptor (KOR) Agonist with a 1,3,5-Trioxazatriquinane Skeleton. |
| AID389665 | Antinociceptive activity in sc dosed mouse assessed as inhibition of acetic acid-induced writhing administered 15 mins before acetic acid challenge | 2008 | Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20 | Design, synthesis, and structure-activity relationship of novel opioid kappa-agonists. |
| AID1197355 | Antagonist activity against human recombinant opioid mu receptor expressed in CHO cell membranes assessed as reduction in DAMGO-induced response after 3 hrs by [35S]GTP-gamma-S binding assay | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Probes for narcotic receptor mediated phenomena 49. N-substituted rac-cis-4a-arylalkyl-1,2,3,4,4a,9a-hexahydrobenzofuro[2,3-c]pyridin-6-ols. |
| AID1689595 | Agonist activity at rat delta opioid receptor expressed in CHO cells incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting method | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Discovery of 3-((dimethylamino)methyl)-4-hydroxy-4-(3-methoxyphenyl)-N-phenylpiperidine-1-carboxamide as novel potent analgesic. |
| AID709663 | Selectivity index, ratio of KI for human delta opioid receptor to KI for human kappa opioid receptor | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 | Discovery and pharmacological evaluation of a diphenethylamine derivative (HS665), a highly potent and selective κ opioid receptor agonist. |
| AID290263 | Antagonist activity against [35S]GTP-gamma-S binding from human kappa opioid receptors expressed in CHO cell membrane | 2007 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6 | High-affinity carbamate analogues of morphinan at opioid receptors. |
| AID1303903 | Sedative activity in sc dosed Kunming mouse assessed as latency to step off the platform after 20 mins by rotation test | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13 | Design, synthesis and biological evaluation of novel tetrahydroisoquinoline quaternary derivatives as peripheral κ-opioid receptor agonists. |
| AID290262 | Agonist activity at huma kappa opioid receptor expressed in CHO cells assessed as U50488-stimulated of [35S]GTP-gamma-S binding | 2007 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6 | High-affinity carbamate analogues of morphinan at opioid receptors. |
| AID329904 | Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay | 2008 | Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8 | Herkinorin analogues with differential beta-arrestin-2 interactions. |
| AID148988 | Affinity to opioid receptor kappa 1 using [3H]U-69593 as radioligand in homogenates of guinea pig brain membranes | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | Methylated analogues of methyl (R)-4-(3,4-dichlorophenylacetyl)- 3-(pyrrolidin-1-ylmethyl)piperazine-1-carboxylate (GR-89,696) as highly potent kappa-receptor agonists: stereoselective synthesis, opioid-receptor affinity, receptor selectivity, and functio |
| AID149180 | Irreversible inhibition of [3H]-DADLE binding to delta opioid receptors of guinea pig brain membranes on pre-incubation with 10E-5 M of the compound. | 1992 | Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12 | Selective reversible and irreversible ligands for the kappa opioid receptor. |
| AID1398499 | Agonist activity at rat MOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding based liquid scintillation counting analysis relative to control | 2018 | Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14 | 7β-Methyl substituent is a structural locus associated with activity cliff for nepenthone analogues. |
| AID270610 | Enhancement of [35S]GTP-gamma-S binding to human KOR expressed in CHO cells relative to U50,488H | 2006 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17 | Synthesis and in vitro evaluation of salvinorin A analogues: effect of configuration at C(2) and substitution at C(18). |
| AID1224135 | Displacement of [3H]U-69593 from kappa-opioid receptor in guinea pig brain membrane | 2014 | Bioorganic & medicinal chemistry, Jul-01, Volume: 22, Issue:13 | Combination of cyclohexane and piperazine based κ-opioid receptor agonists: Synthesis and pharmacological evaluation of trans,trans-configured perhydroquinoxalines. |
| AID147982 | Receptor binding affinity towards opioid receptor kappa | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16 | Substituted 1-(aminomethyl)-2-(arylacetyl)-1,2,3,4-tetrahydroisoquinolines: a novel class of very potent antinociceptive agents with varying degrees of selectivity for kappa and mu opioid receptors. |
| AID1186507 | Agonist activity at human kappa opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP production after 30 mins by HTRF assay | 2014 | Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17 | Discovery, structure-activity relationship studies, and anti-nociceptive effects of 1-phenyl-3,6,6-trimethyl-1,5,6,7-tetrahydro-4H-indazol-4-one as novel opioid receptor agonists. |
| AID148734 | Selectivity kappa/delta | 2000 | Journal of medicinal chemistry, Jan-13, Volume: 43, Issue:1 | Synthesis and opioid receptor affinity of morphinan and benzomorphan derivatives: mixed kappa agonists and mu agonists/antagonists as potential pharmacotherapeutics for cocaine dependence. |
| AID131760 | Tested for effective dose required to produce antinociceptive activity in mice by tail pinch method | 1982 | Journal of medicinal chemistry, Oct, Volume: 25, Issue:10 | Benzeneacetamide amines: structurally novel non-m mu opioids. |
| AID148508 | Effective dose required for antagonist activity against Opioid receptor delta 1 | 1990 | Journal of medicinal chemistry, Jun, Volume: 33, Issue:6 | Naltrindole 5'-isothiocyanate: a nonequilibrium, highly selective delta opioid receptor antagonist. |
| AID450514 | Induction of ERK phosphorylation in rat astrocyte at 1 uM after 10 mins | 2009 | Bioorganic & medicinal chemistry, Aug-15, Volume: 17, Issue:16 | Synthesis and characterizations of novel quinoline derivatives having mixed ligand activities at the kappa and mu receptors: Potential therapeutic efficacy against morphine dependence. |
| AID232429 | Ratio of inhibition of binding to opioid receptor in the presence and absence of NaCl | 1989 | Journal of medicinal chemistry, Feb, Volume: 32, Issue:2 | Synthesis and biological evaluation of 14-alkoxymorphinans. 2. (-)-N-(cyclopropylmethyl)-4,14-dimethoxymorphinan-6-one, a selective mu opioid receptor antagonist. |
| AID594451 | Agonist activity at kappa opioid receptor in rat C6 cells assessed as induction of ERK1/2 phosphorylation at 1 uM after 10 min by Western blot analysis | 2011 | European journal of medicinal chemistry, May, Volume: 46, Issue:5 | Synthesis and biological evaluation of dibenz[b,f][1,5]oxazocine derivatives for agonist activity at κ-opioid receptor. |
| AID601799 | Displacement of [3H]di-o-toylguanidine from sigma 2 receptor in rat liver homogenates | 2011 | European journal of medicinal chemistry, Jun, Volume: 46, Issue:6 | Synthesis of 7,9-diazabicyclo[4.2.2]decanes as conformationally restricted κ receptor agonists: fine tuning of the dihedral angle of the ethylenediamine pharmacophore. |
| AID709665 | Selectivity index, ratio of KI for human mu opioid receptor to KI for human kappa opioid receptor | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 | Discovery and pharmacological evaluation of a diphenethylamine derivative (HS665), a highly potent and selective κ opioid receptor agonist. |
| AID1655379 | Displacement of [3H]diprenorphine human kappa opioid receptor expressed in CHO cell membranes after 1 hr by micro beta2 scintillation counting method | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 | Developing Cyclic Opioid Analogues: Fluorescently Labeled Bioconjugates of Biphalin. |
| AID450512 | Displacement of [3H]dynorphin from human kappa opioid receptor expressed in C6 giloma cells measured total binding per mg of protein at 5 uM | 2009 | Bioorganic & medicinal chemistry, Aug-15, Volume: 17, Issue:16 | Synthesis and characterizations of novel quinoline derivatives having mixed ligand activities at the kappa and mu receptors: Potential therapeutic efficacy against morphine dependence. |
| AID1194140 | Antinociceptive activity in sc dosed mouse by warm water tail-flick test relative to control | 2015 | Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8 | Design, syntheses, and pharmacological characterization of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6α-(isoquinoline-3'-carboxamido)morphinan analogues as opioid receptor ligands. |
| AID149128 | Binding affinity for kappa opioid receptor in absence of 120 mM NaCl and 50 micro M Gpp(NH)p | 1993 | Journal of medicinal chemistry, Jun-25, Volume: 36, Issue:13 | Non-peptide ligands for opioid receptors. Design of kappa-specific agonists. |
| AID601797 | Displacement of [3H]DPDPE from delta opioid receptor in rat brain membranes | 2011 | European journal of medicinal chemistry, Jun, Volume: 46, Issue:6 | Synthesis of 7,9-diazabicyclo[4.2.2]decanes as conformationally restricted κ receptor agonists: fine tuning of the dihedral angle of the ethylenediamine pharmacophore. |
| AID1233291 | Antinociceptive effect in ip dosed C57BL/6 mouse assessed as tail withdrawal latency measured up to 2 hrs by 55 degC Warm water tail withdrawal assay | 2015 | Journal of medicinal chemistry, Jun-25, Volume: 58, Issue:12 | Parallel Synthesis of Hexahydrodiimidazodiazepines Heterocyclic Peptidomimetics and Their in Vitro and in Vivo Activities at μ (MOR), δ (DOR), and κ (KOR) Opioid Receptors. |
| AID594447 | Displacement of [125I]dynorphin from kappa opioid receptor in BALB/c mouse brain membrane at 5 uM by liquid scintillation counting relative to control | 2011 | European journal of medicinal chemistry, May, Volume: 46, Issue:5 | Synthesis and biological evaluation of dibenz[b,f][1,5]oxazocine derivatives for agonist activity at κ-opioid receptor. |
| AID1861723 | Binding affinity to sigma 1 receptor (unknown origin) assessed as inhibition constant by radioligand binding assay | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Design, synthesis and biological evaluation of novel aminopropylcarboxamide derivatives as sigma ligands. |
| AID147844 | Irreversible inhibition of [3H]naloxone binding to opioid receptor kappa of guinea pig brain membranes on preincubation with 10E-5 M of the compound. | 1992 | Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12 | Selective reversible and irreversible ligands for the kappa opioid receptor. |
| AID1773094 | Positive allosteric modulator activity in mouse kappa opioid receptor stably expressed in HEK293 cell membrane assessed as binding affinity of U50,488 to orthosteric binding site incubated with U50,488 alone for 90 mins by radioligand competition binding | 2021 | Journal of natural products, 08-27, Volume: 84, Issue:8 | Plant-Derived Cyclotides Modulate κ-Opioid Receptor Signaling. |
| AID1630716 | Selectivity ratio of Ki for displacement of [3H]U69593 from rat KOR expressed in CHO cells to Ki for displacement of [3H]DAMGO from MOR in HEK293 cells | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21 | An LP1 analogue, selective MOR agonist with a peculiar pharmacological profile, used to scrutiny the ligand binding domain. |
| AID130353 | In vivo antinociceptive activity was determined using mouse acetylcholine induced abdominal constriction test following subcutaneous administration; range (0.23-0.70) | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | A potent new class of kappa-receptor agonist: 4-substituted 1-(arylacetyl)-2-[(dialkylamino)methyl]piperazines. |
| AID381429 | Increase of JNK phosphorylation in U50488 treated untransfected HEK293 cells at 10 uM after 1 hr | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41 | Long-acting kappa opioid antagonists disrupt receptor signaling and produce noncompetitive effects by activating c-Jun N-terminal kinase. |
| AID1630479 | Displacement of [3H]U69,593 from human KOR expressed in HEK293 cell membranes incubated for 90 mins by liquid scintillation counting | 2016 | Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19 | Versatile Picklocks To Access All Opioid Receptors: Tuning the Selectivity and Functional Profile of the Cyclotetrapeptide c[Phe-d-Pro-Phe-Trp] (CJ-15,208). |
| AID389675 | Equilibrium constant, ratio of IC50 for kappa opioid receptor in ddy mouse vas deferens in presence of 1 nM nor-BNI to IC50 for kappa opioid receptor in ddy mouse vas deferens | 2008 | Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20 | Design, synthesis, and structure-activity relationship of novel opioid kappa-agonists. |
| AID1285646 | Displacement of [3H]U 69593 from rat recombinant kappa-type opioid receptor expressed in CHO cells | 2016 | Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8 | Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents. |
| AID128825 | Anti-nociceptive activity (Analgesia reversed by 3 mg/kg of naloxone) after administration through the subcutaneous route to female mice. | 1991 | Journal of medicinal chemistry, Jan, Volume: 34, Issue:1 | 2-(3,4-Dichlorophenyl)-N-methyl-N-[2-(1-pyrrolidinyl)-1-substituted- ethyl]-acetamides: the use of conformational analysis in the development of a novel series of potent opioid kappa agonists. |
| AID1773110 | Positive allosteric modulator activity in mouse kappa opioid receptor stably expressed in HEK293 cell membrane assessed as inhibition of forskolin induced cAMP production by measuring U50,488 Emax incubated with U50,488 alone measured after 30 mins by HTR | 2021 | Journal of natural products, 08-27, Volume: 84, Issue:8 | Plant-Derived Cyclotides Modulate κ-Opioid Receptor Signaling. |
| AID149270 | Binding affinity towards Opioid receptor kappa 1 by displacing the radioligand [3H]U-69593 from guinea pig brain membrane | 2000 | Journal of medicinal chemistry, Jan-13, Volume: 43, Issue:1 | Synthesis and opioid receptor affinity of morphinan and benzomorphan derivatives: mixed kappa agonists and mu agonists/antagonists as potential pharmacotherapeutics for cocaine dependence. |
| AID369070 | Binding affinity to rat MOPR expressed in CHO cells | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3 | Modification of the furan ring of salvinorin A: identification of a selective partial agonist at the kappa opioid receptor. |
| AID709667 | Displacement of [3H]DAMGO from human mu opioid receptor expressed in CHO cell membranes incubated for 60 mins by liquid scintillation counting | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 | Discovery and pharmacological evaluation of a diphenethylamine derivative (HS665), a highly potent and selective κ opioid receptor agonist. |
| AID131763 | Tested for effective dose required to produce narcotic stimulation in mice; not active | 1982 | Journal of medicinal chemistry, Oct, Volume: 25, Issue:10 | Benzeneacetamide amines: structurally novel non-m mu opioids. |
| AID1458131 | Analgesic activity in C57BL/6J mouse assessed as tail withdrawal latency at 5 mg/kg by tail flick test | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15 | Opioid Receptor Modulators with a Cinnamyl Group. |
| AID1875775 | Antinociceptive activity in CD-1 mouse assessed as maximum possible effect at 10 nmol, icv measured after 15 to 120 mins by tail-flick test | 2022 | ACS medicinal chemistry letters, Nov-10, Volume: 13, Issue:11 | Discovery of κ Opioid Receptor (KOR)-Selective d-Tetrapeptides with Improved |
| AID286308 | Agonist activity at human opioid kappa receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding | 2007 | Journal of medicinal chemistry, May-03, Volume: 50, Issue:9 | Pharmacological properties of bivalent ligands containing butorphan linked to nalbuphine, naltrexone, and naloxone at mu, delta, and kappa opioid receptors. |
| AID148721 | Compound was tested for the change in the Opioid receptor kappa 1 binding affinity (Ki(mut)/Ki(wild) for D105N point mutations. | 1998 | Journal of medicinal chemistry, Nov-19, Volume: 41, Issue:24 | Conformational analysis and automated receptor docking of selective arylacetamide-based kappa-opioid agonists. |
| AID1458136 | Agonist activity at histamine H1 receptor (unknown origin) at 10 uM | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15 | Opioid Receptor Modulators with a Cinnamyl Group. |
| AID233908 | Selectivity, ratio of affinity towards mu to kappa opioid receptor | 2000 | Journal of medicinal chemistry, Aug-10, Volume: 43, Issue:16 | Nonpeptide analogues of dynorphin A(1-8): design, synthesis, and pharmacological evaluation of kappa-selective agonists. |
| AID640425 | Displacement of [3H]diprenorphine from human KOPR expressed in CHO cells | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2 | Differential signaling properties at the kappa opioid receptor of 12-epi-salvinorin A and its analogues. |
| AID601798 | Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in guinea pig brain membranes | 2011 | European journal of medicinal chemistry, Jun, Volume: 46, Issue:6 | Synthesis of 7,9-diazabicyclo[4.2.2]decanes as conformationally restricted κ receptor agonists: fine tuning of the dihedral angle of the ethylenediamine pharmacophore. |
| AID255651 | Concentration required to enhance [35S]GTP-gamma-S, binding to human Opioid receptor kappa expressed in CHO cells | 2005 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 15, Issue:19 | Synthesis and in vitro pharmacological studies of C(4) modified salvinorin A analogues. |
| AID406410 | Protection against Bacillus anthracis protective antigen and lethal toxin-diphtheria toxin chimeric protein mediated cytotoxicity in mouse RAW264.7 cells assessed as cell viability | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Amiodarone and bepridil inhibit anthrax toxin entry into host cells. |
| AID240367 | Effective concentration for activation of human Opioid receptor kappa 1 expressed in chinese hamster ovary cells to enhance [35S]GTP-gamma-S, binding | 2005 | Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11 | Synthesis and in vitro pharmacological evaluation of salvinorin A analogues modified at C(2). |
| AID514360 | Displacement of [3H]DPDPE from Sprague-Dawley rat delta opioid receptor by liquid scintillation counting | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14 | Evaluation of N-substitution in 6,7-benzomorphan compounds. |
| AID270608 | Inhibition of [3H]diprenorphine binding to human KOR expressed in CHO cells | 2006 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17 | Synthesis and in vitro evaluation of salvinorin A analogues: effect of configuration at C(2) and substitution at C(18). |
| AID228522 | Tested for ratio between opioid receptor kappa and opioid receptor mu binding; 1/178 | 1992 | Journal of medicinal chemistry, Nov-27, Volume: 35, Issue:24 | N-terminal alkylated derivatives of [D-Pro10]dynorphin A-(1-11) are highly selective for kappa-opioid receptors. |
| AID149130 | Binding affinity for kappa opioid receptor was evaluated by displacing [3H]- diprenorphine | 1993 | Journal of medicinal chemistry, Jun-25, Volume: 36, Issue:13 | Non-peptide ligands for opioid receptors. Design of kappa-specific agonists. |
| AID112520 | In vivo analgesic activity for chemical irritation modality using HCl writhing test in female CF-1 mice administered subcutaneously | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6 | Naphtho and benzo analogues of the kappa opioid agonist trans-(+/-)-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl] benzeneacetamide. |
| AID1528096 | Agonist activity at rat DOR expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting relative to control | |||
| AID149041 | Inhibition of [3H]naloxone binding to opioid receptor in presence of NaCl | 1989 | Journal of medicinal chemistry, Feb, Volume: 32, Issue:2 | Synthesis and biological evaluation of 14-alkoxymorphinans. 2. (-)-N-(cyclopropylmethyl)-4,14-dimethoxymorphinan-6-one, a selective mu opioid receptor antagonist. |
| AID276332 | Binding potency at human kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay | 2006 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21 | Synthesis and in vitro pharmacological studies of new C(4)-modified salvinorin A analogues. |
| AID369071 | Binding affinity to mouse DOPR expressed in CHO cells | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3 | Modification of the furan ring of salvinorin A: identification of a selective partial agonist at the kappa opioid receptor. |
| AID1458127 | Antagonist activity at recombinant human MOR expressed in HEK293T cells assessed as reduction in DAMGO-induced inhibition of forskolin-stimulated cAMP level at 10 uM preincubated for 15 to 20 mins followed by DAMGO and forskolin addition by GloSensor assa | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15 | Opioid Receptor Modulators with a Cinnamyl Group. |
| AID761674 | Displacement of [131I]-[D-Ala2,4'-I-Phe8]alpha-Neoendorphin from opioid receptor in CD-1 mouse brain after 90 mins by competitive binding assay | 2013 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15 | Sandmeyer reaction repurposed for the site-selective, non-oxidizing radioiodination of fully-deprotected peptides: studies on the endogenous opioid peptide α-neoendorphin. |
| AID95362 | Selectivity against kappa receptor in the presence of 0.5 nmol icv SIOM | 1993 | Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17 | A selective delta 1 opioid receptor agonist derived from oxymorphone. Evidence for separate recognition sites for delta 1 opioid receptor agonists and antagonists. |
| AID640424 | Agonist activity at human KOPR expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by liquid scintillation counting | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2 | Differential signaling properties at the kappa opioid receptor of 12-epi-salvinorin A and its analogues. |
| AID1303901 | Displacement of [3H]diprenorphine from human kappa opioid receptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting analysis | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13 | Design, synthesis and biological evaluation of novel tetrahydroisoquinoline quaternary derivatives as peripheral κ-opioid receptor agonists. |
| AID149009 | Affinity for opioid receptor mu sites | 1991 | Journal of medicinal chemistry, Aug, Volume: 34, Issue:8 | (1S)-1-(aminomethyl)-2-(arylacetyl)-1,2,3,4-tetrahydroisoquinoline and heterocycle-condensed tetrahydropyridine derivatives: members of a novel class of very potent kappa opioid analgesics. |
| AID147910 | Binding affinity for the Opioid receptor mu 1 | 1988 | Journal of medicinal chemistry, Apr, Volume: 31, Issue:4 | Highly selective kappa opioid analgesics. Synthesis and structure-activity relationships of novel N-[(2-aminocyclohexyl)aryl]acetamide and N-[(2-aminocyclohexyl)aryloxy]acetamide derivatives. |
| AID149193 | Compound was evaluated for its binding affinity against opioid receptor delta subtype in guinea pig brain (minus cerebellum) using [3H]-DADLE as radioligand. | 1991 | Journal of medicinal chemistry, Jan, Volume: 34, Issue:1 | (2S)-1-(arylacetyl)-2-(aminomethyl)piperidine derivatives: novel, highly selective kappa opioid analgesics. |
| AID147951 | Irreversible inhibition of [3H]-naloxone binding to opioid receptor kappa of guinea pig brain membranes on pre-incubation with 10E-6 M of the compound. | 1992 | Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12 | Selective reversible and irreversible ligands for the kappa opioid receptor. |
| AID149129 | Binding affinity for kappa opioid receptor in presence of 120 mM NaCl and 50 micro M Gpp(NH)p | 1993 | Journal of medicinal chemistry, Jun-25, Volume: 36, Issue:13 | Non-peptide ligands for opioid receptors. Design of kappa-specific agonists. |
| AID709668 | Agonist activity at human kappa opioid receptor expressed in CHO cell membranes incubated for 60 mins by [35S]GTPgammaS binding assay relative to U69,593 | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 | Discovery and pharmacological evaluation of a diphenethylamine derivative (HS665), a highly potent and selective κ opioid receptor agonist. |
| AID129315 | Antinociceptive activity was determined using the mouse acetylcholine-induced abdominal constriction test followed by subcutaneous administration | 1992 | Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3 | New kappa-receptor agonists based upon a 2-[(alkylamino)methyl]piperidine nucleus. |
| AID389671 | Equilibrium constant, ratio of IC50 for kappa opioid receptor in guinea pig ileum in presence of 10 nM nor-BNI to IC50 for kappa opioid receptor in guinea pig ileum | 2008 | Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20 | Design, synthesis, and structure-activity relationship of novel opioid kappa-agonists. |
| AID233963 | Ratio of binding affinity against mu opioid receptor to that of kappa opioid receptor | 1993 | Journal of medicinal chemistry, Jun-25, Volume: 36, Issue:13 | Non-peptide ligands for opioid receptors. Design of kappa-specific agonists. |
| AID290261 | Agonist activity at human opioid kappa receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S binding relative to control | 2007 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6 | High-affinity carbamate analogues of morphinan at opioid receptors. |
| AID148114 | Ratio measured as the Ki(kappa) to that of Ki(mu) values. | 1991 | Journal of medicinal chemistry, Jan, Volume: 34, Issue:1 | Highly selective kappa opioid analgesics. 4. Synthesis of some conformationally restricted naphthalene derivatives with high receptor affinity and selectivity. |
| AID1458135 | Antagonist activity at dopamine D2 receptor (unknown origin) at 10 uM | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15 | Opioid Receptor Modulators with a Cinnamyl Group. |
| AID148735 | Selectivity kappa/mu | 2000 | Journal of medicinal chemistry, Jan-13, Volume: 43, Issue:1 | Synthesis and opioid receptor affinity of morphinan and benzomorphan derivatives: mixed kappa agonists and mu agonists/antagonists as potential pharmacotherapeutics for cocaine dependence. |
| AID516775 | Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as increase of [35S]GTPgammaS binding | 2010 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 20, Issue:19 | Synthesis and biological evaluation of C-2 halogenated analogs of salvinorin A. |
| AID1398503 | Agonist activity at rat DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding based liquid scintillation counting analysis relative to control | 2018 | Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14 | 7β-Methyl substituent is a structural locus associated with activity cliff for nepenthone analogues. |
| AID1689597 | Agonist activity at rat mu opioid receptor expressed in CHO cells incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting method relative to control | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Discovery of 3-((dimethylamino)methyl)-4-hydroxy-4-(3-methoxyphenyl)-N-phenylpiperidine-1-carboxamide as novel potent analgesic. |
| AID296058 | Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding after 60 mins | 2007 | Bioorganic & medicinal chemistry, Jun-15, Volume: 15, Issue:12 | In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors. |
| AID227968 | Ke value was measured as antagonist/ (IC50 ratio - 1) | 1994 | Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19 | Synthesis and opioid activity of 7-oxygenated 2,3,4,4a,5,6,7,7a-octahydro-1H-benzofuro[3,2-e]isoquinolin-9-ols. |
| AID150392 | Inhibition of [3H]naloxone binding to opioid receptor in presence of NaCl | 1989 | Journal of medicinal chemistry, Feb, Volume: 32, Issue:2 | Synthesis and biological evaluation of 14-alkoxymorphinans. 2. (-)-N-(cyclopropylmethyl)-4,14-dimethoxymorphinan-6-one, a selective mu opioid receptor antagonist. |
| AID148158 | Maximal percent inhibitory activity in stimulating [35S]-GTP-gamma S binding mediated by the Opioid receptor kappa 1 in chinese Hamster Ovary (CHO) cell membranes; Not Tested | 2003 | Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24 | Design and synthesis of novel dimeric morphinan ligands for kappa and micro opioid receptors. |
| AID1458137 | Antagonist activity at histamine H1 receptor (unknown origin) at 10 uM | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15 | Opioid Receptor Modulators with a Cinnamyl Group. |
| AID221722 | Antinociceptive activity determined in vivo in tail flick assay in male Swiss mice with 0.2 mg/kg Naloxone | 1993 | Journal of medicinal chemistry, Jun-25, Volume: 36, Issue:13 | Non-peptide ligands for opioid receptors. Design of kappa-specific agonists. |
| AID1543760 | Displacement of [3H]-U69,593 from KOR in guinea pig brain membranes incubated for 30 mins by liquid scintillation counting | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | (2S)-N-2-methoxy-2-phenylethyl-6,7-benzomorphan compound (2S-LP2): Discovery of a biased mu/delta opioid receptor agonist. |
| AID148883 | Irreversible inhibition of [3H][3H]ethylketocyclazocine binding to mu opioid receptors of guinea pig brain membranes on pre-incubation with 10E-5 M of the compound. | 1992 | Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12 | Selective reversible and irreversible ligands for the kappa opioid receptor. |
| AID776682 | Agonist activity at mouse cloned mu opioid receptor expressed in CHO cells after 60 mins by [35S]GTPgammaS binding assay | 2013 | European journal of medicinal chemistry, Nov, Volume: 69 | Novel 6β-acylaminomorphinans with analgesic activity. |
| AID230524 | Ratio of rotarod value MPE50/antinociceptive activity MPE50 | 2000 | Journal of medicinal chemistry, Aug-10, Volume: 43, Issue:16 | Nonpeptide analogues of dynorphin A(1-8): design, synthesis, and pharmacological evaluation of kappa-selective agonists. |
| AID1630710 | Displacement of [3H]DAMGO from MOR in HEK293 cells | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21 | An LP1 analogue, selective MOR agonist with a peculiar pharmacological profile, used to scrutiny the ligand binding domain. |
| AID329906 | Agonist activity at human recombinant kappa opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay | 2008 | Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8 | Herkinorin analogues with differential beta-arrestin-2 interactions. |
| AID1861725 | Selectivity index, ratio of Ki for sigma 1 receptor (unknown origin) to Ki for sigma 2 receptor (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Design, synthesis and biological evaluation of novel aminopropylcarboxamide derivatives as sigma ligands. |
| AID411136 | Displacement of [3H]U69,593 from kappa opioid receptor in guinea pig cerebellum | 2008 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24 | Synthesis of a novel 6,14-epoxymorphinan derivative and its pharmacology. |
| AID231476 | Ratio between IC50 of the agonist in presence of naloxone and IC50 of the control | 1994 | Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19 | Synthesis and opioid activity of 7-oxygenated 2,3,4,4a,5,6,7,7a-octahydro-1H-benzofuro[3,2-e]isoquinolin-9-ols. |
| AID369068 | Agonist activity at human KOPR expressed in CHO cells assessed as enhancement of [35S]GTPgammaS binding | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3 | Modification of the furan ring of salvinorin A: identification of a selective partial agonist at the kappa opioid receptor. |
| AID1355417 | Agonist activity at human kappa opioid receptor expressed in HEK293 assessed as inhibition forskolin-induced cAMP accumulation at 0.00001 to 100 uM after 15 mins by cAMP EIA relative to control | 2018 | Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13 | Constraining Endomorphin-1 by β,α-Hybrid Dipeptide/Heterocycle Scaffolds: Identification of a Novel κ-Opioid Receptor Selective Partial Agonist. |
| AID1773102 | Positive allosteric modulator activity in mouse kappa opioid receptor stably expressed in HEK293 cell membrane assessed as inhibition of forskolin induced cAMP production by measuring U50,488 EC50 incubated with U50,488 alone measured after 30 mins by HTR | 2021 | Journal of natural products, 08-27, Volume: 84, Issue:8 | Plant-Derived Cyclotides Modulate κ-Opioid Receptor Signaling. |
| AID1358125 | Displacement of [3H]diprenorphine from human KOR expressed in African green monkey COS1 cell membranes at 1 uM incubated for 1 hr by scintillation counting method | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Synthesis of 7β-hydroxy-8-ketone opioid derivatives with antagonist activity at mu- and delta-opioid receptors. |
| AID1722003 | Toxicity in OX1R knock out mouse assessed as increase in conditioned place aversion at 1 to 4 mg/kg, sc | 2020 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 30, Issue:17 | Discovery of attenuation effect of orexin 1 receptor to aversion of nalfurafine: Synthesis and evaluation of D-nor-nalfurafine derivatives and analyses of the three active conformations of nalfurafine. |
| AID1773126 | Positive allosteric modulator activity in mouse kappa opioid receptor stably expressed in HEK293 cell membrane assessed as beta-arrestin recruitment by measuring U50,488 Emax using furimazine as a substrate pretreated for 5 mins followed by incubation wit | 2021 | Journal of natural products, 08-27, Volume: 84, Issue:8 | Plant-Derived Cyclotides Modulate κ-Opioid Receptor Signaling. |
| AID514361 | Displacement of [3H]U69593 from Sprague-Dawley rat kappa opioid receptor in guinea pig cerebella by liquid scintillation counting | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14 | Evaluation of N-substitution in 6,7-benzomorphan compounds. |
| AID321651 | Displacement of [3H]diprenorphine from rat mu opioid receptor expressed in CHO cells | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3 | Standard protecting groups create potent and selective kappa opioids: salvinorin B alkoxymethyl ethers. |
| AID417161 | Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding relative to basal level | 2009 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8 | Syntheses of novel high affinity ligands for opioid receptors. |
| AID450521 | Displacement of [3H]dynorphin from human kappa opioid receptor expressed in C6 giloma cells | 2009 | Bioorganic & medicinal chemistry, Aug-15, Volume: 17, Issue:16 | Synthesis and characterizations of novel quinoline derivatives having mixed ligand activities at the kappa and mu receptors: Potential therapeutic efficacy against morphine dependence. |
| AID131532 | Effective dose at 10 mg/kg of nor-BNI was administered subcutaneously 10 min before agonist were administered in mice to test the antinociceptive activity. | 2000 | Journal of medicinal chemistry, Aug-10, Volume: 43, Issue:16 | Nonpeptide analogues of dynorphin A(1-8): design, synthesis, and pharmacological evaluation of kappa-selective agonists. |
| AID481095 | Displacement of [3H]U69593 from kappa opioid receptor in guinea pig brain membrane after 150 mins by scintillation counting | 2010 | Journal of medicinal chemistry, May-27, Volume: 53, Issue:10 | Conformationally constrained kappa receptor agonists: stereoselective synthesis and pharmacological evaluation of 6,8-diazabicyclo[3.2.2]nonane derivatives. |
| AID707252 | Displacement of [3H]U69,593 from human KOR expressed in HEK293 cells after 90 mins by liquid scintillation counting | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 | Opioid activity profiles of oversimplified peptides lacking in the protonable N-terminus. |
| AID1355420 | Displacement of [3H]U69,593 from human kappa opioid receptor expressed in HEK293 cell membranes after 2 hrs by liquid scintillation spectrometry | 2018 | Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13 | Constraining Endomorphin-1 by β,α-Hybrid Dipeptide/Heterocycle Scaffolds: Identification of a Novel κ-Opioid Receptor Selective Partial Agonist. |
| AID223600 | Opioid receptor kappa agonist potency was determined in vitro using rabbit vas deferens(LVD) preparation | 1992 | Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3 | New kappa-receptor agonists based upon a 2-[(alkylamino)methyl]piperidine nucleus. |
| AID1185655 | Displacement of [3H]Cl-977 from kappa opioid receptor in guinea pig brain membranes after 2 hrs by scintillation counting analysis | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | Synthesis and pharmacological evaluation of 5-pyrrolidinylquinoxalines as a novel class of peripherally restricted κ-opioid receptor agonists. |
| AID481097 | Displacement of [3H]Cl977 from human kappa opioid receptor expressed in HEK293 cells | 2010 | Journal of medicinal chemistry, May-27, Volume: 53, Issue:10 | Conformationally constrained kappa receptor agonists: stereoselective synthesis and pharmacological evaluation of 6,8-diazabicyclo[3.2.2]nonane derivatives. |
| AID147959 | Compound was evaluated for the opioid receptor kappa affinity using guinea pig brain membranes. | 1991 | Journal of medicinal chemistry, Jan, Volume: 34, Issue:1 | 2-(3,4-Dichlorophenyl)-N-methyl-N-[2-(1-pyrrolidinyl)-1-substituted- ethyl]-acetamides: the use of conformational analysis in the development of a novel series of potent opioid kappa agonists. |
| AID594450 | Agonist activity at kappa opioid receptor in rat C6 cells assessed as induction of ERK1/2 phosphorylation at 40 uM after 10 min by Western blot analysis | 2011 | European journal of medicinal chemistry, May, Volume: 46, Issue:5 | Synthesis and biological evaluation of dibenz[b,f][1,5]oxazocine derivatives for agonist activity at κ-opioid receptor. |
| AID389679 | Selectivity ratio of Ke for delta opioid receptor in ddy mouse vas deferens to Ke for kappa opioid receptor in ddy mouse vas deferens | 2008 | Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20 | Design, synthesis, and structure-activity relationship of novel opioid kappa-agonists. |
| AID147956 | Binding affinity against opioid receptor kappa, in guinea pig brain membrane, using [3H]bremazocine as the radioligand. | 1991 | Journal of medicinal chemistry, Nov, Volume: 34, Issue:11 | Structure/activity studies related to 2-(3,4-dichlorophenyl)-N-methyl-N-[2-(1-pyrrolidinyl)-1-substituted- ethyl]acetamides: a novel series of potent and selective kappa-opioid agonists. |
| AID719290 | Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation counting | 2012 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24 | Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 8. High affinity ligands for opioid receptors in the picomolar Ki range: oxygenated N-(2-[1,1'-biphenyl]-4-ylethyl) analogues of 8-CAC. |
| AID149940 | Tested for binding affinity by [3H]diprenorphine displacement for Opioid receptor delta 1 are carried on crude membrane fractions obtained from the whole rat brain minus cerebellum. | 2000 | Journal of medicinal chemistry, Aug-10, Volume: 43, Issue:16 | Nonpeptide analogues of dynorphin A(1-8): design, synthesis, and pharmacological evaluation of kappa-selective agonists. |
| AID389682 | Selectivity ratio of Ke for mu opioid receptor in guinea pig ileum to Ke for kappa opioid receptor in guinea pig ileum | 2008 | Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20 | Design, synthesis, and structure-activity relationship of novel opioid kappa-agonists. |
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| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 258 (15.84) | 18.7374 |
| 1990's | 729 (44.75) | 18.2507 |
| 2000's | 402 (24.68) | 29.6817 |
| 2010's | 191 (11.72) | 24.3611 |
| 2020's | 49 (3.01) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (26.71) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 3 (0.18%) | 5.53% |
| Reviews | 14 (0.84%) | 6.00% |
| Case Studies | 1 (0.06%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 1,646 (98.92%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||