norbinaltorphimine: kappa opiate receptor antagonist; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 5480230 |
| CHEMBL ID | 573214 |
| CHEBI ID | 81529 |
| SCHEMBL ID | 12013206 |
| MeSH ID | M0147411 |
| Synonym |
|---|
| gtpl1642 |
| 4,8:11,15-dimethano-20h-bisbenzofuro(2,3-a:3',2'-i)dipyrido(4,3-b:3',4'-h)carbazole-1,8a,10a,18-tetrol, 7,12-bis(cyclopropylmethyl)-5,6,7,8,9,10,11,12,13,14,19a,20b-dodecahydro-20-methyl-, (8r-(4br*,8alpha,8abeta,10aalpha,11beta,14ar*,19aalpha,20bbeta))- |
| nor-binaltorphimine |
| nor-bni |
| PDSP2_001420 |
| LOPAC0_000806 |
| 11,12,13,14,19a,20b-dodecahydro-, (4bs,8r,8as,10as,11r,14as,19ar,20br)- |
| 4,8:11,15-dimethano-20h-bisbenzofuro(2,3-a:3',2'-i)dipyrido(4,3-b:3',4'-h)carbazole-1,8a,10a,18-tetrol,7,12-bis(cyclopropylmethyl)-5,6,7,8,9,10,11,12,13,14,19a,20b-dodecahydro-20-methyl-, (8r-(4br*,8a |
| lpha,8abeta,10aalpha,11beta,14ar*,19aalpha,20bbeta))- 4,8:11,15-dimethano-20h-bisbenzofuro[2,3-a:3',2'-i]dipyrido[3,4-h:4',3'-b]carbazole-1,8a,10a,18-tetrol, 7,12-bis(cyclopropylmethyl)-5,6,7,8,9,10, |
| ta,10aalpha,11beta,14as*,19aalpha,20bbeta)]- |
| 4,8:11,15-dimethano-20h-bisbenzofuro[2,3-a:3',2'-i]dipyrido[4,3-b:3',4'-h]carbazole-1,8a,10a,18-tetrol, 7,12-bis(cyclopropylmethyl)-5,6,7,8,9,10,11,12,13,14,19a,20b-dodecahydro-, (4bs,8r,8as,10as,11r, |
| 14as,19ar,20br)- (9ci) |
| 105618-26-6 |
| 4,8:11,15-dimethano-20h-bisbenzofuro[2,3-a:3',2'-i]dipyrido[4,3-b:3',4'-h]carbazole-1,8a,10a,18-tetrol, 7,12-bis(cyclopropylmethyl)-5,6,7,8,9,10,11,12,13,14,19a,20b-dodecahydro-, [8r-(4bs*,8alpha,8abe |
| norbinaltorphimine |
| NCGC00024547-03 |
| NCGC00024547-02 |
| NCGC00024547-04 |
| C18130 , |
| norbni |
| CHEMBL573214 |
| (-)-norbinaltorphimine |
| nor-binaltorphamine |
| chebi:81529 , |
| CCG-204890 |
| bdbm82551 |
| nor-bni (hci)2 |
| 36ooq86qm1 , |
| unii-36ooq86qm1 |
| 4,8:11,15-dimethano-20h-bisbenzofuro(2,3-a:3',2'-i)dipyrido(4,3-b:3',4'-h)carbazole-1,8a,10a,18-tetrol, 7,12-bis(cyclopropylmethyl)-5,6,7,8,9,10,11,12,13,14,19a,20b-dodecahydro-, (4bs,8r,8as,10as,11r,14as,19ar,20br)- |
| BP-20300 |
| NCGC00024547-06 |
| SCHEMBL12013206 |
| n-demethylbinaltorphimine |
| n-demethylbinaltrorphimine |
| APSUXPSYBJVPPS-YAUKWVCOSA-N |
| (1s,2s,7s,8s,12r,20r,24r,32r)-11,33-bis(cyclopropylmethyl)-19,25-dioxa-11,22,33-triazaundecacyclo[24.9.1.18,14.01,24.02,32.04,23.05,21.07,12.08,20.030,36.018,37]heptatriaconta-4(23),5(21),14(37),15,17,26,28,30(36)-octaene-2,7,17,27-tetrol |
| Q27087998 |
| SDCCGSBI-0050783.P002 |
| DTXSID90897163 |
Norbinaltorphimine (nor-BNI) is a bifunctional reagent developed as a selective antagonist of the kappa opioid receptor.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Norbinaltorphimine (nor-BNI) is a bifunctional reagent developed as a selective antagonist of the kappa opioid receptor. " | ( A brief study of the selectivity of norbinaltorphimine, (-)-cyclofoxy, and (+)-cyclofoxy among opioid receptor subtypes in vitro. Bykov, V; De Costa, BR; Jacobson, AE; Newman, AH; Reid, A; Rice, KC; Rothman, RB, 1988) | 1.99 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "Pretreatment with norbinaltorphimine or naltriben also attenuated the antinociceptive response to i.t., but not i.c.v., [Dmt(1)]DALDA." | ( Endogenous opioid peptides contribute to antinociceptive potency of intrathecal [Dmt1]DALDA. Qian, X; Soong, Y; Szeto, HH; Wu, D; Zhao, GM, 2003) | 0.64 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " Taken together, these results demonstrate that MPClE is a novel, potent, orally active and safe analgesic drug that targets κ-opioid receptors." | ( A novel, potent, oral active and safe antinociceptive pyrazole targeting kappa opioid receptors. Athayde, ML; Boligon, AA; Bonacorso, HG; Calixto, JB; Ferreira, J; Machado, P; Martins, MA; Oliveira, SM; Rosa, F; Rossato, MF; Rubin, MA; Silva, CR; Tonello, R; Trevisan, G; Walker, CI; Zanatta, N, 2013) | 0.39 |
| " Unfortunately, we have shown that morphine administered in the acute phase of SCI results in significant, adverse secondary consequences including compromised locomotor and sensory recovery." | ( Nor-Binaltorphimine Blocks the Adverse Effects of Morphine after Spinal Cord Injury. Aceves, AR; Aceves, M; Bancroft, EA; Hook, MA, 2017) | 0.46 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " These results provide pharmacokinetic support for the long-lasting antagonistic effects of nor-BNI." | ( Pharmacokinetic evidence for the long-lasting effect of nor-binaltorphimine, a potent kappa opioid receptor antagonist, in mice. Kiguchi, N; Kishioka, S; Ko, MC; Kobayashi, Y; Saika, F; Wakida, N; Woods, JH; Yamamoto, C, 2013) | 0.39 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs." | ( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019) | 0.51 |
Naloxone (1 microM) or norbinaltorphimine (10 nM) shifted the dose-response curve of (-)-U50,488H to the right by 100-fold.
| Excerpt | Relevance | Reference |
|---|---|---|
| " At all pretreatment times, the antinociceptive dose-response lines for these kappa agonists were displaced to the right to various degrees in a parallel fashion; an increasing rightward displacement of the U69,593 and bremazocine antinociceptive dose-response lines was observed at 1 and 3 days after a single nor-BNI pretreatment, with a gradual return toward the control level at later times after pretreatment." | ( Extremely long-lasting antagonistic actions of nor-binaltorphimine (nor-BNI) in the mouse tail-flick test. Horan, P; Porreca, F; Taylor, J; Yamamura, HI, 1992) | 0.28 |
| " 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 |
| " dose-response studies with TCTAP (mu), naltrindole (delta) and norbinaltorphimine (kappa)." | ( The role of multiple opioid receptors in the maintenance of stimulation-induced feeding. Carr, KD; Papadouka, V, 1994) | 0.53 |
| " dose-response studies with TCTAP (mu), norbinaltorphimine (kappa), and naltrindole (delta)." | ( The role of multiple opioid receptors in the potentiation of reward by food restriction. Carr, KD; Papadouka, V, 1994) | 0.56 |
| " Preliminary experiments established the pharmacodynamics and dose-response for NorBNI." | ( Cardiorespiratory and sleep-wake behavior in developing swine: kappa-opioid influence. Faltus, RE; Inman, JD; Laferrière, A; Moss, IR, 1995) | 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 |
| "Local perfusion with ibogaine (10(-6) M-10(-3) M) via microdialysis probes in the nucleus accumbens or striatum of rats produced a biphasic dose-response effect on extracellular dopamine levels." | ( Neuropharmacological characterization of local ibogaine effects on dopamine release. Berger, SP; Broderick, PA; Hsu, K; Reid, MS; Souza, KH, 1996) | 0.29 |
| " 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) | 0.6 |
| " It is concluded that blockade of the kappa-opioid receptor by nor-binaltorphimine may produce a rightward shift of the unit dose-response relationship of cocaine reward, thus decreasing the sensitivity to cocaine reward." | ( Kappa-opioid receptor blockade with nor-binaltorphimine modulates cocaine self-administration in drug-naive rats. Gerrits, MA; Kuzmin, AV; Van Ree, JM, 1998) | 0.3 |
| " The 2 d agonist exposure (1 microM) caused a shift in the U69,593 dose-response curve that was greater in the potassium-stimulated paradigm (140-fold) than in the spontaneous release assay (sixfold)." | ( kappa-Opioid tolerance and dependence in cultures of dopaminergic midbrain neurons. Dalman, FC; O'Malley, KL, 1999) | 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 |
| " Because its pharmacological characterization has not been fully identified, the present study examined whether a dose-response range of general and selective opioid antagonists as well as antisense oligodeoxynucleotide (AS ODN) opioid probes altered daytime feeding over a 4-h time course elicited by dynorphin." | ( Dynorphin A(1-17)-induced feeding: pharmacological characterization using selective opioid antagonists and antisense probes in rats. Bodnar, RJ; Grossman, HC; Hadjimarkou, MM; Pasternak, GW; Rossi, GC; Silva, RM, 2002) | 0.31 |
| " Antinociceptive dose-response curves were constructed for spinal Delta(9)-THC and WIN 55,212-2 in prodynorphin knock-out mice and in wild-type littermates." | ( Dynorphin-independent spinal cannabinoid antinociception. Gardell, LR; Lai, J; Ossipov, MH; Porreca, F; Vanderah, TW, 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 dose-response study with the selective kappa antagonist nor-binaltorphimine (nor-BNI) showed that a low dose (1." | ( The dynamic relationship between mu and kappa opioid receptors in body temperature regulation. Adler, MW; Chen, X; Geller, EB; McClatchy, DB; Tallarida, RJ, 2005) | 0.33 |
| "0 mg/kg) dose-response and time-course (10, 20, and 30 min) effects in a thermal nociceptive assay, and 2) the ability for the KOP antagonist norBNI (10." | ( Antinociceptive profile of salvinorin A, a structurally unique kappa opioid receptor agonist. McCurdy, CR; Nieto, MJ; Smith, GH; Sufka, KJ; Warnick, JE, 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 |
| "0 mg/kg) attenuated the priming effects of cocaine, shifting the cocaine dose-response function rightward and downward." | ( Attenuation of cocaine-induced reinstatement of drug seeking in squirrel monkeys: kappa opioid and serotonergic mechanisms. Platt, DM; Rowlett, JK; Rüedi-Bettschen, D; Spealman, RD, 2010) | 0.36 |
| " The same sequence of experiments was repeated in the isolated heart model using the maximal protective dose of remifentanil from the dose-response studies." | ( Remifentanil post-conditioning attenuates cardiac ischemia-reperfusion injury via kappa or delta opioid receptor activation. Irwin, MG; Jiang, LL; Li, R; Wong, GT, 2010) | 0.36 |
| " 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 |
| Class | Description |
|---|---|
| isoquinolines | A class of organic heteropolycyclic compound consisting of isoquinoline and its substitution derivatives. |
| [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) |
|---|---|---|---|---|---|---|---|
| thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 0.3030 | 0.1000 | 20.8793 | 79.4328 | AID588453; AID588456 |
| GLS protein | Homo sapiens (human) | Potency | 12.5893 | 0.3548 | 7.9355 | 39.8107 | AID624146 |
| Microtubule-associated protein tau | Homo sapiens (human) | Potency | 24.0682 | 0.1800 | 13.5574 | 39.8107 | AID1460; AID1468 |
| regulator of G-protein signaling 4 | Homo sapiens (human) | Potency | 37.6858 | 0.5318 | 15.4358 | 37.6858 | AID504845 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 33.1734 | 0.0013 | 10.1577 | 42.8575 | AID1259252 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 25.9056 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 50.1187 | 0.0060 | 26.1688 | 89.1251 | AID488953 |
| flap endonuclease 1 | Homo sapiens (human) | Potency | 11.9173 | 0.1337 | 25.4129 | 89.1251 | AID488816; AID588795 |
| [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) |
|---|---|---|---|---|---|---|---|
| Mu-type opioid receptor | Homo sapiens (human) | EC50 (µMol) | 0.1200 | 0.0000 | 0.3263 | 9.4000 | AID482611 |
| Delta-type opioid receptor | Homo sapiens (human) | EC50 (µMol) | 0.3800 | 0.0000 | 0.4332 | 8.3000 | AID482612 |
| Kappa-type opioid receptor | Homo sapiens (human) | EC50 (µMol) | 0.0060 | 0.0000 | 0.2244 | 8.9900 | AID482613 |
| Mitogen-activated protein kinase 8 | Homo sapiens (human) | EC50 (µMol) | 0.1580 | 0.0100 | 0.3738 | 1.2400 | AID381427 |
| Mitogen-activated protein kinase 9 | Homo sapiens (human) | EC50 (µMol) | 0.1580 | 0.0100 | 0.3738 | 1.2400 | AID381427 |
| Mitogen-activated protein kinase 10 | Homo sapiens (human) | EC50 (µMol) | 0.1580 | 0.0870 | 0.4950 | 1.2400 | AID381427 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID631361 | Displacement of [3H]diprenorphine from human opioid delta receptor expressed in HEK293 cells after 120 mins by scintillation counting | 2011 | Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23 | Discovery of aminobenzyloxyarylamides as κ opioid receptor selective antagonists: application to preclinical development of a κ opioid receptor antagonist receptor occupancy tracer. |
| AID151620 | Inhibition of [3H]DAMGO binding to Opioid receptor mu 1 of rat brain tissue | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 | Identification of (3R)-7-hydroxy-N-((1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)- 3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl)-1,2,3,4-tetrahydro- 3-isoquinolinecarboxamide as a novel potent and selective opioid kappa receptor antagonist. |
| AID147896 | Antagonist activity on agonist stimulated [35S]GTP-gamma-S, binding in guinea pig caudate membranes (10 uM DAMGO as the agonist ligand for mu-receptor) | 2003 | Bioorganic & medicinal chemistry letters, Feb-10, Volume: 13, Issue:3 | Synthesis, opioid receptor binding, and functional activity of 5'-substituted 17-cyclopropylmethylpyrido[2',3':6,7]morphinans. |
| AID148236 | Binding affinity towards human cloned Opioid receptor delta 1 using [3H]Cl-DPDPE | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 | Identification of (3R)-7-hydroxy-N-((1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)- 3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl)-1,2,3,4-tetrahydro- 3-isoquinolinecarboxamide as a novel potent and selective opioid kappa receptor antagonist. |
| AID231890 | Compound was tested for antagonist activity against kappa opioid receptor on electrically stimulated guinea pig ileal longitudinal muscle myenteric plexus (GPI) at 100 nM using EK as agonist ligand. | 1991 | Journal of medicinal chemistry, Apr, Volume: 34, Issue:4 | Role of the spacer in conferring kappa opioid receptor selectivity to bivalent ligands related to norbinaltorphimine. |
| AID148013 | Binding affinity against cloned human Opioid receptor kappa 1 transfected into chinese hamster ovary cells using [3H]U-69593 as radioligand | 2003 | Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25 | Guanidino N-substituted and N,N-disubstituted derivatives of the kappa-opioid antagonist GNTI. |
| AID148222 | Antagonist activity on agonist (SNC-80) stimulated [35S]GTP-gamma-S, binding in cloned delta opioid receptors | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | Identification of the first trans-(3R,4R)- dimethyl-4-(3-hydroxyphenyl)piperidine derivative to possess highly potent and selective opioid kappa receptor antagonist activity. |
| AID141513 | The binding affinity against mu-opioid receptor using [3H]- DAMGO as radioligand | 1994 | Journal of medicinal chemistry, May-13, Volume: 37, Issue:10 | Structure-activity relationship of N17'-substituted norbinaltorphimine congeners. Role of the N17' basic group in the interaction with a putative address subsite on the kappa opioid receptor. |
| AID238168 | Antagonist potency towards human delta opioid receptor in [35S]GTP-gamma-S, assay | 2004 | Journal of medicinal chemistry, Oct-07, Volume: 47, Issue:21 | Identification of a new scaffold for opioid receptor antagonism based on the 2-amino-1,1-dimethyl-7-hydroxytetralin pharmacophore. |
| AID311281 | Antagonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S assay | 2007 | Journal of natural products, Aug, Volume: 70, Issue:8 | Flavonoids as opioid receptor ligands: identification and preliminary structure-activity relationships. |
| AID149134 | Binding affinity of compound for Opioid receptor kappa 1 was determined using [3H]U-69593 as radioligand from guinea pig caudate | 2004 | Journal of medicinal chemistry, Feb-12, Volume: 47, Issue:4 | Importance of phenolic address groups in opioid kappa receptor selective antagonists. |
| AID147883 | Inhibition of [35S]GTP-gamma-S, binding in cloned Opioid receptor mu 1 stimulated by DAMGO | 2003 | Journal of medicinal chemistry, May-08, Volume: 46, Issue:10 | 2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy. |
| AID631391 | Selectivity ratio of Kb for human opioid delta receptor expressed in HEK293 cells to Kb for human opioid kappa receptor expressed in CHO cells | 2011 | Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23 | Discovery of aminobenzyloxyarylamides as κ opioid receptor selective antagonists: application to preclinical development of a κ opioid receptor antagonist receptor occupancy tracer. |
| AID128802 | Antagonism of kappa1 opioid agonist (U-50,488)-induced antinociception upon intrathecal administration in mice at a dose of 250 pmol | 2004 | Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12 | A bivalent ligand (KDN-21) reveals spinal delta and kappa opioid receptors are organized as heterodimers that give rise to delta(1) and kappa(2) phenotypes. Selective targeting of delta-kappa heterodimers. |
| AID227093 | Ratio of the IC50 of delta receptor agonist, [D-Ala-2, D-Leu5]-enkephalin in the presence of compound in MVD divided by the control IC50. | 2000 | Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14 | Potent and selective indolomorphinan antagonists of the kappa-opioid receptor. |
| AID234389 | delta/kappa ratio of the compound | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | Identification of the first trans-(3R,4R)- dimethyl-4-(3-hydroxyphenyl)piperidine derivative to possess highly potent and selective opioid kappa receptor antagonist activity. |
| AID1191369 | Antagonist activity at kappa opioid receptor (unknown origin) | 2015 | European journal of medicinal chemistry, Jan-27, Volume: 90 | Novel fluoroalkyl derivatives of selective kappa opioid receptor antagonist JDTic: Design, synthesis, pharmacology and molecular modeling studies. |
| AID502178 | Displacement of [3H]DAMGO from mu opioid receptor in guinea pig forebrain | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17 | Synthesis of pyrrolomorphinan derivatives as kappa opioid agonists. |
| AID747954 | Antagonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Discovery of N-{4-[(3-hydroxyphenyl)-3-methylpiperazin-1-yl]methyl-2-methylpropyl}-4-phenoxybenzamide analogues as selective kappa opioid receptor antagonists. |
| AID261106 | Inhibition of DAMGO stimulated [35S]GTP-gamma-S binding to cloned human mu opioid receptor expressed in CHO cells | 2006 | Journal of medicinal chemistry, Mar-09, Volume: 49, Issue:5 | N-substituted 4beta-methyl-5-(3-hydroxyphenyl)-7alpha-amidomorphans are potent, selective kappa opioid receptor antagonists. |
| AID148215 | Antagonistic activity against cloned human Opioid receptor delta 1 using DPDPE as ligand in [35S]GTP-gamma-S, assay | 2003 | Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25 | Guanidino N-substituted and N,N-disubstituted derivatives of the kappa-opioid antagonist GNTI. |
| AID381431 | Increase of JNK phosphorylation in mouse spinal cord at 10 mg/kg, ip 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. |
| AID148833 | Antagonist activity was evaluated in the guinea pig ileum assay against U50,488- selective agonist of opioid receptor kappa 1 | 2001 | Journal of medicinal chemistry, Sep-13, Volume: 44, Issue:19 | [2',6'-Dimethyltyrosine]dynorphin A(1-11)-NH2 analogues lacking an N-terminal amino group: potent and selective kappa opioid antagonists. |
| AID128808 | Antagonism of kappa2 opioid agonist (bremazocine)-induced antinociception upon intrathecal administration in mice at a dose of 250 pmol | 2004 | Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12 | A bivalent ligand (KDN-21) reveals spinal delta and kappa opioid receptors are organized as heterodimers that give rise to delta(1) and kappa(2) phenotypes. Selective targeting of delta-kappa heterodimers. |
| AID148704 | Opioid antagonist potency, determined in the guinea pig ileum (GPI) preparation, by employing EK (kappa-opioid) as agonist, expressed as IC50 ratio (tested at 20 nM) | 2001 | Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13 | Transformation of a kappa-opioid receptor antagonist to a kappa-agonist by transfer of a guanidinium group from the 5'- to 6'-position of naltrindole. |
| AID150975 | In vitro binding affinity to human Opioid receptor mu 1 on CHO cell membranes using [3H]diprenorphine displacement. | 2003 | Journal of medicinal chemistry, May-22, Volume: 46, Issue:11 | Structure-activity relationships of dynorphin a analogues modified in the address sequence. |
| AID381426 | Displacement of [3H]U69,593 from kappa opioid receptor in mouse brain tissue | 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. |
| AID148240 | Binding affinity towards cloned human Opioid receptor delta 1 in CHO cell membranes. | 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. |
| AID227211 | Ratio of the IC50 of mu receptor agonist, Morphine in the presence of compound in GPI divided by the control IC50. | 2000 | Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14 | Potent and selective indolomorphinan antagonists of the kappa-opioid receptor. |
| AID234513 | Selectivity of compound for mu opioid receptor to that of kappa opioid receptor in guinea pig caudate membranes | 2004 | Journal of medicinal chemistry, Feb-12, Volume: 47, Issue:4 | Importance of phenolic address groups in opioid kappa receptor selective antagonists. |
| AID574378 | Displacement of [3H]NTI from delta opioid receptor in guinea pig forebrain | 2011 | Bioorganic & medicinal chemistry, Feb-01, Volume: 19, Issue:3 | Synthesis of 6,14-epoxymorphinan derivatives and their pharmacologies. |
| AID148957 | Binding affinity of compound was measured against Opioid receptor kappa 1 on electrically stimulated guinea pig ileal longitudinal muscle myenteric plexus (GPI) at 100 nM preparation using EK as agonist | 1991 | Journal of medicinal chemistry, Apr, Volume: 34, Issue:4 | Role of the spacer in conferring kappa opioid receptor selectivity to bivalent ligands related to norbinaltorphimine. |
| AID239230 | Inhibition of [3H]diprenorphine binding to rat Opioid receptor delta 1 expressed in C6 cells | 2005 | Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5 | Major effect of pyrrolic N-benzylation in norbinaltorphimine, the selective kappa-opioid receptor antagonist. |
| AID631364 | Antagonist activity at human opioid kappa receptor expressed in CHO cells assessed as inhibition of U69593-induced [35S]GTP-gamma-S binding after 4 hrs by scintillation counting | 2011 | Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23 | Discovery of aminobenzyloxyarylamides as κ opioid receptor selective antagonists: application to preclinical development of a κ opioid receptor antagonist receptor occupancy tracer. |
| AID229386 | Selectivity ratio of delta opioid receptor to that of kappa opioid receptor | 1994 | Journal of medicinal chemistry, May-13, Volume: 37, Issue:10 | Structure-activity relationship of N17'-substituted norbinaltorphimine congeners. Role of the N17' basic group in the interaction with a putative address subsite on the kappa opioid receptor. |
| AID147987 | Displacement of [3H]U-69593 from human recombinant Opioid receptor kappa 1 on CHO cell membranes. | 2003 | Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8 | 14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles. |
| AID148923 | Binding affinity of compound was measured against Opioid receptor delta 1 in mouse vas deferens (MVD) smooth muscle preparation at 100 nM using DADLE as standard agonist | 1991 | Journal of medicinal chemistry, Apr, Volume: 34, Issue:4 | Role of the spacer in conferring kappa opioid receptor selectivity to bivalent ligands related to norbinaltorphimine. |
| AID148097 | Ability to displace DPDPE from human recombinant Opioid receptor delta 1 in CHO cells using [35S]- GTP-gamma S Assay | 2003 | Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2 | The role of the side chain in determining relative delta- and kappa-affinity in C5'-substituted analogues of naltrindole. |
| AID1181414 | Displacement of [3H]DAMGO from human recombinant mu opioid receptor expressed in CHO cell membranes after 60 mins by scintillation counting method | 2014 | Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15 | Pyrrolo- and pyridomorphinans: non-selective opioid antagonists and delta opioid agonists/mu opioid partial agonists. |
| AID148832 | Antagonist activity was evaluated in the guinea pig ileum assay against Dyn A(1-13)-selective agonist of opioid receptor kappa 1 | 2001 | Journal of medicinal chemistry, Sep-13, Volume: 44, Issue:19 | [2',6'-Dimethyltyrosine]dynorphin A(1-11)-NH2 analogues lacking an N-terminal amino group: potent and selective kappa opioid antagonists. |
| AID127053 | Compound was evaluated for antinociceptive activity in mouse; IA means inactive | 2000 | Bioorganic & medicinal chemistry letters, Nov-06, Volume: 10, Issue:21 | N-Cyclohexylethyl-N-noroxymorphindole: a mu-opioid preferring analogue of naltrindole. |
| AID149081 | Binding affinity was measured on delta opioid receptor | 2001 | Journal of medicinal chemistry, Sep-13, Volume: 44, Issue:19 | [2',6'-Dimethyltyrosine]dynorphin A(1-11)-NH2 analogues lacking an N-terminal amino group: potent and selective kappa opioid antagonists. |
| AID229507 | Ratio of IC50 in the presence of morphine to that of control IC50 in guinea pig ileum at 20 nM | 1988 | Journal of medicinal chemistry, Jul, Volume: 31, Issue:7 | Only one pharmacophore is required for the kappa opioid antagonist selectivity of norbinaltorphimine. |
| AID230648 | Ki ratio measured as the ke values of Opioid receptor delta 1/Opioid receptor kappa 1 from guinea pig brain membranes. | 1991 | Journal of medicinal chemistry, Apr, Volume: 34, Issue:4 | Role of the spacer in conferring kappa opioid receptor selectivity to bivalent ligands related to norbinaltorphimine. |
| AID232139 | Ratio of (Ki) delta-opioid receptor to that of (Ki) kappa-opioid receptor | 2003 | Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25 | Guanidino N-substituted and N,N-disubstituted derivatives of the kappa-opioid antagonist GNTI. |
| AID613641 | Displacement of [3H]diprenorphine from human kappa opioid receptor expressed in CHO cells after 1 hr by liquid scintillation counting | 2011 | Journal of medicinal chemistry, Aug-25, Volume: 54, Issue:16 | Design and discovery of a selective small molecule κ opioid antagonist (2-methyl-N-((2'-(pyrrolidin-1-ylsulfonyl)biphenyl-4-yl)methyl)propan-1-amine, PF-4455242). |
| AID502180 | Selectivity ratio of Ki for mu opioid receptor in guinea pig forebrain to Ki for kappa opioid receptor in guinea pig cerebellum | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17 | Synthesis of pyrrolomorphinan derivatives as kappa opioid agonists. |
| AID150830 | Ability to displace DAMGO from human recombinant Opioid receptor mu 1 in CHO cells using [35S]- GTP-gamma S Assay | 2003 | Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2 | The role of the side chain in determining relative delta- and kappa-affinity in C5'-substituted analogues of naltrindole. |
| AID631348 | Selectivity ratio of Kb for human opioid mu receptor expressed in CHO cells to Kb for human opioid kappa receptor expressed in CHO cells | 2011 | Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23 | Discovery of aminobenzyloxyarylamides as κ opioid receptor selective antagonists: application to preclinical development of a κ opioid receptor antagonist receptor occupancy tracer. |
| AID296740 | Antagonist activity at human kappa opioid receptor expressed in CHO cells by [35S]GTP-gamma-S assay | 2007 | Journal of medicinal chemistry, Aug-09, Volume: 50, Issue:16 | Probes for narcotic receptor mediated phenomena. 34. Synthesis and structure-activity relationships of a potent mu-agonist delta-antagonist and an exceedingly potent antinociceptive in the enantiomeric C9-substituted 5-(3-hydroxyphenyl)-N-phenylethylmorph |
| AID747947 | Selectivity ratio of Ke for human mu opioid receptor to Ke for human kappa opioid receptor | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Discovery of N-{4-[(3-hydroxyphenyl)-3-methylpiperazin-1-yl]methyl-2-methylpropyl}-4-phenoxybenzamide analogues as selective kappa opioid receptor antagonists. |
| AID240317 | Agonist activity against Opioid receptor mu 1 expressed in C6 cells in [35S]-GTP-gamma S assay; No stimulation up to 10000 nM | 2005 | Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5 | Major effect of pyrrolic N-benzylation in norbinaltorphimine, the selective kappa-opioid receptor antagonist. |
| AID148938 | Opioid antagonist potencies against Opioid receptor delta 1 from mouse vas-deferens preparation employing [D-Ala2,D-Leu5]enkephalin (DADLE) as agonist. | 1998 | Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25 | Mutational evidence for a common kappa antagonist binding pocket in the wild-type kappa and mutant mu[K303E] opioid receptors. |
| AID148990 | Antagonist activity on agonist stimulated [35S]GTP-gamma-S, binding in guinea pig caudate membranes (10 uM U69,593 as the agonist ligand for kappa-receptor) | 2003 | Bioorganic & medicinal chemistry letters, Feb-10, Volume: 13, Issue:3 | Synthesis, opioid receptor binding, and functional activity of 5'-substituted 17-cyclopropylmethylpyrido[2',3':6,7]morphinans. |
| AID150016 | Antagonistic activity at Opioid receptor mu 1 in electrically stimulated Guinea pig ileum using morphine as the agonist at 20 nM | 1988 | Journal of medicinal chemistry, Jul, Volume: 31, Issue:7 | Only one pharmacophore is required for the kappa opioid antagonist selectivity of norbinaltorphimine. |
| AID1536327 | Antinociceptive activity in Kunming mouse model of thermal-induced nociception assessed as increase in latency to tail withdrawal at 10 nmol, icv measured up to 60 mins by tail flick test | |||
| AID229397 | Selectivity ratio of kappa opioid receptor to that of delta opioid receptor | 1994 | Journal of medicinal chemistry, May-13, Volume: 37, Issue:10 | Structure-activity relationship of N17'-substituted norbinaltorphimine congeners. Role of the N17' basic group in the interaction with a putative address subsite on the kappa opioid receptor. |
| AID631362 | Selectivity ratio of Ki for human opioid mu receptor expressed in CHO cells to Ki for human opioid kappa receptor expressed in CHO cells | 2011 | Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23 | Discovery of aminobenzyloxyarylamides as κ opioid receptor selective antagonists: application to preclinical development of a κ opioid receptor antagonist receptor occupancy tracer. |
| AID148706 | Ratio of IC50 of ethylketazocine (EK) in the presence (100 nM) to that of ethylketazocine (EK) alone, against kappa opioid receptor in Guinea pig ileum preparation | 1993 | Journal of medicinal chemistry, Jan-08, Volume: 36, Issue:1 | A remarkable change of opioid receptor selectivity on the attachment of a peptidomimetic kappa address element to the delta antagonist, natrindole: 5'-[N2-alkylamidino)methyl]naltrindole derivatives as a novel class of kappa opioid receptor antagonists. |
| AID1245411 | Selectivity ratio of Ke for cloned human mu opioid receptor to Ke for cloned human kappa opioid receptor | 2015 | Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19 | Design, synthesis, and pharmacological evaluation of JDTic analogs to examine the significance of the 3- and 4-methyl substituents. |
| AID148153 | Agonist activity towards human Opioid receptor kappa 1 mediated [35S]GTP-gamma-S, binding calculated as maximum stimulation | 2003 | Journal of medicinal chemistry, May-22, Volume: 46, Issue:11 | Structure-activity relationships of dynorphin a analogues modified in the address sequence. |
| AID296545 | Displacement of [3H]diprenorphine from human recombinant kappa opioid receptor expressed in in CHO cells | 2007 | Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13 | Synthesis and biological activity of nociceptin/orphanin FQ analogues substituted in position 7 or 11 with Calpha,alpha-dialkylated amino acids. |
| AID231486 | Ratio between Kappa receptor, Mu receptor and Delta receptor determined with U50, 488 as k Antagonist; 1/123/44 | 2001 | Journal of medicinal chemistry, Sep-13, Volume: 44, Issue:19 | [2',6'-Dimethyltyrosine]dynorphin A(1-11)-NH2 analogues lacking an N-terminal amino group: potent and selective kappa opioid antagonists. |
| AID233292 | Selectivity ratio is IC50 value of kappa-opioid receptor to that of mu-opioid receptor | 1993 | Journal of medicinal chemistry, Jan-08, Volume: 36, Issue:1 | A remarkable change of opioid receptor selectivity on the attachment of a peptidomimetic kappa address element to the delta antagonist, natrindole: 5'-[N2-alkylamidino)methyl]naltrindole derivatives as a novel class of kappa opioid receptor antagonists. |
| AID148006 | In vitro binding affinity towards human Opioid receptor kappa 1 on CHO cell membranes using [3H]diprenorphine displacement. | 2003 | Journal of medicinal chemistry, May-22, Volume: 46, Issue:11 | Structure-activity relationships of dynorphin a analogues modified in the address sequence. |
| AID148993 | Inhibition of opioid receptor mu by displacing 1 nM [3H]DAGO in guinea pig brain membrane | 1992 | Journal of medicinal chemistry, Nov-27, Volume: 35, Issue:24 | O3-(2-carbomethoxyallyl) ethers of opioid ligands derived from oxymorphone, naltrexone, etorphine, diprenorphine, norbinaltorphimine, and naltrindole. Unexpected O3-dealkylation in the opioid radioligand displacement assay. |
| AID1350689 | Antagonist activity at human KOR expressed in CHO cell membranes assessed as inhibition of U50488-induced [35S]-GTPgammaS binding preincubated for 5 mins followed by U50488 and [35S]-GTPgammaS addition measured after 80 mins | 2018 | Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14 | Synthesis and Evaluation of a Novel Bivalent Selective Antagonist for the Mu-Delta Opioid Receptor Heterodimer that Reduces Morphine Withdrawal in Mice. |
| AID1191371 | Selectivity ratio of Ki for delta opioid receptor (unknown origin) to Ki for kappa opioid receptor (unknown origin) | 2015 | European journal of medicinal chemistry, Jan-27, Volume: 90 | Novel fluoroalkyl derivatives of selective kappa opioid receptor antagonist JDTic: Design, synthesis, pharmacology and molecular modeling studies. |
| AID1181416 | Displacement of [3H]Cl-DPDPE from human recombinant delta opioid receptor expressed in CHO cell membranes after 60 mins by scintillation counting method | 2014 | Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15 | Pyrrolo- and pyridomorphinans: non-selective opioid antagonists and delta opioid agonists/mu opioid partial agonists. |
| AID229396 | Selectivity ratio of kappa opioid receptor to that of mu opioid receptor | 1994 | Journal of medicinal chemistry, May-13, Volume: 37, Issue:10 | Structure-activity relationship of N17'-substituted norbinaltorphimine congeners. Role of the N17' basic group in the interaction with a putative address subsite on the kappa opioid receptor. |
| AID149765 | Antagonist activity on agonist stimulated [35S]GTP-gamma-S, binding in guinea pig caudate membranes (10 uM SNC-80 as the agonist ligand for delta-receptor) | 2003 | Bioorganic & medicinal chemistry letters, Feb-10, Volume: 13, Issue:3 | Synthesis, opioid receptor binding, and functional activity of 5'-substituted 17-cyclopropylmethylpyrido[2',3':6,7]morphinans. |
| AID229497 | Ratio of IC50 DADLE and antagonist binding to delta opioid receptor | 1988 | Journal of medicinal chemistry, Apr, Volume: 31, Issue:4 | Binaltorphimine-related bivalent ligands and their kappa opioid receptor antagonist selectivity. |
| AID150024 | Antagonistic activity against DAMGO and guinea pig caudate Opioid receptor mu 1 in [35S]GTP-gamma-S, assay | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 | Identification of (3R)-7-hydroxy-N-((1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)- 3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl)-1,2,3,4-tetrahydro- 3-isoquinolinecarboxamide as a novel potent and selective opioid kappa receptor antagonist. |
| AID232696 | Selectivity ratio of Ki at mu opioid receptor to Ki at kappa opioid receptor | 2002 | Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16 | Discovery of an opioid kappa receptor selective pure antagonist from a library of N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphans. |
| AID151283 | Binding affinity of compound for Opioid receptor mu 1 was determined using [3H]DAMGO as radioligand from rat brain tissue | 2004 | Journal of medicinal chemistry, Feb-12, Volume: 47, Issue:4 | Importance of phenolic address groups in opioid kappa receptor selective antagonists. |
| AID148972 | Opioid antagonist potencies against Opioid receptor kappa 1 from guinea pig ileum employing ethylketazocine (EKC) as agonist. | 1998 | Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25 | Mutational evidence for a common kappa antagonist binding pocket in the wild-type kappa and mutant mu[K303E] opioid receptors. |
| AID229883 | Selectivity ratio, ratio of binding affinity of mu to kappa opioid receptor | 2000 | Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14 | Potent and selective indolomorphinan antagonists of the kappa-opioid receptor. |
| AID148845 | Inhibition of U69,593 antagonistic activity in [35S]GTP-gamma-S, assay against guinea pig Opioid receptor kappa 1 | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 | Identification of (3R)-7-hydroxy-N-((1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)- 3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl)-1,2,3,4-tetrahydro- 3-isoquinolinecarboxamide as a novel potent and selective opioid kappa receptor antagonist. |
| AID233597 | Ratio of Ke value to kappa receptor to that of mu receptor | 1998 | Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25 | Mutational evidence for a common kappa antagonist binding pocket in the wild-type kappa and mutant mu[K303E] opioid receptors. |
| AID226663 | Antagonist activity determined in the [35S]GTP-gamma-S, binding assay relative to 25 nM [D-Ala3] Dyn A (1-11)-NH2. | 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. |
| AID148597 | Mutant factor against mu-[K303E] with Opioid receptor kappa 1 for binding affinity | 1998 | Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25 | Mutational evidence for a common kappa antagonist binding pocket in the wild-type kappa and mutant mu[K303E] opioid receptors. |
| AID231485 | Ratio between Kappa receptor, Mu receptor and Delta receptor determined with Dyn A (1-13)as k Antagonist; 1/71/25 | 2001 | Journal of medicinal chemistry, Sep-13, Volume: 44, Issue:19 | [2',6'-Dimethyltyrosine]dynorphin A(1-11)-NH2 analogues lacking an N-terminal amino group: potent and selective kappa opioid antagonists. |
| AID1181415 | Displacement of [3H]U69593 from human recombinant kappa opioid receptor expressed in CHO cell membranes after 60 mins by scintillation counting method | 2014 | Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15 | Pyrrolo- and pyridomorphinans: non-selective opioid antagonists and delta opioid agonists/mu opioid partial agonists. |
| AID238173 | Antagonistic activity against rat opioid receptor mu 1 expressed in C6 cells in [35S]GTP gamma S assay | 2005 | Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5 | Major effect of pyrrolic N-benzylation in norbinaltorphimine, the selective kappa-opioid receptor antagonist. |
| AID574381 | Selectivity ratio of Ki for delta opioid receptor in guinea pig forebrain to Ki for mu opioid receptor in guinea pig forebrain | 2011 | Bioorganic & medicinal chemistry, Feb-01, Volume: 19, Issue:3 | Synthesis of 6,14-epoxymorphinan derivatives and their pharmacologies. |
| AID613672 | Displacement of [3H]diprenorphine from human delta opioid receptor expressed in CHO cells after 1 hr by liquid scintillation counting | 2011 | Journal of medicinal chemistry, Aug-25, Volume: 54, Issue:16 | Design and discovery of a selective small molecule κ opioid antagonist (2-methyl-N-((2'-(pyrrolidin-1-ylsulfonyl)biphenyl-4-yl)methyl)propan-1-amine, PF-4455242). |
| AID150833 | Antagonistic activity against cloned human Opioid receptor mu 1 using DAMGO as ligand in [35S]GTP-gamma-S, assay | 2003 | Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25 | Guanidino N-substituted and N,N-disubstituted derivatives of the kappa-opioid antagonist GNTI. |
| AID149779 | Binding affinity determined on Opioid receptor delta 1 in Guinea pig brain membranes using radioligand [3H]DADLE | 1998 | Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26 | Identification of an opioid kappa receptor subtype-selective N-substituent for (+)-(3R,4R)-dimethyl-4-(3-hydroxyphenyl)piperidine. |
| AID413923 | Antagonist activity at human kappa opioid receptor expressed in CHO cells assessed as inhibition of U50,488-induced [35S]GTPgammaS binding | 2008 | Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24 | Probes for narcotic receptor mediated phenomena. 37. Synthesis and opioid binding affinity of the final pair of oxide-bridged phenylmorphans, the ortho- and para-b-isomers and their N-phenethyl analogues, and the synthesis of the N-phenethyl analogues of |
| AID151124 | Binding affinity using [3H]diprenorphine as the radioligand against wild-type Opioid receptor mu 1 in COS-7 cells | 2000 | Journal of medicinal chemistry, Apr-20, Volume: 43, Issue:8 | Binding of norbinaltorphimine (norBNI) congeners to wild-type and mutant mu and kappa opioid receptors: molecular recognition loci for the pharmacophore and address components of kappa antagonists. |
| AID148099 | Ability to inhibit stimulation of [35S]GTP-gamma-S, binding in cloned human Opioid receptor delta 1 transfected in CHO cells using C1-DPDPE as radioligand | 2002 | Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16 | Discovery of an opioid kappa receptor selective pure antagonist from a library of N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphans. |
| AID148010 | Binding affinity towards cloned human Opioid receptor kappa 1 in CHO cell membranes. | 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. |
| AID234510 | Selectivity of compound for delta opioid receptor to that of kappa opioid receptor | 2004 | Journal of medicinal chemistry, Feb-12, Volume: 47, Issue:4 | Importance of phenolic address groups in opioid kappa receptor selective antagonists. |
| AID148841 | Antagonistic activity for Opioid receptor kappa 1 of guinea pig ileal longitudinal muscle at 100 nM | 1988 | Journal of medicinal chemistry, Apr, Volume: 31, Issue:4 | Binaltorphimine-related bivalent ligands and their kappa opioid receptor antagonist selectivity. |
| AID239386 | Inhibition of [3H]U-69593 binding to human kappa opioid receptor expressed in CHO cells | 2004 | Journal of medicinal chemistry, Oct-07, Volume: 47, Issue:21 | Identification of a new scaffold for opioid receptor antagonism based on the 2-amino-1,1-dimethyl-7-hydroxytetralin pharmacophore. |
| AID148151 | Agonist activity towards human Opioid receptor kappa 1 mediated [35S]GTP-gamma-S, binding calculated as maximum inhibition | 2003 | Journal of medicinal chemistry, May-22, Volume: 46, Issue:11 | Structure-activity relationships of dynorphin a analogues modified in the address sequence. |
| AID105934 | Maximal inhibition of compound was measured on Mouse vas deferens(MVD) preparation | 1991 | Journal of medicinal chemistry, Apr, Volume: 34, Issue:4 | Role of the spacer in conferring kappa opioid receptor selectivity to bivalent ligands related to norbinaltorphimine. |
| AID311284 | Selectivity for antagonist activity at human delta opioid receptor to kappa opioid receptor expressed in CHO cells by [35S]GTP-gamma-S assay | 2007 | Journal of natural products, Aug, Volume: 70, Issue:8 | Flavonoids as opioid receptor ligands: identification and preliminary structure-activity relationships. |
| AID148070 | Stimulation of [35S]GTP-gamma-S, binding at human recombinant Opioid receptor delta 1 transfected into CHO cells. | 2003 | Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8 | 14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles. |
| AID148176 | Binding affinity using [3H]diprenorphine as the radioligand against E297K mutant Opioid receptor kappa 1 in COS-7 cells | 2000 | Journal of medicinal chemistry, Apr-20, Volume: 43, Issue:8 | Binding of norbinaltorphimine (norBNI) congeners to wild-type and mutant mu and kappa opioid receptors: molecular recognition loci for the pharmacophore and address components of kappa antagonists. |
| AID150033 | Inhibition of [35S]GTP-gamma-S, binding from Opioid receptor delta 1 in Guinea pig Caudate stimulated by SNC80 | 1998 | Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26 | Identification of an opioid kappa receptor subtype-selective N-substituent for (+)-(3R,4R)-dimethyl-4-(3-hydroxyphenyl)piperidine. |
| AID150042 | The binding affinity on delta-opioid receptor using [3H]- DPDPE as radioligand | 1994 | Journal of medicinal chemistry, May-13, Volume: 37, Issue:10 | Structure-activity relationship of N17'-substituted norbinaltorphimine congeners. Role of the N17' basic group in the interaction with a putative address subsite on the kappa opioid receptor. |
| AID233596 | Ratio of Ke value to kappa receptor to that of delta receptor | 1998 | Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25 | Mutational evidence for a common kappa antagonist binding pocket in the wild-type kappa and mutant mu[K303E] opioid receptors. |
| AID234512 | Selectivity of compound for mu opioid receptor to that of kappa opioid receptor | 2004 | Journal of medicinal chemistry, Feb-12, Volume: 47, Issue:4 | Importance of phenolic address groups in opioid kappa receptor selective antagonists. |
| AID410719 | Displacement of [3H]Naltrindole form human delta opioid receptor expressed in CHO cells | 2009 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 19, Issue:1 | Syntheses and opioid receptor binding properties of carboxamido-substituted opioids. |
| AID381435 | Increase in JNK phosphorylation in pertussis toxin treated HEK293 cells expressing GFP tagged kappa opioid receptor 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. |
| AID410720 | Displacement of [3H]U69593 form human kappa opioid receptor expressed in CHO cells | 2009 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 19, Issue:1 | Syntheses and opioid receptor binding properties of carboxamido-substituted opioids. |
| AID442694 | Ratio of Ke for human cloned mu opioid receptor to Ke for human cloned kappa opioid receptor | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23 | Synthesis and in vitro opioid receptor functional antagonism of methyl-substituted analogues of (3R)-7-hydroxy-N-[(1S)-1-{[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl}-2-methylpropyl]-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide (JDTic). |
| AID149630 | Inhibition of Opioid receptor delta 1 by displacing 1 nM [3H]DPDPE in guinea pig brain membrane | 1992 | Journal of medicinal chemistry, Nov-27, Volume: 35, Issue:24 | O3-(2-carbomethoxyallyl) ethers of opioid ligands derived from oxymorphone, naltrexone, etorphine, diprenorphine, norbinaltorphimine, and naltrindole. Unexpected O3-dealkylation in the opioid radioligand displacement assay. |
| AID631365 | Antagonist activity at human opioid mu receptor expressed in CHO cells assessed as inhibition of DAMGO-induced [35S]GTP-gamma-S binding after 4 hrs by scintillation counting | 2011 | Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23 | Discovery of aminobenzyloxyarylamides as κ opioid receptor selective antagonists: application to preclinical development of a κ opioid receptor antagonist receptor occupancy tracer. |
| AID149675 | Binding affinity on HEK293 cells transiently transfected with plasmids encoding the rat Opioid receptor delta 1 | 2000 | Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14 | Potent and selective indolomorphinan antagonists of the kappa-opioid receptor. |
| AID147960 | Inhibition of opioid receptor kappa by displacing 0.5 nM [3H]bremazocine in guinea pig brain membrane | 1992 | Journal of medicinal chemistry, Nov-27, Volume: 35, Issue:24 | O3-(2-carbomethoxyallyl) ethers of opioid ligands derived from oxymorphone, naltrexone, etorphine, diprenorphine, norbinaltorphimine, and naltrindole. Unexpected O3-dealkylation in the opioid radioligand displacement assay. |
| AID147887 | Opioid antagonist potencies against Opioid receptor mu 1 from guinea pig ileum employing morphine(M) as agonist. | 1998 | Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25 | Mutational evidence for a common kappa antagonist binding pocket in the wild-type kappa and mutant mu[K303E] opioid receptors. |
| AID77794 | Functional antagonism was obtained by the ability of compound to inhibit stimulation of [35S]GTP gamma S binding produced by selective agonists U69,593 in guinea pig caudate membranes | 2004 | Journal of medicinal chemistry, Feb-12, Volume: 47, Issue:4 | Importance of phenolic address groups in opioid kappa receptor selective antagonists. |
| AID482618 | Intrinsic activity at human recombinant delta opioid receptor expressed in CHO cells up to 10 uM | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Analogues of (3R)-7-hydroxy-N-[(1S)-1-{[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl}-2-methylpropyl)-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide (JDTic). Synthesis and in vitro and in vivo opioid receptor antagonist activity. |
| AID1232255 | Antagonist activity against human kappa opioid receptor expressed in human U2OS cells co-expressing beta-arrestin2 pre-treated for 15 mins before U69,593 stimulation for 90 mins by DiscoveRx beta-arrestin2 recruitment based PathHunter assay | 2015 | Bioorganic & medicinal chemistry, Jul-15, Volume: 23, Issue:14 | Potency enhancement of the κ-opioid receptor antagonist probe ML140 through sulfonamide constraint utilizing a tetrahydroisoquinoline motif. |
| AID149437 | Inhibition of stimulation of [35S]GTP-gamma-S, binding produced by the selective agonist (U69593, kappa-receptor), in guinea pig caudate membranes | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | Identification of the first trans-(3R,4R)- dimethyl-4-(3-hydroxyphenyl)piperidine derivative to possess highly potent and selective opioid kappa receptor antagonist activity. |
| AID149759 | Inhibition of [35S]GTP-gamma-S, binding in cloned Opioid receptor delta 1 stimulated by SNC-80 | 2003 | Journal of medicinal chemistry, May-08, Volume: 46, Issue:10 | 2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy. |
| AID152388 | Displacement of [3H]- diprenorphine from mu-W318A-receptor expressed in HEK 293 cells | 2001 | Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6 | Investigation of the selectivity of oxymorphone- and naltrexone-derived ligands via site-directed mutagenesis of opioid receptors: exploring the "address" recognition locus. |
| AID229500 | Ratio of IC50 morphine and antagonist binding to opioid receptor | 1988 | Journal of medicinal chemistry, Apr, Volume: 31, Issue:4 | Binaltorphimine-related bivalent ligands and their kappa opioid receptor antagonist selectivity. |
| AID147881 | Inhibition of [35S]GTP-gamma-S, binding in cloned human Opioid receptor kappa 1 stimulated by U69, 593 | 2003 | Journal of medicinal chemistry, May-08, Volume: 46, Issue:10 | 2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy. |
| AID229505 | Ratio of IC50 in the presence of ethylketazocine to that of control IC50 in guinea pig ileum at 20 nM | 1988 | Journal of medicinal chemistry, Jul, Volume: 31, Issue:7 | Only one pharmacophore is required for the kappa opioid antagonist selectivity of norbinaltorphimine. |
| AID152381 | Binding affinity to mu-opioid receptor of rat brain using [3H]DAMGO as radioligand | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | Identification of the first trans-(3R,4R)- dimethyl-4-(3-hydroxyphenyl)piperidine derivative to possess highly potent and selective opioid kappa receptor antagonist activity. |
| AID381432 | Increase of JNK phosphorylation in mouse striatum at 10 mg/kg, ip 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. |
| AID149760 | Inhibition of [35S]GTP-gamma-S, binding in guines pig caudate stimulated by SNC-80 for Opioid receptor delta 1 | 2003 | Journal of medicinal chemistry, May-08, Volume: 46, Issue:10 | 2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy. |
| AID148840 | Antagonistic activity at Opioid receptor kappa 1 in electrically stimulated Guinea pig ileum using ethylketazocine as the agonist at 20 nM concentration | 1988 | Journal of medicinal chemistry, Jul, Volume: 31, Issue:7 | Only one pharmacophore is required for the kappa opioid antagonist selectivity of norbinaltorphimine. |
| AID148217 | Inhibition of [35S]GTP-gamma-S, binding in cloned human Opioid receptor delta 1 stimulated by DPDPE | 2003 | Journal of medicinal chemistry, May-08, Volume: 46, Issue:10 | 2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy. |
| AID226813 | Ratio of antagonist activities at mu versus delta receptors | 2003 | Bioorganic & medicinal chemistry letters, Feb-10, Volume: 13, Issue:3 | Synthesis, opioid receptor binding, and functional activity of 5'-substituted 17-cyclopropylmethylpyrido[2',3':6,7]morphinans. |
| AID148939 | Opioid antagonist potency, determined in mouse vas deferens (MVD) preparation, using DADLE (delta-opioid) as agonist (Ke=antagonist/IC50 ratio -1) | 2001 | Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13 | Transformation of a kappa-opioid receptor antagonist to a kappa-agonist by transfer of a guanidinium group from the 5'- to 6'-position of naltrindole. |
| AID148587 | Displacement of [3H]diprenorphine from opioid receptor kappa 1 expressed in HEK 293 cells | 2001 | Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6 | Investigation of the selectivity of oxymorphone- and naltrexone-derived ligands via site-directed mutagenesis of opioid receptors: exploring the "address" recognition locus. |
| AID232040 | Selectivity between mu receptor and kappa receptor | 2003 | Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2 | The role of the side chain in determining relative delta- and kappa-affinity in C5'-substituted analogues of naltrindole. |
| AID150841 | Displacement of [3H]DAMGO from human recombinant Opioid receptor mu 1 on CHO cell membranes. | 2003 | Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8 | 14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles. |
| AID238169 | Antagonist potency towards human kappa opioid receptor in [35S]GTP-gamma-S, assay | 2004 | Journal of medicinal chemistry, Oct-07, Volume: 47, Issue:21 | Identification of a new scaffold for opioid receptor antagonism based on the 2-amino-1,1-dimethyl-7-hydroxytetralin pharmacophore. |
| AID148331 | Percent stimulation of [35S]GTP-gamma-S, binding in recombinant human Opioid receptor mu 1 transfected into CHO cells: Antagonist activity | 2003 | Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8 | 14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles. |
| AID232066 | Compound was tested for antagonist activity against mu opioid receptor on electrically stimulated guinea pig ileal longitudinal muscle myenteric plexus (GPI) at 100 nM using DAMGO as agonist ligand. | 1991 | Journal of medicinal chemistry, Apr, Volume: 34, Issue:4 | Role of the spacer in conferring kappa opioid receptor selectivity to bivalent ligands related to norbinaltorphimine. |
| AID148583 | Displacement of [3H]diprenorphine from delta-W284E-receptor expressed in HEK 293 cells | 2001 | Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6 | Investigation of the selectivity of oxymorphone- and naltrexone-derived ligands via site-directed mutagenesis of opioid receptors: exploring the "address" recognition locus. |
| AID234511 | Selectivity of compound for delta opioid receptor to that of kappa opioid receptor in guinea pig caudate membranes | 2004 | Journal of medicinal chemistry, Feb-12, Volume: 47, Issue:4 | Importance of phenolic address groups in opioid kappa receptor selective antagonists. |
| AID148016 | Compound was evaluated for its binding affinity by displacing [3H]U-69593 to human cloned Kappa opioid receptor transfected into CHO cells using [35S]GTP-gamma-S, assay | 2000 | Bioorganic & medicinal chemistry letters, Oct-16, Volume: 10, Issue:20 | Selective kappa-opioid antagonists related to naltrindole. Effect of side-chain spacer in the 5'-amidinoalkyl series. |
| AID151123 | Binding affinity using [3H]diprenorphine as the radioligand against K303E Opioid receptor mu 1 in COS-7 cells | 2000 | Journal of medicinal chemistry, Apr-20, Volume: 43, Issue:8 | Binding of norbinaltorphimine (norBNI) congeners to wild-type and mutant mu and kappa opioid receptors: molecular recognition loci for the pharmacophore and address components of kappa antagonists. |
| AID574377 | Displacement of [3H]DAMGO from mu opioid receptor in guinea pig forebrain | 2011 | Bioorganic & medicinal chemistry, Feb-01, Volume: 19, Issue:3 | Synthesis of 6,14-epoxymorphinan derivatives and their pharmacologies. |
| 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. |
| AID233094 | Ratio of antagonistic activity for delta and kappa receptors | 1988 | Journal of medicinal chemistry, Apr, Volume: 31, Issue:4 | Binaltorphimine-related bivalent ligands and their kappa opioid receptor antagonist selectivity. |
| AID311280 | Antagonist activity at human kappa opioid receptor expressed in CHO cells by [35S]GTP-gamma-S assay | 2007 | Journal of natural products, Aug, Volume: 70, Issue:8 | Flavonoids as opioid receptor ligands: identification and preliminary structure-activity relationships. |
| AID152222 | Antagonist activity was evaluated in the guinea pig ileum assay against TAPP-selective agonist of Mu receptor | 2001 | Journal of medicinal chemistry, Sep-13, Volume: 44, Issue:19 | [2',6'-Dimethyltyrosine]dynorphin A(1-11)-NH2 analogues lacking an N-terminal amino group: potent and selective kappa opioid antagonists. |
| AID148898 | Antinociceptive activity was determined in vivo in all opioid type tests, expressed as AD50 administered subcutaneously | 2000 | Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26 | Synthesis and in vitro and in vivo activity of (-)-(1R,5R,9R)- and (+)-(1S,5S,9S)-N-alkenyl-, -N-alkynyl-, and -N-cyanoalkyl-5, 9-dimethyl-2'-hydroxy-6,7-benzomorphan homologues. |
| AID149125 | Binding affinity determined on Opioid receptor kappa 1 in Guinea pig brain membranes using radioligand [3H]U-69593 | 1998 | Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26 | Identification of an opioid kappa receptor subtype-selective N-substituent for (+)-(3R,4R)-dimethyl-4-(3-hydroxyphenyl)piperidine. |
| AID149250 | Binding affinity of compound for opioid receptor delta 1 was determined using [3H]DADLE as radioligand from rat brain tissue | 2004 | Journal of medicinal chemistry, Feb-12, Volume: 47, Issue:4 | Importance of phenolic address groups in opioid kappa receptor selective antagonists. |
| AID238166 | Antagonist potency towards human mu opioid receptor in [35S]GTP-gamma-S, assay | 2004 | Journal of medicinal chemistry, Oct-07, Volume: 47, Issue:21 | Identification of a new scaffold for opioid receptor antagonism based on the 2-amino-1,1-dimethyl-7-hydroxytetralin pharmacophore. |
| AID381420 | Inhibition of U50488-induced analgesic activity against C57BL/6 mouse assessed as tail withdrawal latency at 10 mg/kg, ip upto 21 days | 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. |
| AID631359 | Displacement of [3H]diprenorphine from human opioid kappa receptor expressed in CHO cells after 120 mins by scintillation counting | 2011 | Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23 | Discovery of aminobenzyloxyarylamides as κ opioid receptor selective antagonists: application to preclinical development of a κ opioid receptor antagonist receptor occupancy tracer. |
| AID149267 | Binding affinity was measured on opioid receptor kappa 1 | 2001 | Journal of medicinal chemistry, Sep-13, Volume: 44, Issue:19 | [2',6'-Dimethyltyrosine]dynorphin A(1-11)-NH2 analogues lacking an N-terminal amino group: potent and selective kappa opioid antagonists. |
| AID148931 | Delta opioid Antagonism (100 nM) is expressed as (Ke = [antagonist] / (IC50 ratio -1) | 2000 | Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14 | Potent and selective indolomorphinan antagonists of the kappa-opioid receptor. |
| AID230645 | Ke ratio measured as the ke values of mu receptor (GPI)/kappa receptor(MVD) using UF0488H/DAMGO as the agonist. | 1991 | Journal of medicinal chemistry, Apr, Volume: 34, Issue:4 | Role of the spacer in conferring kappa opioid receptor selectivity to bivalent ligands related to norbinaltorphimine. |
| AID482614 | Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay relative to control | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Analogues of (3R)-7-hydroxy-N-[(1S)-1-{[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl}-2-methylpropyl)-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide (JDTic). Synthesis and in vitro and in vivo opioid receptor antagonist activity. |
| AID229499 | Ratio of IC50 ethylketazocine and antagonist binding to opioid receptor | 1988 | Journal of medicinal chemistry, Apr, Volume: 31, Issue:4 | Binaltorphimine-related bivalent ligands and their kappa opioid receptor antagonist selectivity. |
| AID224566 | Ratio of IC50 of morphine (M) in the presence (100 nM) to that of morphine (M) alone, against mu opioid receptor in Guinea pig ileum preparation. | 1993 | Journal of medicinal chemistry, Jan-08, Volume: 36, Issue:1 | A remarkable change of opioid receptor selectivity on the attachment of a peptidomimetic kappa address element to the delta antagonist, natrindole: 5'-[N2-alkylamidino)methyl]naltrindole derivatives as a novel class of kappa opioid receptor antagonists. |
| AID240361 | Agonist activity against Opioid receptor delta 1 expressed in C6 cells in [35S]-GTP-gamma S assay; No stimulation up to 10000 nM | 2005 | Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5 | Major effect of pyrrolic N-benzylation in norbinaltorphimine, the selective kappa-opioid receptor antagonist. |
| AID1232256 | Antagonist activity against HA-tagged human recombinant kappa opioid receptor expressed in CHO cells assessed as inhibition of U69,593-induced ERK phosphorylation pre-incubated with compound before U69,593 stimulation for 10 mins relative to control | 2015 | Bioorganic & medicinal chemistry, Jul-15, Volume: 23, Issue:14 | Potency enhancement of the κ-opioid receptor antagonist probe ML140 through sulfonamide constraint utilizing a tetrahydroisoquinoline motif. |
| AID148973 | Opioid antagonist potency towards opioid receptor kappa 1 determined in guinea pig ileum preparation | 2001 | Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13 | Transformation of a kappa-opioid receptor antagonist to a kappa-agonist by transfer of a guanidinium group from the 5'- to 6'-position of naltrindole. |
| AID232695 | Selectivity ratio of Ki at delta opioid receptor to Ki at kappa opioid receptor | 2002 | Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16 | Discovery of an opioid kappa receptor selective pure antagonist from a library of N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphans. |
| AID229803 | Ratio of Ki for delta receptor to that of kappa receptor | 1998 | Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26 | Identification of an opioid kappa receptor subtype-selective N-substituent for (+)-(3R,4R)-dimethyl-4-(3-hydroxyphenyl)piperidine. |
| AID148598 | Mutant factor of the compound against kappa[E297K] with Opioid receptor kappa 1 for binding affinity. | 1998 | Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25 | Mutational evidence for a common kappa antagonist binding pocket in the wild-type kappa and mutant mu[K303E] opioid receptors. |
| AID149088 | Displacement of [3H]- diprenorphine from delta-receptor expressed in HEK 293 cells | 2001 | Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6 | Investigation of the selectivity of oxymorphone- and naltrexone-derived ligands via site-directed mutagenesis of opioid receptors: exploring the "address" recognition locus. |
| AID246699 | In vivo effective concentration for agonist activity in mouse tail withdrawal assay for antinociception after 24 hr of pre treatment with U-69,593 sc administration (32 mg/kg) | 2005 | Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5 | Major effect of pyrrolic N-benzylation in norbinaltorphimine, the selective kappa-opioid receptor antagonist. |
| AID152220 | Opioid antagonist potency, determined in guinea pig ileum (GPI) preparation, using morphine (mu-opioid) as agonist, expressed as IC50 ratio (tested at 20 nM) | 2001 | Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13 | Transformation of a kappa-opioid receptor antagonist to a kappa-agonist by transfer of a guanidinium group from the 5'- to 6'-position of naltrindole. |
| AID148447 | Mutant factor against mutant receptor with Opioid receptor kappa 1 | 1998 | Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25 | Mutational evidence for a common kappa antagonist binding pocket in the wild-type kappa and mutant mu[K303E] opioid receptors. |
| AID150976 | Binding affinity towards human cloned Opioid receptor mu 1 using [3H]DAMGO | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 | Identification of (3R)-7-hydroxy-N-((1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)- 3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl)-1,2,3,4-tetrahydro- 3-isoquinolinecarboxamide as a novel potent and selective opioid kappa receptor antagonist. |
| AID148568 | Binding affinity on HEK293 cells transiently transfected with plasmids encoding the rat Opioid receptor kappa 1 | 2000 | Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14 | Potent and selective indolomorphinan antagonists of the kappa-opioid receptor. |
| AID149982 | Percent stimulation of [35S]GTP-gamma-S, binding in recombinant human Opioid receptor kappa 1 transfected into CHO cells: Antagonist activity | 2003 | Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8 | 14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles. |
| AID77793 | Functional antagonism was obtained by the ability of compound to inhibit stimulation of [35S]GTP gamma S binding produced by selective agonists SNC-80 in guinea pig caudate membranes | 2004 | Journal of medicinal chemistry, Feb-12, Volume: 47, Issue:4 | Importance of phenolic address groups in opioid kappa receptor selective antagonists. |
| AID239407 | Inhibition of [3H]C1-DPDPE binding to human delta opioid receptor expressed in CHO cells | 2004 | Journal of medicinal chemistry, Oct-07, Volume: 47, Issue:21 | Identification of a new scaffold for opioid receptor antagonism based on the 2-amino-1,1-dimethyl-7-hydroxytetralin pharmacophore. |
| AID147880 | Antagonistic activity against human cloned Opioid receptor kappa 1 using U69,593 in [35S]GTP-gamma-S, assay | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 | Identification of (3R)-7-hydroxy-N-((1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)- 3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl)-1,2,3,4-tetrahydro- 3-isoquinolinecarboxamide as a novel potent and selective opioid kappa receptor antagonist. |
| AID223581 | Inhibitory activity against kappa-opioid receptor in guinea pig ileum longitudinal muscle using ethylketazocine | 1993 | Journal of medicinal chemistry, Aug-06, Volume: 36, Issue:16 | Synthesis and kappa-opioid antagonist selectivity of a norbinaltorphimine congener. Identification of the address moiety required for kappa-antagonist activity. |
| AID482611 | Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Analogues of (3R)-7-hydroxy-N-[(1S)-1-{[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl}-2-methylpropyl)-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide (JDTic). Synthesis and in vitro and in vivo opioid receptor antagonist activity. |
| AID239262 | Inhibition of [3H]diprenorphine binding to human opioid receptor kappa 1 expressed in CHO cells | 2005 | Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5 | Major effect of pyrrolic N-benzylation in norbinaltorphimine, the selective kappa-opioid receptor antagonist. |
| AID516471 | Binding affinity to kappa opioid receptor | 2010 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 20, Issue:19 | Discovery of 8-azabicyclo[3.2.1]octan-3-yloxy-benzamides as selective antagonists of the kappa opioid receptor. Part 1. |
| AID612052 | Antagonist activity against human recombinant mu opioid receptor expressed in CHO cells assessed as inhibition of [35S]GTP-gamma-S binding after 3 hrs by liquid scintillation counting | 2011 | Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11 | Probes for narcotic receptor mediated phenomena. Part 42: synthesis and in vitro pharmacological characterization of the N-methyl and N-phenethyl analogues of the racemic ortho-c and para-c oxide-bridged phenylmorphans. |
| AID1232253 | Antagonist activity against HA-tagged human recombinant kappa opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay | 2015 | Bioorganic & medicinal chemistry, Jul-15, Volume: 23, Issue:14 | Potency enhancement of the κ-opioid receptor antagonist probe ML140 through sulfonamide constraint utilizing a tetrahydroisoquinoline motif. |
| AID147875 | Ability to displace U-69,593 from human recombinant Opioid receptor kappa 1 in CHO cells using [35S]- GTP-gamma S Assay | 2003 | Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2 | The role of the side chain in determining relative delta- and kappa-affinity in C5'-substituted analogues of naltrindole. |
| AID149788 | Binding affinity to delta-opioid receptor of rat brain using [3H]DADLE as radioligand | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | Identification of the first trans-(3R,4R)- dimethyl-4-(3-hydroxyphenyl)piperidine derivative to possess highly potent and selective opioid kappa receptor antagonist activity. |
| AID228147 | Binding affinity towards human kappa,mu,delta receptors was calculated as the ratio; 1/210/52 | 2003 | Journal of medicinal chemistry, May-22, Volume: 46, Issue:11 | Structure-activity relationships of dynorphin a analogues modified in the address sequence. |
| AID357094 | Antinociceptive effect in intrathecally dosed NY1DD transgenic mouse after 6 hrs by heat tail flick test | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Apr-03, Volume: 104, Issue:14 | Naloxone acts as a potent analgesic in transgenic mouse models of sickle cell anemia. |
| AID128674 | Antagonism of delta1 opioid agonist (DPDPE)-induced antinociception upon intrathecal administration in mice at a dose of 250 pmol | 2004 | Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12 | A bivalent ligand (KDN-21) reveals spinal delta and kappa opioid receptors are organized as heterodimers that give rise to delta(1) and kappa(2) phenotypes. Selective targeting of delta-kappa heterodimers. |
| AID381421 | Inhibition of U50488-induced analgesic activity against C57BL/6 mouse assessed as tail withdrawal latency at 10 mg/kg, ip after 28 days | 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. |
| AID149089 | Displacement of [3H]- diprenorphine from mu-K303E-receptor expressed in HEK 293 cells | 2001 | Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6 | Investigation of the selectivity of oxymorphone- and naltrexone-derived ligands via site-directed mutagenesis of opioid receptors: exploring the "address" recognition locus. |
| AID482619 | Intrinsic activity at human recombinant kappa opioid receptor expressed in CHO cells up to 10 uM | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Analogues of (3R)-7-hydroxy-N-[(1S)-1-{[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl}-2-methylpropyl)-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide (JDTic). Synthesis and in vitro and in vivo opioid receptor antagonist activity. |
| AID1629759 | Antagonist activity at mouse kappa opioid receptor-1 expressed in CHO cell membranes assessed as inhibition of U50,488H-induced [35S]GTPgammaS binding incubated for 60 mins by scintillation spectroscopic analysis | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18 | Mitragynine/Corynantheidine Pseudoindoxyls As Opioid Analgesics with Mu Agonism and Delta Antagonism, Which Do Not Recruit β-Arrestin-2. |
| AID232140 | Ratio of (Ki) mu-opioid receptor to that of (Ki) kappa-opioid receptor | 2003 | Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25 | Guanidino N-substituted and N,N-disubstituted derivatives of the kappa-opioid antagonist GNTI. |
| AID224572 | Binding affinity for mu opioid receptor was determined using radioligand [3H][D-Ala2,MePhe4,Gly-ol6]enkephalin (DAMGO) in Guinea pig brain membranes. | 1993 | Journal of medicinal chemistry, Jan-08, Volume: 36, Issue:1 | A remarkable change of opioid receptor selectivity on the attachment of a peptidomimetic kappa address element to the delta antagonist, natrindole: 5'-[N2-alkylamidino)methyl]naltrindole derivatives as a novel class of kappa opioid receptor antagonists. |
| AID450017 | Displacement of [3H]DPDPE from delta opioid receptor expressed in HEK293 cells by visible spectrophotometry | 2009 | Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18 | Synthesis and pharmacological evaluation of 6-naltrexamine analogs for alcohol cessation. |
| AID231541 | Ratio of binding affinity towards kappa, mu and delta opioid receptor; 1/155/53 | 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. |
| AID148177 | Binding affinity using [3H]diprenorphine as the radioligand against wild-type Opioid receptor kappa 1 in COS-7 cells | 2000 | Journal of medicinal chemistry, Apr-20, Volume: 43, Issue:8 | Binding of norbinaltorphimine (norBNI) congeners to wild-type and mutant mu and kappa opioid receptors: molecular recognition loci for the pharmacophore and address components of kappa antagonists. |
| AID232039 | Selectivity between delta receptor and kappa receptor | 2003 | Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2 | The role of the side chain in determining relative delta- and kappa-affinity in C5'-substituted analogues of naltrindole. |
| AID233141 | Selectivity ratio of delta and kappa opioid receptor | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 | Identification of (3R)-7-hydroxy-N-((1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)- 3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl)-1,2,3,4-tetrahydro- 3-isoquinolinecarboxamide as a novel potent and selective opioid kappa receptor antagonist. |
| AID256843 | Inhibition of DAMGO stimulated [35S]GTP-gamma-S binding to cloned human mu opioid receptor | 2005 | Journal of medicinal chemistry, Dec-29, Volume: 48, Issue:26 | N-substituted cis-4a-(3-hydroxyphenyl)-8a-methyloctahydroisoquinolines are opioid receptor pure antagonists. |
| AID574379 | Selectivity ratio of Ki for mu opioid receptor in guinea pig forebrain to Ki for kappa opioid receptor in guinea pig cerebellum | 2011 | Bioorganic & medicinal chemistry, Feb-01, Volume: 19, Issue:3 | Synthesis of 6,14-epoxymorphinan derivatives and their pharmacologies. |
| AID148221 | Ability to displace [3H]DPDPE from human recombinant Opioid receptor delta 1 in CHO cells | 2003 | Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2 | The role of the side chain in determining relative delta- and kappa-affinity in C5'-substituted analogues of naltrindole. |
| AID1181420 | Antagonist activity at human recombinant mu opioid receptor expressed in CHO cell membranes assessed as inhibition of DAMGO-induced response after 60 mins by [35S]GTPgammaS binding assay | 2014 | Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15 | Pyrrolo- and pyridomorphinans: non-selective opioid antagonists and delta opioid agonists/mu opioid partial agonists. |
| AID150025 | Binding affinity of compound was measured against Opioid receptor mu 1 on electrically stimulated guinea pig ileal longitudinal muscle myenteric plexus (GPI)at 100 nM preparation using DAMGO as agonist | 1991 | Journal of medicinal chemistry, Apr, Volume: 34, Issue:4 | Role of the spacer in conferring kappa opioid receptor selectivity to bivalent ligands related to norbinaltorphimine. |
| AID357093 | Antinociceptive effect in icv dosed NY1DD transgenic mouse after 1 hr by heat tail flick test | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Apr-03, Volume: 104, Issue:14 | Naloxone acts as a potent analgesic in transgenic mouse models of sickle cell anemia. |
| AID77792 | Functional antagonism was obtained by the ability of compound to inhibit stimulation of [35S]GTP gamma S binding produced by selective agonists DAMGO in guinea pig caudate membranes | 2004 | Journal of medicinal chemistry, Feb-12, Volume: 47, Issue:4 | Importance of phenolic address groups in opioid kappa receptor selective antagonists. |
| AID233363 | Selectivity ratio of mu and kappa opioid receptor | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 | Identification of (3R)-7-hydroxy-N-((1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)- 3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl)-1,2,3,4-tetrahydro- 3-isoquinolinecarboxamide as a novel potent and selective opioid kappa receptor antagonist. |
| AID149428 | Inhibition of [35S]GTP-gamma-S, binding from Opioid receptor kappa 1 in Guinea pig Caudate stimulated by U69,593 | 1998 | Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26 | Identification of an opioid kappa receptor subtype-selective N-substituent for (+)-(3R,4R)-dimethyl-4-(3-hydroxyphenyl)piperidine. |
| AID229398 | Selectivity ratio of mu opioid receptor to that of kappa opioid receptor | 1994 | Journal of medicinal chemistry, May-13, Volume: 37, Issue:10 | Structure-activity relationship of N17'-substituted norbinaltorphimine congeners. Role of the N17' basic group in the interaction with a putative address subsite on the kappa opioid receptor. |
| AID230641 | Ke ratio measured as the ke values of Opioid receptor delta 1(GPI)/Opioid receptor kappa 1(MVD) using DADLE/M as the agonist. | 1991 | Journal of medicinal chemistry, Apr, Volume: 34, Issue:4 | Role of the spacer in conferring kappa opioid receptor selectivity to bivalent ligands related to norbinaltorphimine. |
| AID233142 | Selectivity ratio of of delta and kappa opioid receptor | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 | Identification of (3R)-7-hydroxy-N-((1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)- 3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl)-1,2,3,4-tetrahydro- 3-isoquinolinecarboxamide as a novel potent and selective opioid kappa receptor antagonist. |
| AID148220 | Displacement of [3H]C1-DPDPE from human recombinant Opioid receptor delta 1 on CHO cell membranes. | 2003 | Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8 | 14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles. |
| AID502620 | Antagonist activity at human delta opioid receptor expressed in HEK cells assessed as inhibition of SNC-80-induced [35S]GTPgammaS binding | 2010 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 20, Issue:18 | SAR development of a series of 8-azabicyclo[3.2.1]octan-3-yloxy-benzamides as kappa opioid receptor antagonists. Part 2. |
| AID150988 | Compound was evaluated for its binding affinity by displacing DAMGO to human cloned mu opioid receptor transfected into CHO cells using [35S]GTP-gamma-S, assay | 2000 | Bioorganic & medicinal chemistry letters, Oct-16, Volume: 10, Issue:20 | Selective kappa-opioid antagonists related to naltrindole. Effect of side-chain spacer in the 5'-amidinoalkyl series. |
| AID147888 | Opioid receptor mu 1 Antagonism (100 nM) is expressed as (Ke = [antagonist] / (IC50 ratio -1) | 2000 | Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14 | Potent and selective indolomorphinan antagonists of the kappa-opioid receptor. |
| AID1181426 | Antagonist activity at human recombinant delta opioid receptor expressed in CHO cell membranes assessed as inhibition of DPDPE-induced response after 60 mins by [35S]GTPgammaS binding assay | 2014 | Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15 | Pyrrolo- and pyridomorphinans: non-selective opioid antagonists and delta opioid agonists/mu opioid partial agonists. |
| AID747950 | Antagonist activity at human delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTPgammaS binding | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Discovery of N-{4-[(3-hydroxyphenyl)-3-methylpiperazin-1-yl]methyl-2-methylpropyl}-4-phenoxybenzamide analogues as selective kappa opioid receptor antagonists. |
| AID1191370 | Selectivity ratio of Ki for mu opioid receptor (unknown origin) to Ki for kappa opioid receptor (unknown origin) | 2015 | European journal of medicinal chemistry, Jan-27, Volume: 90 | Novel fluoroalkyl derivatives of selective kappa opioid receptor antagonist JDTic: Design, synthesis, pharmacology and molecular modeling studies. |
| AID234391 | mu/kappa ratio of the compound | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | Identification of the first trans-(3R,4R)- dimethyl-4-(3-hydroxyphenyl)piperidine derivative to possess highly potent and selective opioid kappa receptor antagonist activity. |
| AID502181 | Selectivity ratio of Ki for delta opioid receptor in guinea pig forebrain to Ki for kappa opioid receptor in guinea pig cerebellum | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17 | Synthesis of pyrrolomorphinan derivatives as kappa opioid agonists. |
| AID147878 | Antagonistic activity against cloned human Opioid receptor kappa 1 using U69,593 as ligand in [35S]GTP-gamma-S, assay | 2003 | Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25 | Guanidino N-substituted and N,N-disubstituted derivatives of the kappa-opioid antagonist GNTI. |
| AID256847 | Selectivity for cloned human delta opioid receptor over kappa opioid receptor | 2005 | Journal of medicinal chemistry, Dec-29, Volume: 48, Issue:26 | N-substituted cis-4a-(3-hydroxyphenyl)-8a-methyloctahydroisoquinolines are opioid receptor pure antagonists. |
| AID233291 | Selectivity ratio is IC50 value of kappa-opioid receptor to that of delta-opioid receptor | 1993 | Journal of medicinal chemistry, Jan-08, Volume: 36, Issue:1 | A remarkable change of opioid receptor selectivity on the attachment of a peptidomimetic kappa address element to the delta antagonist, natrindole: 5'-[N2-alkylamidino)methyl]naltrindole derivatives as a novel class of kappa opioid receptor antagonists. |
| AID243084 | Relative binding affinity for rat Opioid receptor delta 1 and human Opioid receptor kappa 1 | 2005 | Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5 | Major effect of pyrrolic N-benzylation in norbinaltorphimine, the selective kappa-opioid receptor antagonist. |
| AID150989 | Compound was evaluated for its binding affinity to CHO cells expressing cloned human Opioid receptor mu 1 by displacing [3H]-DAMGO | 2000 | Bioorganic & medicinal chemistry letters, Oct-16, Volume: 10, Issue:20 | Selective kappa-opioid antagonists related to naltrindole. Effect of side-chain spacer in the 5'-amidinoalkyl series. |
| AID1810955 | Analgesic activity in chronic visceral hypersensitivity-induced chronic abdominal pain mouse model assessed as reduction in colonic nociceptor mechano-sensitivity at 0.1 uM measured at 5 mins by Von Frey filament assay | 2021 | Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13 | Design of a Stable Cyclic Peptide Analgesic Derived from Sunflower Seeds that Targets the κ-Opioid Receptor for the Treatment of Chronic Abdominal Pain. |
| AID148981 | Ability to displace [3H]U-69593 from Opioid receptor kappa 1 of guinea pig brain | 2002 | Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16 | Discovery of an opioid kappa receptor selective pure antagonist from a library of N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphans. |
| AID149774 | Binding affinity against Opioid receptor delta 1 was measured in the guinea pig brain membranes using [3H]DADLE in the presence of 1 uM unlabeled DAMGO as radioligand | 1991 | Journal of medicinal chemistry, Apr, Volume: 34, Issue:4 | Role of the spacer in conferring kappa opioid receptor selectivity to bivalent ligands related to norbinaltorphimine. |
| AID148475 | Inhibition of total opioid receptor by displacing 0.5 nM [3H]bremazocine in guinea pig brain membrane | 1992 | Journal of medicinal chemistry, Nov-27, Volume: 35, Issue:24 | O3-(2-carbomethoxyallyl) ethers of opioid ligands derived from oxymorphone, naltrexone, etorphine, diprenorphine, norbinaltorphimine, and naltrindole. Unexpected O3-dealkylation in the opioid radioligand displacement assay. |
| AID149551 | The binding affinity on kappa-opioid receptor using [3H]- U-69,593 as radioligand | 1994 | Journal of medicinal chemistry, May-13, Volume: 37, Issue:10 | Structure-activity relationship of N17'-substituted norbinaltorphimine congeners. Role of the N17' basic group in the interaction with a putative address subsite on the kappa opioid receptor. |
| AID1461556 | Antimicrobial activity against Trichomonas vaginalis after 48 hrs by neutral red staining based invert microscopic analysis | 2017 | Bioorganic & medicinal chemistry, 08-15, Volume: 25, Issue:16 | Antitrichomonal activity of δ opioid receptor antagonists, 7-benzylidenenaltrexone derivatives. |
| AID149260 | Inhibition of [3H]U-69593 binding to Opioid receptor kappa 1 of guinea pig brain | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 | Identification of (3R)-7-hydroxy-N-((1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)- 3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl)-1,2,3,4-tetrahydro- 3-isoquinolinecarboxamide as a novel potent and selective opioid kappa receptor antagonist. |
| AID233295 | Selectivity ratio is Ki value of mu-opioid receptor to that of kappa-opioid receptor | 1993 | Journal of medicinal chemistry, Jan-08, Volume: 36, Issue:1 | A remarkable change of opioid receptor selectivity on the attachment of a peptidomimetic kappa address element to the delta antagonist, natrindole: 5'-[N2-alkylamidino)methyl]naltrindole derivatives as a novel class of kappa opioid receptor antagonists. |
| AID574380 | Selectivity ratio of Ki for delta opioid receptor in guinea pig forebrain to Ki for kappa opioid receptor in guinea pig cerebellum | 2011 | Bioorganic & medicinal chemistry, Feb-01, Volume: 19, Issue:3 | Synthesis of 6,14-epoxymorphinan derivatives and their pharmacologies. |
| AID516453 | Antagonist activity at human kappa opioid receptor assessed as inhibition of dynorphin A-induced [35S]GTPgammaS binding | 2010 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 20, Issue:19 | Discovery of 8-azabicyclo[3.2.1]octan-3-yloxy-benzamides as selective antagonists of the kappa opioid receptor. Part 1. |
| AID482613 | Agonist activity at human recombinant kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Analogues of (3R)-7-hydroxy-N-[(1S)-1-{[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl}-2-methylpropyl)-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide (JDTic). Synthesis and in vitro and in vivo opioid receptor antagonist activity. |
| AID239172 | Inhibition of [3H]diprenorphine binding to rat Opioid receptor mu 1 expressed in C6 cells | 2005 | Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5 | Major effect of pyrrolic N-benzylation in norbinaltorphimine, the selective kappa-opioid receptor antagonist. |
| AID233862 | Selectivity between mu opioid receptor and delta opioid receptor. | 2003 | Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8 | 14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles. |
| AID148056 | Inhibition of [35S]GTP-gamma-S, binding from Opioid receptor mu 1 in Guinea pig Caudate stimulated by DAMGO | 1998 | Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26 | Identification of an opioid kappa receptor subtype-selective N-substituent for (+)-(3R,4R)-dimethyl-4-(3-hydroxyphenyl)piperidine. |
| AID482610 | Selectivity for human delta opioid receptor over kappa opioid receptor | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Analogues of (3R)-7-hydroxy-N-[(1S)-1-{[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl}-2-methylpropyl)-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide (JDTic). Synthesis and in vitro and in vivo opioid receptor antagonist activity. |
| AID152377 | Antagonist activity on agonist (DAMGO) stimulated [35S]GTP-gamma-S, binding in cloned mu opioid receptors | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | Identification of the first trans-(3R,4R)- dimethyl-4-(3-hydroxyphenyl)piperidine derivative to possess highly potent and selective opioid kappa receptor antagonist activity. |
| AID138709 | Inhibitory activity against mu-opioid receptor in guinea pig ileum longitudinal muscle using morphine | 1993 | Journal of medicinal chemistry, Aug-06, Volume: 36, Issue:16 | Synthesis and kappa-opioid antagonist selectivity of a norbinaltorphimine congener. Identification of the address moiety required for kappa-antagonist activity. |
| AID148645 | Inhibitory activity against delta-opioid receptor in mouse vas deferens preparation using DADLE | 1993 | Journal of medicinal chemistry, Aug-06, Volume: 36, Issue:16 | Synthesis and kappa-opioid antagonist selectivity of a norbinaltorphimine congener. Identification of the address moiety required for kappa-antagonist activity. |
| AID229881 | Selectivity ratio, ratio of Ke value of mu to kappa opioid receptor | 2000 | Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14 | Potent and selective indolomorphinan antagonists of the kappa-opioid receptor. |
| AID222424 | Antagonist activity determined in the guinea pig assay against [D-Ala3] Dyn A (1-11)-NH2 at 1 uM | 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. |
| AID149893 | Binding affinity for delta opioid receptor was determined using radioligand [3H]DPDPE in Guinea pig brain membranes. | 1993 | Journal of medicinal chemistry, Jan-08, Volume: 36, Issue:1 | A remarkable change of opioid receptor selectivity on the attachment of a peptidomimetic kappa address element to the delta antagonist, natrindole: 5'-[N2-alkylamidino)methyl]naltrindole derivatives as a novel class of kappa opioid receptor antagonists. |
| AID229878 | Selectivity ratio, ratio of Ke value of delta to kappa opioid receptor | 2000 | Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14 | Potent and selective indolomorphinan antagonists of the kappa-opioid receptor. |
| AID150026 | Binding affinity of compound was measured against Opioid receptor mu 1 on electrically stimulated guinea pig ileal longitudinal muscle myenteric plexus (GPI)at 100 nM preparation using M as agonist | 1991 | Journal of medicinal chemistry, Apr, Volume: 34, Issue:4 | Role of the spacer in conferring kappa opioid receptor selectivity to bivalent ligands related to norbinaltorphimine. |
| AID607798 | Antagonist activity at human kappa opioid receptor expressed in CHO cells coexpressing human recombinant KOP after 3 hrs by [35S]GTPgammaS binding assay | 2011 | Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14 | Probes for narcotic receptor mediated phenomena. 43. Synthesis of the ortho-a and para-a, and improved synthesis and optical resolution of the ortho-b and para-b oxide-bridged phenylmorphans: compounds with moderate to low opioid-receptor affinity. |
| AID149269 | Binding affinity to opioid receptor kappa 1 of guinea pig brain, using [3H]U-69593 as radioligand | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | Identification of the first trans-(3R,4R)- dimethyl-4-(3-hydroxyphenyl)piperidine derivative to possess highly potent and selective opioid kappa receptor antagonist activity. |
| AID516454 | Antagonist activity at human mu opioid receptor assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding | 2010 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 20, Issue:19 | Discovery of 8-azabicyclo[3.2.1]octan-3-yloxy-benzamides as selective antagonists of the kappa opioid receptor. Part 1. |
| AID261109 | Selectivity for human kappa opioid receptor over human mu opioid receptor | 2006 | Journal of medicinal chemistry, Mar-09, Volume: 49, Issue:5 | N-substituted 4beta-methyl-5-(3-hydroxyphenyl)-7alpha-amidomorphans are potent, selective kappa opioid receptor antagonists. |
| AID128680 | Antagonism of delta2 opioid agonist (deltorphin II)-induced antinociception upon intrathecal administration in mice at a dose of 250 pmol | 2004 | Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12 | A bivalent ligand (KDN-21) reveals spinal delta and kappa opioid receptors are organized as heterodimers that give rise to delta(1) and kappa(2) phenotypes. Selective targeting of delta-kappa heterodimers. |
| AID148446 | Effect on binding affinity of mutational exchange of Glu297 in the Opioid receptor kappa 1 in transiently expressed rat cos-7 cells activity expressed as binding ratio with nor-BNI. | 1998 | Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25 | Mutational evidence for a common kappa antagonist binding pocket in the wild-type kappa and mutant mu[K303E] opioid receptors. |
| AID631393 | Agonist activity at human opioid mu receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding at 10 uM | 2011 | Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23 | Discovery of aminobenzyloxyarylamides as κ opioid receptor selective antagonists: application to preclinical development of a κ opioid receptor antagonist receptor occupancy tracer. |
| AID226664 | Antagonist activity determined in the [35S]GTP-gamma-S, binding assay relative to 50 nM 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. |
| AID232137 | Ratio of (Ke) delta-opioid receptor to that of (Ke) kappa-opioid receptor | 2003 | Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25 | Guanidino N-substituted and N,N-disubstituted derivatives of the kappa-opioid antagonist GNTI. |
| AID148344 | Stimulation of DAMGO binding in recombinant human Opioid receptor mu 1 transfected into CHO cells | 2003 | Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8 | 14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles. |
| AID1181423 | Antagonist activity at human recombinant kappa opioid receptor expressed in CHO cell membranes assessed as inhibition of U69593-induced response after 60 mins by [35S]GTPgammaS binding assay | 2014 | Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15 | Pyrrolo- and pyridomorphinans: non-selective opioid antagonists and delta opioid agonists/mu opioid partial agonists. |
| AID482612 | Agonist activity at human recombinant delta opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Analogues of (3R)-7-hydroxy-N-[(1S)-1-{[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl}-2-methylpropyl)-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide (JDTic). Synthesis and in vitro and in vivo opioid receptor antagonist activity. |
| AID1245410 | Antagonist activity at cloned human kappa opioid receptor assessed as inhibition of U69593-induced [35S]GTPgammaS binding | 2015 | Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19 | Design, synthesis, and pharmacological evaluation of JDTic analogs to examine the significance of the 3- and 4-methyl substituents. |
| AID227967 | Antagonist potency at a concentration of 100 nM | 1994 | Journal of medicinal chemistry, May-13, Volume: 37, Issue:10 | Structure-activity relationship of N17'-substituted norbinaltorphimine congeners. Role of the N17' basic group in the interaction with a putative address subsite on the kappa opioid receptor. |
| AID631392 | Agonist activity at human opioid kappa receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding at 10 uM | 2011 | Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23 | Discovery of aminobenzyloxyarylamides as κ opioid receptor selective antagonists: application to preclinical development of a κ opioid receptor antagonist receptor occupancy tracer. |
| AID149069 | In vitro binding affinity to human Opioid receptor delta 1 on CHO cell membranes using [3H]diprenorphine displacement. | 2003 | Journal of medicinal chemistry, May-22, Volume: 46, Issue:11 | Structure-activity relationships of dynorphin a analogues modified in the address sequence. |
| AID256845 | Inhibition of U69,593 stimulated [35S]GTP-gamma-S binding to cloned human kappa opioid receptor | 2005 | Journal of medicinal chemistry, Dec-29, Volume: 48, Issue:26 | N-substituted cis-4a-(3-hydroxyphenyl)-8a-methyloctahydroisoquinolines are opioid receptor pure antagonists. |
| AID148806 | Antagonist activity was evaluated in the mouse vas deferens assay against DPDPE which is selective agonist of Delta receptor | 2001 | Journal of medicinal chemistry, Sep-13, Volume: 44, Issue:19 | [2',6'-Dimethyltyrosine]dynorphin A(1-11)-NH2 analogues lacking an N-terminal amino group: potent and selective kappa opioid antagonists. |
| AID147915 | Binding affinity of compound was measured against Opioid receptor mu 1 on electrically stimulated guinea pig ileal longitudinal muscle myenteric plexus (GPI)at 100 nM preparation using DAMGO as agonist | 1991 | Journal of medicinal chemistry, Apr, Volume: 34, Issue:4 | Role of the spacer in conferring kappa opioid receptor selectivity to bivalent ligands related to norbinaltorphimine. |
| AID240362 | Agonist activity against Opioid receptor kappa 1 expressed in CHO cells in [35S]-GTP-gamma S assay; No stimulation up to 10000 nM | 2005 | Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5 | Major effect of pyrrolic N-benzylation in norbinaltorphimine, the selective kappa-opioid receptor antagonist. |
| AID1232257 | Antagonist activity against human kappa opioid receptor expressed in human U2OS cells co-expressing beta-arrestin2 pre-treated for 15 mins before U69,593 stimulation for 90 mins by DiscoveRx beta-arrestin2 recruitment based PathHunter assay relative to co | 2015 | Bioorganic & medicinal chemistry, Jul-15, Volume: 23, Issue:14 | Potency enhancement of the κ-opioid receptor antagonist probe ML140 through sulfonamide constraint utilizing a tetrahydroisoquinoline motif. |
| AID502179 | Displacement of [3H]NTI from delta opioid receptor in guinea pig forebrain | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17 | Synthesis of pyrrolomorphinan derivatives as kappa opioid agonists. |
| AID727479 | Antagonist activity at KOR (unknown origin) assessed as inhibition of U69593-stimulated [35S]GTPgammaS binding | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6 | Development of κ opioid receptor antagonists. |
| AID148786 | Opioid antagonist potency, determined in mouse vas deferens (MVD) preparation, using DADLE (delta-opioid) as agonist, expressed as IC50 ratio | 2001 | Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13 | Transformation of a kappa-opioid receptor antagonist to a kappa-agonist by transfer of a guanidinium group from the 5'- to 6'-position of naltrindole. |
| AID609328 | Antimalarial activity against chloroquine-resistant Plasmodium chabaudi infected in mouse assessed as parasitemia at 10 mg/kg, po administered for 3 consecutive days | 2011 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16 | Opioid δ₁ receptor antagonist 7-benzylidenenaltrexone as an effective resistance reverser for chloroquine-resistant Plasmodium chabaudi. |
| AID243076 | Relative binding affinity for rat Opioid receptor mu 1 and human Opioid receptor kappa 1 | 2005 | Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5 | Major effect of pyrrolic N-benzylation in norbinaltorphimine, the selective kappa-opioid receptor antagonist. |
| AID150979 | Binding affinity towards cloned human Opioid receptor mu 1 in CHO cell membranes. | 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. |
| AID261107 | Inhibition of DPDPE stimulated [35S]GTP-gamma-S binding to cloned human delta opioid receptor expressed in CHO cells | 2006 | Journal of medicinal chemistry, Mar-09, Volume: 49, Issue:5 | N-substituted 4beta-methyl-5-(3-hydroxyphenyl)-7alpha-amidomorphans are potent, selective kappa opioid receptor antagonists. |
| AID148216 | Antagonistic activity against human cloned Opioid receptor delta 1 using DPDPE in [35S]GTP-gamma-S, assay | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 | Identification of (3R)-7-hydroxy-N-((1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)- 3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl)-1,2,3,4-tetrahydro- 3-isoquinolinecarboxamide as a novel potent and selective opioid kappa receptor antagonist. |
| AID233096 | Ratio of antagonistic activity for mu and kappa receptors | 1988 | Journal of medicinal chemistry, Apr, Volume: 31, Issue:4 | Binaltorphimine-related bivalent ligands and their kappa opioid receptor antagonist selectivity. |
| AID148017 | Compound was evaluated for its binding affinity to CHO cells expressing cloned human Opioid receptor kappa 1 by displacing [3H]U-69593 | 2000 | Bioorganic & medicinal chemistry letters, Oct-16, Volume: 10, Issue:20 | Selective kappa-opioid antagonists related to naltrindole. Effect of side-chain spacer in the 5'-amidinoalkyl series. |
| AID482616 | Agonist activity at human recombinant kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay relative to control | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Analogues of (3R)-7-hydroxy-N-[(1S)-1-{[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl}-2-methylpropyl)-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide (JDTic). Synthesis and in vitro and in vivo opioid receptor antagonist activity. |
| AID150238 | Antagonistic activity towards Opioid receptors in the guinea pig ileum | 2003 | Journal of medicinal chemistry, May-22, Volume: 46, Issue:11 | Structure-activity relationships of dynorphin a analogues modified in the address sequence. |
| AID148244 | Binding affinity against cloned human Opioid receptor delta 1 transfected into chinese hamster ovary cells using [3H]Cl-DPDPE as radioligand | 2003 | Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25 | Guanidino N-substituted and N,N-disubstituted derivatives of the kappa-opioid antagonist GNTI. |
| AID147988 | Ability to displace [3H]U-69593 from human recombinant Opioid receptor kappa 1 in CHO cells | 2003 | Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2 | The role of the side chain in determining relative delta- and kappa-affinity in C5'-substituted analogues of naltrindole. |
| AID149996 | Stimulation of U-69,593 binding at human recombinant Opioid receptor kappa 1 transfected into CHO cells. | 2003 | Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8 | 14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles. |
| AID230224 | Inhibitory concentration was tested on electrically stimulated mouse vas deferens using DADLE as delta opioid receptor agonist at 100 nM of the compound | 1994 | Journal of medicinal chemistry, May-13, Volume: 37, Issue:10 | Structure-activity relationship of N17'-substituted norbinaltorphimine congeners. Role of the N17' basic group in the interaction with a putative address subsite on the kappa opioid receptor. |
| AID256844 | Inhibition of DPDPE stimulated [35S]GTP-gamma-S binding to cloned human delta opioid receptor | 2005 | Journal of medicinal chemistry, Dec-29, Volume: 48, Issue:26 | N-substituted cis-4a-(3-hydroxyphenyl)-8a-methyloctahydroisoquinolines are opioid receptor pure antagonists. |
| AID612053 | Antagonist activity against human recombinant kappa opioid receptor expressed in CHO cells assessed as inhibition of [35S]GTP-gamma-S binding after 3 hrs by liquid scintillation counting | 2011 | Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11 | Probes for narcotic receptor mediated phenomena. Part 42: synthesis and in vitro pharmacological characterization of the N-methyl and N-phenethyl analogues of the racemic ortho-c and para-c oxide-bridged phenylmorphans. |
| AID232458 | Selectivity ratio between kappa-opioid receptor to delta-opioid receptor | 1993 | Journal of medicinal chemistry, Aug-06, Volume: 36, Issue:16 | Synthesis and kappa-opioid antagonist selectivity of a norbinaltorphimine congener. Identification of the address moiety required for kappa-antagonist activity. |
| AID229805 | Ratio of Ki for mu receptor to that of kappa receptor | 1998 | Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26 | Identification of an opioid kappa receptor subtype-selective N-substituent for (+)-(3R,4R)-dimethyl-4-(3-hydroxyphenyl)piperidine. |
| AID148393 | Antagonistic activity for Opioid receptor delta 1 in mouse vas deferens at 200 nM | 1988 | Journal of medicinal chemistry, Apr, Volume: 31, Issue:4 | Binaltorphimine-related bivalent ligands and their kappa opioid receptor antagonist selectivity. |
| AID230649 | Ki ratio measured as the ke values of mu receptor/kappa receptor from guinea pig brain membranes. | 1991 | Journal of medicinal chemistry, Apr, Volume: 34, Issue:4 | Role of the spacer in conferring kappa opioid receptor selectivity to bivalent ligands related to norbinaltorphimine. |
| AID233294 | Selectivity ratio is Ki value of delta-opioid receptor to that of kappa-opioid receptor | 1993 | Journal of medicinal chemistry, Jan-08, Volume: 36, Issue:1 | A remarkable change of opioid receptor selectivity on the attachment of a peptidomimetic kappa address element to the delta antagonist, natrindole: 5'-[N2-alkylamidino)methyl]naltrindole derivatives as a novel class of kappa opioid receptor antagonists. |
| AID147884 | Inhibition of [35S]GTP-gamma-S, binding in guines pig caudate stimulated by DAMGO for Opioid receptor mu 1 | 2003 | Journal of medicinal chemistry, May-08, Volume: 46, Issue:10 | 2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy. |
| AID150842 | Ability to displace [3H]DAMGO from human recombinant Opioid receptor mu 1 in CHO cells | 2003 | Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2 | The role of the side chain in determining relative delta- and kappa-affinity in C5'-substituted analogues of naltrindole. |
| AID150983 | Binding affinity against cloned human Opioid receptor mu 1 transfected into chinese hamster ovary cells using [3H]DAMGO as radioligand | 2003 | Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25 | Guanidino N-substituted and N,N-disubstituted derivatives of the kappa-opioid antagonist GNTI. |
| AID613642 | Displacement of [3H]diprenorphine from human mu opioid receptor expressed in CHO cells after 1 hr by liquid scintillation counting | 2011 | Journal of medicinal chemistry, Aug-25, Volume: 54, Issue:16 | Design and discovery of a selective small molecule κ opioid antagonist (2-methyl-N-((2'-(pyrrolidin-1-ylsulfonyl)biphenyl-4-yl)methyl)propan-1-amine, PF-4455242). |
| AID482606 | Antagonist activity at human recombinant mu opioid receptor expressed in CHO cells assessed as inhibition of DAMGO-induced [35S]GTPgammaS binding | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Analogues of (3R)-7-hydroxy-N-[(1S)-1-{[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl}-2-methylpropyl)-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide (JDTic). Synthesis and in vitro and in vivo opioid receptor antagonist activity. |
| AID603175 | Displacement of [125I]-IBNalA from KOR-1 expressed in CHO cells | 2011 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 21, Issue:13 | Generation of novel radiolabeled opiates through site-selective iodination. |
| AID1245408 | Antagonist activity at cloned human mu opioid receptor assessed as inhibition of DAMGO-induced [35S]GTPgammaS binding | 2015 | Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19 | Design, synthesis, and pharmacological evaluation of JDTic analogs to examine the significance of the 3- and 4-methyl substituents. |
| AID238174 | Antagonistic activity against rat opioid receptor delta 1 expressed in C6 cells in [35S]GTP gamma S assay | 2005 | Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5 | Major effect of pyrrolic N-benzylation in norbinaltorphimine, the selective kappa-opioid receptor antagonist. |
| AID148248 | Compound was evaluated for functional opioid activity by stimulation of [35S]GTP-gamma-S, in cloned human Opioid receptor delta 1 transfected into CHO cells | 2000 | Bioorganic & medicinal chemistry letters, Oct-16, Volume: 10, Issue:20 | Selective kappa-opioid antagonists related to naltrindole. Effect of side-chain spacer in the 5'-amidinoalkyl series. |
| AID148585 | Displacement of [3H]diprenorphine from k-Y312A-receptor expressed in HEK 293 cells | 2001 | Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6 | Investigation of the selectivity of oxymorphone- and naltrexone-derived ligands via site-directed mutagenesis of opioid receptors: exploring the "address" recognition locus. |
| AID149783 | Inhibition of [3H]-DADLE binding to Opioid receptor delta 1 of rat brain tissue | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 | Identification of (3R)-7-hydroxy-N-((1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)- 3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl)-1,2,3,4-tetrahydro- 3-isoquinolinecarboxamide as a novel potent and selective opioid kappa receptor antagonist. |
| AID148588 | Effect on binding affinity of mutational exchange of Glu297 in the Opioid receptor kappa 1 in transiently expressed rat cos-7 cells activity expressed as binding affinity. | 1998 | Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25 | Mutational evidence for a common kappa antagonist binding pocket in the wild-type kappa and mutant mu[K303E] opioid receptors. |
| AID482609 | Selectivity for human mu opioid receptor over kappa opioid receptor | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Analogues of (3R)-7-hydroxy-N-[(1S)-1-{[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl}-2-methylpropyl)-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide (JDTic). Synthesis and in vitro and in vivo opioid receptor antagonist activity. |
| AID233860 | Selectivity between kappa opioid receptor and delta opioid receptor. | 2003 | Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8 | 14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles. |
| AID482615 | Agonist activity at human recombinant delta opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay relative to control | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Analogues of (3R)-7-hydroxy-N-[(1S)-1-{[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl}-2-methylpropyl)-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide (JDTic). Synthesis and in vitro and in vivo opioid receptor antagonist activity. |
| AID231936 | Ratio for binding affinity against CHO cells transfected with cloned human delta opioid receptor to that of kappa opioid receptor | 2000 | Bioorganic & medicinal chemistry letters, Oct-16, Volume: 10, Issue:20 | Selective kappa-opioid antagonists related to naltrindole. Effect of side-chain spacer in the 5'-amidinoalkyl series. |
| AID631363 | Selectivity ratio of Ki for human opioid delta receptor expressed in HEK293 cells to Ki for human opioid kappa receptor expressed in CHO cells | 2011 | Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23 | Discovery of aminobenzyloxyarylamides as κ opioid receptor selective antagonists: application to preclinical development of a κ opioid receptor antagonist receptor occupancy tracer. |
| AID502618 | Antagonist activity at human kappa opioid receptor expressed in HEK cells assessed as inhibition of dynorphin A-induced [35S]GTPgammaS binding | 2010 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 20, Issue:18 | SAR development of a series of 8-azabicyclo[3.2.1]octan-3-yloxy-benzamides as kappa opioid receptor antagonists. Part 2. |
| AID147989 | Antagonist activity on agonist (U50,488) stimulated [35S]GTP-gamma-S, binding in cloned opioid receptor kappa 1 | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | Identification of the first trans-(3R,4R)- dimethyl-4-(3-hydroxyphenyl)piperidine derivative to possess highly potent and selective opioid kappa receptor antagonist activity. |
| AID229766 | Ratio of Inhibition of [35S]GTP-gamma-S, binding in cloned opioid receptor (mu/kappa) | 2003 | Journal of medicinal chemistry, May-08, Volume: 46, Issue:10 | 2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy. |
| AID747946 | Selectivity ratio of Ke for human delta opioid receptor to Ke for human kappa opioid receptor | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Discovery of N-{4-[(3-hydroxyphenyl)-3-methylpiperazin-1-yl]methyl-2-methylpropyl}-4-phenoxybenzamide analogues as selective kappa opioid receptor antagonists. |
| AID502177 | Displacement of [3H]U69593 from kappa opioid receptor in guinea pig cerebellum | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17 | Synthesis of pyrrolomorphinan derivatives as kappa opioid agonists. |
| AID482608 | Antagonist activity at human recombinant kappa opioid receptor expressed in CHO cells assessed as inhibition of U69593-induced [35S]GTPgammaS binding | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Analogues of (3R)-7-hydroxy-N-[(1S)-1-{[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl}-2-methylpropyl)-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide (JDTic). Synthesis and in vitro and in vivo opioid receptor antagonist activity. |
| AID442695 | Ratio of Ke for human cloned delta opioid receptor to Ke for human cloned kappa opioid receptor | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23 | Synthesis and in vitro opioid receptor functional antagonism of methyl-substituted analogues of (3R)-7-hydroxy-N-[(1S)-1-{[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl}-2-methylpropyl]-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide (JDTic). |
| AID149144 | Binding affinity for k opioid receptor was determined using [3H]U-69593 radioligand in Guinea pig brain membranes | 1993 | Journal of medicinal chemistry, Jan-08, Volume: 36, Issue:1 | A remarkable change of opioid receptor selectivity on the attachment of a peptidomimetic kappa address element to the delta antagonist, natrindole: 5'-[N2-alkylamidino)methyl]naltrindole derivatives as a novel class of kappa opioid receptor antagonists. |
| AID149758 | Antagonistic activity against SNC-80 and guinea pig caudate Opioid receptor delta 1 in [35S]GTP-gamma-S, assay | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 | Identification of (3R)-7-hydroxy-N-((1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)- 3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl)-1,2,3,4-tetrahydro- 3-isoquinolinecarboxamide as a novel potent and selective opioid kappa receptor antagonist. |
| AID381428 | Inhibition of kappa opioid dependent ERK1/2 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. |
| AID229765 | Ratio of Inhibition of [35S]GTP-gamma-S, binding in cloned opioid receptor (delta/kappa) | 2003 | Journal of medicinal chemistry, May-08, Volume: 46, Issue:10 | 2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy. |
| AID148964 | Inhibition of [35S]GTP-gamma-S, binding in cloned Opioid receptor kappa 1 stimulated by U69, 593 | 2003 | Journal of medicinal chemistry, May-08, Volume: 46, Issue:10 | 2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy. |
| AID226789 | Ratio of antagonist activities at kappa versus delta receptors | 2003 | Bioorganic & medicinal chemistry letters, Feb-10, Volume: 13, Issue:3 | Synthesis, opioid receptor binding, and functional activity of 5'-substituted 17-cyclopropylmethylpyrido[2',3':6,7]morphinans. |
| AID152389 | Displacement of [3H]- diprenorphine from mu-receptor expressed in HEK 293 cells | 2001 | Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6 | Investigation of the selectivity of oxymorphone- and naltrexone-derived ligands via site-directed mutagenesis of opioid receptors: exploring the "address" recognition locus. |
| AID152229 | inhibition of stimulation of [35S]GTP-gamma-S, binding produced by the selective agonist (DAMGO, mu-receptor), in guinea pig caudate membranes | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | Identification of the first trans-(3R,4R)- dimethyl-4-(3-hydroxyphenyl)piperidine derivative to possess highly potent and selective opioid kappa receptor antagonist activity. |
| AID381437 | Increase of JNK phosphorylation in U50488 treated HEK293 cells expressing GFP tagged kappa opioid receptor relative to U50,488 | 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. |
| AID1528104 | Antagonist activity at human KOR expressed in CHO cell membranes assessed as inhibition of U50,488H-stiumulated [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting | |||
| AID261108 | Inhibition of U69,593 stimulated [35S]GTP-gamma-S binding to cloned human kappa opioid receptor expressed in CHO cells | 2006 | Journal of medicinal chemistry, Mar-09, Volume: 49, Issue:5 | N-substituted 4beta-methyl-5-(3-hydroxyphenyl)-7alpha-amidomorphans are potent, selective kappa opioid receptor antagonists. |
| AID232068 | Compound was tested for antagonist activity against mu opioid receptor on electrically stimulated guinea pig ileal longitudinal muscle myenteric plexus (GPI) at 100 nM using M as agonist ligand. IC50 | 1991 | Journal of medicinal chemistry, Apr, Volume: 34, Issue:4 | Role of the spacer in conferring kappa opioid receptor selectivity to bivalent ligands related to norbinaltorphimine. |
| AID151589 | Ability to displace [3H]DAMGO from Opioid receptor mu 1 of rat brain | 2002 | Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16 | Discovery of an opioid kappa receptor selective pure antagonist from a library of N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphans. |
| AID516455 | Antagonist activity at human delta opioid receptor assessed as inhibition of SNC80-stimulated [35S]GTPgammaS binding | 2010 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 20, Issue:19 | Discovery of 8-azabicyclo[3.2.1]octan-3-yloxy-benzamides as selective antagonists of the kappa opioid receptor. Part 1. |
| AID442691 | Antagonist activity at human cloned mu opioid receptor expressed in CHO cells assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23 | Synthesis and in vitro opioid receptor functional antagonism of methyl-substituted analogues of (3R)-7-hydroxy-N-[(1S)-1-{[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl}-2-methylpropyl]-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide (JDTic). |
| AID231494 | Ratio between Kappa receptor, Mu receptor and Delta receptor; 1/35/22 | 2001 | Journal of medicinal chemistry, Sep-13, Volume: 44, Issue:19 | [2',6'-Dimethyltyrosine]dynorphin A(1-11)-NH2 analogues lacking an N-terminal amino group: potent and selective kappa opioid antagonists. |
| AID147825 | compound was tested for antagonist activity against Opioid receptor delta 1 in mouse vas deferens (MVD) smooth muscle preparation at 100 nM using DADLE as agonist | 1991 | Journal of medicinal chemistry, Apr, Volume: 34, Issue:4 | Role of the spacer in conferring kappa opioid receptor selectivity to bivalent ligands related to norbinaltorphimine. |
| AID238175 | Antagonistic activity against human opioid receptor kappa 1 expressed in CHO cells in [35S]GTP gamma S assay | 2005 | Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5 | Major effect of pyrrolic N-benzylation in norbinaltorphimine, the selective kappa-opioid receptor antagonist. |
| AID230643 | Ke ratio measured as the ke values of mu receptor (GPI)/kappa receptor(MVD) using EK/M as the agonist. | 1991 | Journal of medicinal chemistry, Apr, Volume: 34, Issue:4 | Role of the spacer in conferring kappa opioid receptor selectivity to bivalent ligands related to norbinaltorphimine. |
| AID1245412 | Selectivity ratio of Ke for cloned human delta opioid receptor to Ke for cloned human kappa opioid receptor | 2015 | Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19 | Design, synthesis, and pharmacological evaluation of JDTic analogs to examine the significance of the 3- and 4-methyl substituents. |
| AID231935 | Ratio for binding affinity against CHO cells transfected with cloned human delta opioid receptor to that of k opioid receptor | 2000 | Bioorganic & medicinal chemistry letters, Oct-16, Volume: 10, Issue:20 | Selective kappa-opioid antagonists related to naltrindole. Effect of side-chain spacer in the 5'-amidinoalkyl series. |
| AID152223 | Opioid antagonist potency, determined in guinea pig ileum (GPI) preparation, using morphine (mu-opioid) as agonist (Ke=antagonist/IC50 ratio -1) | 2001 | Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13 | Transformation of a kappa-opioid receptor antagonist to a kappa-agonist by transfer of a guanidinium group from the 5'- to 6'-position of naltrindole. |
| AID502619 | Antagonist activity at human mu opioid receptor expressed in HEK cells assessed as inhibition of DAMGO-induced [35S]GTPgammaS binding | 2010 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 20, Issue:18 | SAR development of a series of 8-azabicyclo[3.2.1]octan-3-yloxy-benzamides as kappa opioid receptor antagonists. Part 2. |
| AID442693 | Antagonist activity at human cloned kappa opioid receptor expressed in CHO cells assessed as inhibition of U69593-stimulated [35S]GTPgammaS binding | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23 | Synthesis and in vitro opioid receptor functional antagonism of methyl-substituted analogues of (3R)-7-hydroxy-N-[(1S)-1-{[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl}-2-methylpropyl]-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide (JDTic). |
| AID631394 | Agonist activity at human opioid delta receptor expressed in HEK293 cells assessed as stimulation of [35S]-GTPgammaS binding at 10 uM | 2011 | Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23 | Discovery of aminobenzyloxyarylamides as κ opioid receptor selective antagonists: application to preclinical development of a κ opioid receptor antagonist receptor occupancy tracer. |
| AID230223 | Inhibitory concentration was tested on electrically stimulated guinea pig ileal longitudinal muscle using ethylketazocine as kappa opioid receptor agonist at 100 nM of the compound | 1994 | Journal of medicinal chemistry, May-13, Volume: 37, Issue:10 | Structure-activity relationship of N17'-substituted norbinaltorphimine congeners. Role of the N17' basic group in the interaction with a putative address subsite on the kappa opioid receptor. |
| AID229503 | Ratio of IC50 in the presence of DADLE to that of control IC50 in guinea pig ileum at 20 nM | 1988 | Journal of medicinal chemistry, Jul, Volume: 31, Issue:7 | Only one pharmacophore is required for the kappa opioid antagonist selectivity of norbinaltorphimine. |
| AID232689 | Selectivity ratio of Ke at delta opioid receptor to Ki at kappa opioid receptor | 2002 | Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16 | Discovery of an opioid kappa receptor selective pure antagonist from a library of N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphans. |
| AID73191 | Maximal inhibition of compound was measured on guinea pig ileal longitudinal muscle (GPI) preparation at 1 uM concentration | 1991 | Journal of medicinal chemistry, Apr, Volume: 34, Issue:4 | Role of the spacer in conferring kappa opioid receptor selectivity to bivalent ligands related to norbinaltorphimine. |
| AID232138 | Ratio of (Ke) mu-opioid receptor to that of (Ke) kappa-opioid receptor | 2003 | Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25 | Guanidino N-substituted and N,N-disubstituted derivatives of the kappa-opioid antagonist GNTI. |
| AID149136 | Binding affinity of compound was measured against Opioid receptor kappa 1 on electrically stimulated guinea pig ileal longitudinal muscle myenteric plexus (GPI) at 100 nM preparation using U-50,488H as agonist | 1991 | Journal of medicinal chemistry, Apr, Volume: 34, Issue:4 | Role of the spacer in conferring kappa opioid receptor selectivity to bivalent ligands related to norbinaltorphimine. |
| AID148789 | Ratio of IC50 of [D-Ala2,D-Leu5]enkephalin (DADLE) in the presence (100 nM) to that of [(DADLE) alone, against delta opioid receptor in mouse vas deferens preparation | 1993 | Journal of medicinal chemistry, Jan-08, Volume: 36, Issue:1 | A remarkable change of opioid receptor selectivity on the attachment of a peptidomimetic kappa address element to the delta antagonist, natrindole: 5'-[N2-alkylamidino)methyl]naltrindole derivatives as a novel class of kappa opioid receptor antagonists. |
| AID222423 | Antagonist activity determined in the guinea pig assay against U50,488 at 1 uM | 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. |
| AID150832 | Ability to inhibit stimulation of [35S]GTP-gamma-S, binding in cloned human Opioid receptor mu 1 transfected in CHO cells using [3H]DAMGO as radioligand | 2002 | Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16 | Discovery of an opioid kappa receptor selective pure antagonist from a library of N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphans. |
| AID229764 | Ratio of Inhibition of [35S]GTP-gamma-S, binding in cloned human opioid receptor (mu/kappa) | 2003 | Journal of medicinal chemistry, May-08, Volume: 46, Issue:10 | 2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy. |
| AID232690 | Selectivity ratio of Ke at mu opioid receptor to Ki at kappa opioid receptor | 2002 | Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16 | Discovery of an opioid kappa receptor selective pure antagonist from a library of N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphans. |
| AID227092 | Ratio of the IC50 of Kappa receptor agonist, ethylketazocine in the presence of compound in GPI divided by the control IC50. | 2000 | Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14 | Potent and selective indolomorphinan antagonists of the kappa-opioid receptor. |
| AID150839 | Inhibition of [35S]GTP-gamma-S, binding in cloned human Opioid receptor mu 1 stimulated by DAMGO | 2003 | Journal of medicinal chemistry, May-08, Volume: 46, Issue:10 | 2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy. |
| AID1245409 | Antagonist activity at cloned human delta opioid receptor assessed as inhibition of DPDPE-induced [35S]GTPgammaS binding | 2015 | Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19 | Design, synthesis, and pharmacological evaluation of JDTic analogs to examine the significance of the 3- and 4-methyl substituents. |
| AID256846 | Selectivity for cloned human mu opioid receptor over kappa opioid receptor | 2005 | Journal of medicinal chemistry, Dec-29, Volume: 48, Issue:26 | N-substituted cis-4a-(3-hydroxyphenyl)-8a-methyloctahydroisoquinolines are opioid receptor pure antagonists. |
| AID150035 | Inhibition of stimulation of [35S]GTP-gamma-S, binding produced by the selective agonist (SNC-80, delta-receptor), in guinea pig caudate membranes | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | Identification of the first trans-(3R,4R)- dimethyl-4-(3-hydroxyphenyl)piperidine derivative to possess highly potent and selective opioid kappa receptor antagonist activity. |
| AID450030 | Antagonist activity at delta opioid receptor expressed in HEK293 cells assessed as inhibition of compound 14-induced [35S]GTPgammaS binding | 2009 | Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18 | Synthesis and pharmacological evaluation of 6-naltrexamine analogs for alcohol cessation. |
| AID311283 | Selectivity for antagonist activity at human mu opioid receptor to kappa opioid receptor expressed in CHO cells by [35S]GTP-gamma-S assay | 2007 | Journal of natural products, Aug, Volume: 70, Issue:8 | Flavonoids as opioid receptor ligands: identification and preliminary structure-activity relationships. |
| AID1184631 | Antinociceptive activity in mouse assessed as inhibition of EM-2-induced jumping at 1 ug, icv by hot-plate test | 2014 | Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17 | Antinociceptive and antidepressant-like action of endomorphin-2 analogs with proline surrogates in position 2. |
| AID233364 | Selectivity ratio of of mu and kappa opioid receptor | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 | Identification of (3R)-7-hydroxy-N-((1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)- 3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl)-1,2,3,4-tetrahydro- 3-isoquinolinecarboxamide as a novel potent and selective opioid kappa receptor antagonist. |
| AID147947 | Percent stimulation of [35S]GTP-gamma-S, binding in recombinant human Opioid receptor delta 1 transfected into CHO cells | 2003 | Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8 | 14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles. |
| AID148007 | Binding affinity towards human cloned Opioid receptor kappa 1 using [3H]U-69593 | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 | Identification of (3R)-7-hydroxy-N-((1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)- 3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl)-1,2,3,4-tetrahydro- 3-isoquinolinecarboxamide as a novel potent and selective opioid kappa receptor antagonist. |
| AID148958 | Binding affinity of compound was measured against Opioid receptor kappa 1 on electrically stimulated guinea pig ileal longitudinal muscle myenteric plexus (GPI) at 100 nM preparation using U-50,488H as agonist | 1991 | Journal of medicinal chemistry, Apr, Volume: 34, Issue:4 | Role of the spacer in conferring kappa opioid receptor selectivity to bivalent ligands related to norbinaltorphimine. |
| AID148249 | Compound was evaluated for its binding affinity to CHO cells expressing cloned human Opioid receptor delta 1 by displacement of [3H]Cl-DPDPE | 2000 | Bioorganic & medicinal chemistry letters, Oct-16, Volume: 10, Issue:20 | Selective kappa-opioid antagonists related to naltrindole. Effect of side-chain spacer in the 5'-amidinoalkyl series. |
| AID482617 | Intrinsic activity at human recombinant mu opioid receptor expressed in CHO cells up to 10 uM | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Analogues of (3R)-7-hydroxy-N-[(1S)-1-{[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl}-2-methylpropyl)-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide (JDTic). Synthesis and in vitro and in vivo opioid receptor antagonist activity. |
| AID246697 | In vivo effective concentration for agonist activity in mouse tail withdrawal assay for antinociception after 24 hr of pre treatment with U-69,593 icv administration (10 nmol) | 2005 | Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5 | Major effect of pyrrolic N-benzylation in norbinaltorphimine, the selective kappa-opioid receptor antagonist. |
| AID574376 | Displacement of [3H]U69593 from kappa opioid receptor in guinea pig cerebellum | 2011 | Bioorganic & medicinal chemistry, Feb-01, Volume: 19, Issue:3 | Synthesis of 6,14-epoxymorphinan derivatives and their pharmacologies. |
| AID239328 | Inhibition of [3H]DAMGO binding to human Mu opioid receptor expressed in CHO cells | 2004 | Journal of medicinal chemistry, Oct-07, Volume: 47, Issue:21 | Identification of a new scaffold for opioid receptor antagonism based on the 2-amino-1,1-dimethyl-7-hydroxytetralin pharmacophore. |
| AID152227 | Binding affinity was measured on mu opioid receptor | 2001 | Journal of medicinal chemistry, Sep-13, Volume: 44, Issue:19 | [2',6'-Dimethyltyrosine]dynorphin A(1-11)-NH2 analogues lacking an N-terminal amino group: potent and selective kappa opioid antagonists. |
| AID229882 | Selectivity ratio, ratio of binding affinity of delta to kappa opioid receptor | 2000 | Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14 | Potent and selective indolomorphinan antagonists of the kappa-opioid receptor. |
| AID232459 | Selectivity ratio between kappa-opioid receptor to mu-opioid receptor | 1993 | Journal of medicinal chemistry, Aug-06, Volume: 36, Issue:16 | Synthesis and kappa-opioid antagonist selectivity of a norbinaltorphimine congener. Identification of the address moiety required for kappa-antagonist activity. |
| AID609329 | Reversal of chloroquine-resistance in Plasmodium chabaudi infected in mouse at 10 mg/kg, po coadministered with chloroquine 3 mg/kg, iv administered for 3 consecutive days measured on day 4 | 2011 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16 | Opioid δ₁ receptor antagonist 7-benzylidenenaltrexone as an effective resistance reverser for chloroquine-resistant Plasmodium chabaudi. |
| AID230901 | Ratio of antagonistic activity at delta to kappa receptor | 1988 | Journal of medicinal chemistry, Jul, Volume: 31, Issue:7 | Only one pharmacophore is required for the kappa opioid antagonist selectivity of norbinaltorphimine. |
| AID311282 | Antagonist activity at human delta opioid receptor expressed in CHO cells by [35S]GTPgammaS assay | 2007 | Journal of natural products, Aug, Volume: 70, Issue:8 | Flavonoids as opioid receptor ligands: identification and preliminary structure-activity relationships. |
| AID150837 | Antagonistic activity against human cloned Opioid receptor mu 1 using DAMGO in [35S]GTP-gamma-S, assay | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 | Identification of (3R)-7-hydroxy-N-((1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)- 3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl)-1,2,3,4-tetrahydro- 3-isoquinolinecarboxamide as a novel potent and selective opioid kappa receptor antagonist. |
| AID149756 | Antagonistic activity at Opioid receptor delta 1 in electrically stimulated Guinea pig ileum using DADLE as the agonist at 20 nM | 1988 | Journal of medicinal chemistry, Jul, Volume: 31, Issue:7 | Only one pharmacophore is required for the kappa opioid antagonist selectivity of norbinaltorphimine. |
| AID147877 | Ability to inhibit stimulation of [35S]GTP-gamma-S, binding in cloned human Opioid receptor kappa 1 transfected in CHO cells using [3H]-U-69,593 as radioligand | 2002 | Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16 | Discovery of an opioid kappa receptor selective pure antagonist from a library of N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphans. |
| AID232063 | Compound was tested for antagonist activity against kappa opioid receptor on electrically stimulated guinea pig ileal longitudinal muscle myenteric plexus (GPI) at 100 nM using U-50,488H as agonist ligand. | 1991 | Journal of medicinal chemistry, Apr, Volume: 34, Issue:4 | Role of the spacer in conferring kappa opioid receptor selectivity to bivalent ligands related to norbinaltorphimine. |
| AID261110 | Selectivity for human kappa opioid receptor over human delta opioid receptor | 2006 | Journal of medicinal chemistry, Mar-09, Volume: 49, Issue:5 | N-substituted 4beta-methyl-5-(3-hydroxyphenyl)-7alpha-amidomorphans are potent, selective kappa opioid receptor antagonists. |
| AID410721 | Ratio of Ki for human mu opioid receptor to Ki for human kappa opioid receptor expressed in CHO cells | 2009 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 19, Issue:1 | Syntheses and opioid receptor binding properties of carboxamido-substituted opioids. |
| AID603174 | Displacement of [125I]-IBNtxA from KOR-1 expressed in CHO cells | 2011 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 21, Issue:13 | Generation of novel radiolabeled opiates through site-selective iodination. |
| AID410718 | Displacement of [3H]DAMGO form human mu opioid receptor expressed in CHO cells | 2009 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 19, Issue:1 | Syntheses and opioid receptor binding properties of carboxamido-substituted opioids. |
| AID230222 | Inhibitory concentration was tested on electrically stimulated guinea pig ileal longitudinal muscle using Morphine as mu opioid receptor agonist at 100 nM of the compound | 1994 | Journal of medicinal chemistry, May-13, Volume: 37, Issue:10 | Structure-activity relationship of N17'-substituted norbinaltorphimine congeners. Role of the N17' basic group in the interaction with a putative address subsite on the kappa opioid receptor. |
| AID747949 | Antagonist activity at human kappa opioid receptor expressed in CHO cells assessed as inhibition of U69,593-stimulated [35S]GTPgammaS binding | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Discovery of N-{4-[(3-hydroxyphenyl)-3-methylpiperazin-1-yl]methyl-2-methylpropyl}-4-phenoxybenzamide analogues as selective kappa opioid receptor antagonists. |
| AID151766 | Effect on binding affinity of mutational exchange of Lys303 in the Opioid receptor mu 1 in transiently expressed rat cos-7 cells activity expressed as binding affinity. | 1998 | Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25 | Mutational evidence for a common kappa antagonist binding pocket in the wild-type kappa and mutant mu[K303E] opioid receptors. |
| AID442692 | Antagonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTPgammaS binding | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23 | Synthesis and in vitro opioid receptor functional antagonism of methyl-substituted analogues of (3R)-7-hydroxy-N-[(1S)-1-{[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl}-2-methylpropyl]-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide (JDTic). |
| AID381438 | Reversal of inhibition of U50488-induced analgesic activity against C57BL/6 mouse assessed as tail withdrawal latency at 10 mg/kg, ip after 8 days in presence of SP600125 | 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. |
| AID147854 | Antagonistic activity in the Opioid receptor kappa 1-mediated [35S]GTP-gamma-S, binding assay against 50 nM U-50,488 | 2003 | Journal of medicinal chemistry, May-22, Volume: 46, Issue:11 | Structure-activity relationships of dynorphin a analogues modified in the address sequence. |
| AID148175 | Binding affinity using [3H]diprenorphine as the radioligand against E297A mutant Opioid receptor kappa 1 in COS-7 cells | 2000 | Journal of medicinal chemistry, Apr-20, Volume: 43, Issue:8 | Binding of norbinaltorphimine (norBNI) congeners to wild-type and mutant mu and kappa opioid receptors: molecular recognition loci for the pharmacophore and address components of kappa antagonists. |
| AID381434 | Effect on mu opioid dependent JNK phosphorylation in U50488 treated HEK293 cells expressing GFP tagged mu opioid receptor 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. |
| AID151614 | Binding affinity on HEK293 cells transiently transfected with plasmids encoding the rat Opioid receptor mu 1 | 2000 | Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14 | Potent and selective indolomorphinan antagonists of the kappa-opioid receptor. |
| AID147908 | Binding affinity determined on Opioid receptor mu 1 in Guinea pig brain membranes using radioligand [3H]DAMGO | 1998 | Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26 | Identification of an opioid kappa receptor subtype-selective N-substituent for (+)-(3R,4R)-dimethyl-4-(3-hydroxyphenyl)piperidine. |
| AID148974 | Opioid receptor kappa 1 Antagonism (100 nM) is expressed as (Ke = [antagonist] / (IC50 ratio -1) | 2000 | Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14 | Potent and selective indolomorphinan antagonists of the kappa-opioid receptor. |
| AID148965 | Inhibition of [35S]GTP-gamma-S, binding in guines pig caudate stimulated by U50, 488 of Opioid receptor kappa 1 | 2003 | Journal of medicinal chemistry, May-08, Volume: 46, Issue:10 | 2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy. |
| AID231938 | Ratio for binding affinity against CHO cells transfected with cloned human mu opioid receptor to that of k opioid receptor | 2000 | Bioorganic & medicinal chemistry letters, Oct-16, Volume: 10, Issue:20 | Selective kappa-opioid antagonists related to naltrindole. Effect of side-chain spacer in the 5'-amidinoalkyl series. |
| AID631347 | Antagonist activity at human opioid delta receptor expressed in HEK293 cells assessed as inhibition of DPDPE-induced [35S]GTP-gamma-S binding after 4 hrs by scintillation counting | 2011 | Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23 | Discovery of aminobenzyloxyarylamides as κ opioid receptor selective antagonists: application to preclinical development of a κ opioid receptor antagonist receptor occupancy tracer. |
| 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. |
| AID150022 | Antagonistic activity for Opioid receptor mu 1 in guinea pig ileal longitudinal muscle at 20 nM | 1988 | Journal of medicinal chemistry, Apr, Volume: 31, Issue:4 | Binaltorphimine-related bivalent ligands and their kappa opioid receptor antagonist selectivity. |
| AID482607 | Antagonist activity at human recombinant delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-induced [35S]GTPgammaS binding | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Analogues of (3R)-7-hydroxy-N-[(1S)-1-{[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl}-2-methylpropyl)-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide (JDTic). Synthesis and in vitro and in vivo opioid receptor antagonist activity. |
| AID149643 | Ability to displace [3H]DADLE from Opioid receptor delta 1 of rat brain | 2002 | Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16 | Discovery of an opioid kappa receptor selective pure antagonist from a library of N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphans. |
| AID410722 | Ratio of Ki for human delta opioid receptor to Ki for human kappa opioid receptor expressed in CHO cells | 2009 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 19, Issue:1 | Syntheses and opioid receptor binding properties of carboxamido-substituted opioids. |
| AID229763 | Ratio of Inhibition of [35S]GTP-gamma-S, binding in cloned human opioid receptor (delta/kappa) | 2003 | Journal of medicinal chemistry, May-08, Volume: 46, Issue:10 | 2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy. |
| AID1232254 | Antagonist activity against HA-tagged human recombinant kappa opioid receptor expressed in CHO cells assessed as inhibition of U69,593-induced ERK phosphorylation pre-incubated with compound before U69,593 stimulation for 10 mins | 2015 | Bioorganic & medicinal chemistry, Jul-15, Volume: 23, Issue:14 | Potency enhancement of the κ-opioid receptor antagonist probe ML140 through sulfonamide constraint utilizing a tetrahydroisoquinoline motif. |
| AID230902 | Ratio of antagonistic activity at mu to kappa receptor | 1988 | Journal of medicinal chemistry, Jul, Volume: 31, Issue:7 | Only one pharmacophore is required for the kappa opioid antagonist selectivity of norbinaltorphimine. |
| 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. |
| AID631360 | Displacement of [3H]diprenorphine from human opioid mu receptor expressed in CHO cells after 120 mins by scintillation counting | 2011 | Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23 | Discovery of aminobenzyloxyarylamides as κ opioid receptor selective antagonists: application to preclinical development of a κ opioid receptor antagonist receptor occupancy tracer. |
| AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347049 | Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
| AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID1347050 | Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
| AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID1347045 | Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
| AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID504836 | Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation | 2002 | The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16 | Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells. |
| AID588378 | qHTS for Inhibitors of ATXN expression: Validation | |||
| AID588349 | qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay | |||
| AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1159607 | Screen for inhibitors of RMI FANCM (MM2) intereaction | 2016 | Journal of biomolecular screening, Jul, Volume: 21, Issue:6 | A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway. |
| AID1346411 | Rat kappa receptor (Opioid receptors) | 1993 | The Biochemical journal, Nov-01, Volume: 295 ( Pt 3) | Molecular cloning of a rat kappa opioid receptor reveals sequence similarities to the mu and delta opioid receptors. |
| AID1346329 | Human kappa receptor (Opioid receptors) | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Hybrid bivalent ligands with opiate and enkephalin pharmacophores. |
| AID1346329 | Human kappa receptor (Opioid receptors) | 1997 | The Journal of pharmacology and experimental therapeutics, Aug, Volume: 282, Issue:2 | Activation of the cloned human kappa opioid receptor by agonists enhances [35S]GTPgammaS binding to membranes: determination of potencies and efficacies of ligands. |
| AID1346329 | Human kappa receptor (Opioid receptors) | 1998 | NIDA research monograph, Mar, Volume: 178 | Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications. |
| AID1346341 | Mouse kappa receptor (Opioid receptors) | 1993 | Proceedings of the National Academy of Sciences of the United States of America, Jul-15, Volume: 90, Issue:14 | Cloning and functional comparison of kappa and delta opioid receptors from mouse brain. |
| AID1346364 | Human mu receptor (Opioid receptors) | 1998 | NIDA research monograph, Mar, Volume: 178 | Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications. |
| AID1346329 | Human kappa receptor (Opioid receptors) | 1995 | Proceedings of the National Academy of Sciences of the United States of America, Jul-18, Volume: 92, Issue:15 | kappa-Opioid receptor in humans: cDNA and genomic cloning, chromosomal assignment, functional expression, pharmacology, and expression pattern in the central nervous system. |
| AID1346329 | Human kappa receptor (Opioid receptors) | 1995 | Life sciences, , Volume: 56, Issue:9 | Cloning of a human kappa opioid receptor from the brain. |
| AID1346411 | Rat kappa receptor (Opioid receptors) | 1993 | Proceedings of the National Academy of Sciences of the United States of America, Nov-01, Volume: 90, Issue:21 | Cloning and pharmacological characterization of a rat kappa opioid receptor. |
| AID1346361 | Human delta receptor (Opioid receptors) | 1998 | NIDA research monograph, Mar, Volume: 178 | Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications. |
| AID1346373 | Mouse delta receptor (Opioid receptors) | 1993 | Proceedings of the National Academy of Sciences of the United States of America, Jul-15, Volume: 90, Issue:14 | Cloning and functional comparison of kappa and delta opioid receptors from mouse brain. |
| AID1346411 | Rat kappa receptor (Opioid receptors) | 1993 | The Biochemical journal, Nov-01, Volume: 295 ( Pt 3) | Molecular cloning and expression of a rat kappa opioid receptor. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 17 (1.87) | 18.7374 |
| 1990's | 355 (39.10) | 18.2507 |
| 2000's | 297 (32.71) | 29.6817 |
| 2010's | 216 (23.79) | 24.3611 |
| 2020's | 23 (2.53) | 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 (28.90) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 4 (0.44%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 914 (99.56%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||