naltrindole: delta opioid receptor antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 5497186 |
| CHEMBL ID | 567175 |
| CHEMBL ID | 1237164 |
| CHEBI ID | 81528 |
| SCHEMBL ID | 12013202 |
| MeSH ID | M0155942 |
| Synonym |
|---|
| gtpl1641 |
| 4,8-methanobenzofuro(2,3-a)pyrido(4,3-b)carbazole-1,8a(9h)-diol, 7-(cyclopropylmethyl)-5,6,7,8,14,14b-hexahydro-, (4bs,8r,8as,14br)- |
| 4,8-methanobenzofuro(2,3-a)pyrido(4,3-b)carbazole-1,8a(9h)-diol, 7-(cyclopropylmethyl)-5,6,7,8,14,14b-hexahydro-, (8r-(4bs*,8alpha,8abeta,14bbeta))- |
| 4,8-methanobenzofuro[2,3-a]pyrido[4,3-b]carbazole-1,8a(9h)-diol, 7-(cyclopropylmethyl)-5,6,7,8,14,14b-hexahydro-, [8r-(4bs*,8alpha,8abeta,14bbeta)]- |
| 4,8-methanobenzofuro[2,3-a]pyrido[4,3-b]carbazole-1,8a(9h)-diol, 7-(cyclopropylmethyl)-5,6,7,8,14,14b-hexahydro-, (4bs,8r,8as,14br)- |
| 4,8-methanobenzofuro[2,3-a]pyrido[4,3-b]carbazole-1,8a(9h)-diol, 7-(cyclopropylmethyl)-5,6,7,8,14,14b-hexahydro-, (4bs,8r,8as,14br)- (9ci) |
| 111555-53-4 |
| 17-cyclopropylmethyl-6,7-dehydro-4,5-epoxy-3,14-dihydroxy-6,7,2',3'-indolomorphinan |
| [3h]-naltrindole |
| naltrindole |
| NTI , |
| HMS2089E12 |
| C18128 |
| CHEMBL567175 |
| chebi:81528 , |
| CHEMBL1237164 , |
| bdbm50370067 |
| g167z38qa4 , |
| unii-g167z38qa4 |
| nih 10589 |
| (4bs,8r,8as,14br)-7-(cyclopropylmethyl)-5,6,7,8,14,14b-hexahydro-4,8-methano[1]benzofuro[2,3-a]pyrido[4,3-b]carbazole-1,8a(9h)-diol |
| ej4 , |
| [3h]naltrindole |
| gtpl3829 |
| WIYUZYBFCWCCQJ-IFKAHUTRSA-N |
| SCHEMBL12013202 |
| DTXSID60912216 |
| Q3743642 |
| (1s,2s,13r,21r)-22-(cyclopropylmethyl)-14-oxa-11,22-diazaheptacyclo[13.9.1.01,13.02,21.04,12.05,10.019,25]pentacosa-4(12),5,7,9,15,17,19(25)-heptaene-2,16-diol |
Naltrindole (1) (NTI) is a highly potent and selective delta-opioid receptor antagonist. It preferentially antagonizes a subset of selective Delta-Opioid agonists. Nal Trindole is a novel delta-OPioid antagonist which is highly potent in vitro.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Naltrindole did not produce any antinociceptive effect alone and did not antagonize the antinociceptive actions of morphine after either i.th." | ( Naltrindole, an opioid delta antagonist, blocks the enhancement of morphine-antinociception induced by a CCKB antagonist in the rat. Kovelowski, CJ; Ossipov, MH; Porreca, F; Vanderah, T, 1994) | 2.45 |
Naltrindole treatment reduced constitutive phosphorylation of Akt/PKB on serine 473 and threonine 308 in cells. Pretreatment with 7-benzylidenenaltrexone (BNTX) or naltriben (NTB) abolished the morphine-induced place preference in mice.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Naltrindole treatment reduced constitutive phosphorylation of Akt/PKB on serine 473 and threonine 308 in cells." | ( Inhibition of akt/protein kinase B signaling by naltrindole in small cell lung cancer cells. Chen, YL; Law, PY; Loh, HH, 2004) | 1.3 |
| "Naltrindole-treated females showed an increased antinociception when compared to unhandled animals of the same gender." | ( Neonatal naltrindole and handling differently affect morphine antinociception in male and female rats. Alberti, I; Fernández, B; Kitchen, I; Viveros, MP, 1999) | 1.44 |
| "naltrindole pretreatment also prevented significant decreases in latency to onset of slow-wave sleep that were seen in the i.c.v." | ( Naltrindole retards tolerance development to morphine-induced effects on EEG and EEG power spectra. Stamidis, H; Young, GA, 1992) | 2.45 |
| "pretreatment with naltrindole, nor-binaltorphimine, and (-)-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine maleate (MK-801), respectively, did not affect the i.t." | ( Nonopioidergic mechanism mediating morphine-induced antianalgesia in the mouse spinal cord. Fujimoto, JM; Leitermann, RJ; Sun, HS; Thompson, J; Tseng, LF; Wu, HE, 2004) | 0.65 |
| "Pretreatment with naltrindole (a non-selective delta-opioid receptor antagonist) and naltriben (a selective delta 2-opioid receptor antagonist), but not 7-benzylidenenaltrexone (a selective delta 1-opioid receptor antagonist), significantly attenuated the discriminative stimulus properties of cocaine." | ( Attenuation of the discriminative stimulus properties of cocaine by delta-opioid receptor antagonists. Funada, M; Misawa, M; Mori, T; Nagase, H; Suzuki, T, 1994) | 0.61 |
| "Pretreatment with naltrindole (NTI: a non-selective delta-opioid receptor antagonist), 7-benzylidenenaltrexone (BNTX: a selective delta 1-opioid receptor antagonist) or naltriben (NTB: a selective delta 2-opioid receptor antagonist) abolished the morphine-induced place preference in ddY mice in a dose-dependent manner." | ( Blockade of delta-opioid receptors prevents morphine-induced place preference in mice. Kamei, J; Misawa, M; Mizoguchi, H; Nagase, H; Suzuki, T; Yoshiike, M, 1994) | 0.61 |
| "Treatment with naltrindole (0.1, 1, or 10 nmol/5 microliters per rat) significantly blocked naloxone-, a nonspecific antagonist, precipitated butorphanol withdrawal behaviors (escape behavior, teeth-chattering, wet shakes, forepaw tremors, ptosis, diarrhea, body weight loss, and hypothermia) at all doses tested, and decreased ejaculation at 0.1 nmol in butorphanol-infused rats." | ( Involvement of delta-opioid receptors in physical dependence on butorphanol. Ho, IK; Hoskins, B; Jaw, SP, 1993) | 0.63 |
| "treatment with naltrindole, and the two highly selective peptide delta-opioid receptor antagonists H-Tyr-Tic-Phe-Phe-OH (TIPP) and H-Tyr-Tic psi [CH2-NH]-Phe-Phe- OH (TIPP[psi]), on the development of morphine tolerance and dependence." | ( Attenuation of morphine tolerance and dependence with the highly selective delta-opioid receptor antagonist TIPP[psi]. Coderre, TJ; Fundytus, ME; Schiller, PW; Shapiro, M; Weltrowska, G, 1995) | 0.63 |
| "treatment with naltrindole elicited increases in Glu and Asp that were similar, although less marked, than those precipitated by CTOP treatment." | ( Mu- and delta-opioid receptor antagonists precipitate similar withdrawal phenomena in butorphanol and morphine dependence. Feng, YZ; Ho, IK; Rockhold, RW; Tokuyama, S; Zhang, T; Zhu, H, 1996) | 0.63 |
| "Pretreatment with naltrindole indicated that the delta-receptors play an equivalent but minor role in mediating both morphine-6-glucuronide and morphine hyperlocomotion." | ( Morphine-6-glucuronide-induced locomotor stimulation in mice: role of opioid receptors. Aasmundstad, TA; Alkana, RL; Grung, M; Handal, M; Mørland, J; Skurtveit, S, 1998) | 0.62 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "This study investigated whether ethanol combined with low doses of morphine produces rewarding effects in rats." | ( Rewarding effects of ethanol combined with low doses of morphine through dopamine D1 receptors. Ise, Y; Katayama, S; Mori, T; Nagase, H; Suzuki, T, 2013) | 0.39 |
Study confirms the differential involvement of micro and delta receptors in ethanol intake. Naltrindole and naltriben (NTB), delta antagonists, blocked 65-99% of [3H]BNTX specific binding at a dosage of 5.
| Excerpt | Relevance | Reference |
|---|---|---|
| " A dose-response curve was also made for the mu-opioid receptor agonist, morphine." | ( Spinal antinociception by Tyr-D-Ser(otbu)-Gly-Phe-Leu-Thr, a selective delta-opioid receptor agonist. Dickenson, AH; Kalso, EA; McQuay, HJ; Sullivan, AF, 1992) | 0.28 |
| " 1) In the presence of a fixed dose of DPDPE (150 nmol), there was a left shift in the dose-response curve of the mu agonist, with the magnitude of the shifts being greater than those anticipated from a simple additive interaction: PL017 (31-fold) > or = DAMGO (20-fold) > morphine (6." | ( Isobolographic and dose-response analyses of the interaction between intrathecal mu and delta agonists: effects of naltrindole and its benzofuran analog (NTB). Malmberg, AB; Yaksh, TL, 1992) | 0.49 |
| "3 nmol/rat of DADELT II and shifted the dose-response curve to the right, without decreasing the maximum effect." | ( Behavioural effects of deltorphins in rats. Angelucci, F; Negri, L; Noviello, V, 1991) | 0.28 |
| " Administration of U50,488H (3 mg/kg), in conjunction with several doses of cocaine, did not shift the cocaine dose-response curve." | ( Assessment of the discriminative stimulus effects of cocaine in the rat: lack of interaction with opioids. Broadbent, J; Dworkin, SI; Gaspard, TM, ) | 0.13 |
| "5 micrograms), parallel rightward shifts of both morphine and RB 101 (mixed enkephalin-degrading-enzyme inhibitor) dose-response curves, were observed, but the concentration of beta-FNA required to reduce the analgesic responses was about 10 times higher for RB 101 (0." | ( Assessment of endogenous enkephalins efficacy in the hot plate test in mice: comparative study with morphine. Noble, F; Roques, BP, 1995) | 0.29 |
| " This EEG activation was greatly attenuated at DPDPE doses greater than 154 nmol/h, resulting in a U-shaped dose-response curve." | ( Effects of the delta-opioid agonist, [D-Pen2,D-Pen5]-enkephalin, on fetal lamb EEG. Cheng, PY; Soong, Y; Szeto, HH; Wu, DL, 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) | 0.56 |
| " 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) | 0.52 |
| " Dose-response and antagonist testing commenced once stable rates of cocaine SA were achieved." | ( Lack of involvement of delta-opioid receptors in mediating the rewarding effects of cocaine. Babovic-Vuksanovic, D; de Vries, TJ; Elmer, G; Shippenberg, TS, 1995) | 0.29 |
| " Once rats had acquired the discrimination an ethanol dose-response test was conducted." | ( The influence of opioid antagonists on the discriminative stimulus effects of ethanol. Spanagel, R, 1996) | 0.29 |
| " Dose-response curves for 1DMe in the presence of naltrindole or naltrexone, delta- and mu-opioid selective antagonists respectively, indicate that 1DMe preferentially reversed mu-receptor-mediated but increased delta-receptor-mediated analgesia." | ( Differential modulation of mu- and delta-opioid antinociception by neuropeptide FF receptors in young mice. Desprat, C; Zajac, JM, 1997) | 0.55 |
| "), shifted the dose-response relationships to the right for each of the antidepressant agents (dothiepin, amitriptyline, sibutramine, (+)-oxaprotiline and paroxetine)." | ( The involvement of the opioidergic system in the antinociceptive mechanism of action of antidepressant compounds. Gray, AM; Sewell, RD; Spencer, PS, 1998) | 0.3 |
| " In the presence of the opioid receptor antagonists, naloxone or naltrindole, the resulting nefopam dose-response relationships were shifted to the right." | ( The involvement of opioidergic and noradrenergic mechanisms in nefopam antinociception. Gray, AM; Nevinson, MJ; Sewell, RD, 1999) | 0.54 |
| "5 mg kg-1) and the time point at which nociceptive responses were recorded (30 min after the administration of the drug) were chosen on the basis of dose-response (0." | ( Preweanling naltrindole administration differentially affects clonidine induced antinociception and plasma adrenaline levels in male and female neonatal rats. Aguilar, A; Alberti, I; Alguacil, LF; Caamaño, M; Fernández, B; Romero, EM; Viveros, MP, 1999) | 0.68 |
| " 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 |
| " Experiment 3 confirmed the differential involvement of micro and delta receptors in ethanol intake through a more comprehensive dose-response analysis of beta-FNA and naltrindole." | ( Social learning about ethanol in preweanling rats: role of endogenous opioids. Hallmark, RA; Hunt, PS, 2004) | 0.52 |
| " These two compounds also exhibited nanomolar potencies in dose-response experiments performed on wild-type, M262T, Y308H, and C328R CAM receptors." | ( Inverse agonism and neutral antagonism at wild-type and constitutively active mutant delta opioid receptors. Befort, K; Décaillot, FM; Filliol, D; Kieffer, BL; Lazarus, LH; Schiller, PW; Schmidhammer, H; Tryoen-Tóth, P, 2005) | 0.33 |
| " 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 |
| " A distinct dose-response effects of these peptides on cocaine locomotion probably arise from differential functional activation (targeting) of the DOR and MOR by both deltorphins analogs." | ( Involvement of delta and mu opioid receptors in the acute and sensitized locomotor action of cocaine in mice. Gibula-Bruzda, E; Izdebski, J; Kotlinska, JH; Witkowska, E, 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 | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Delta-type opioid receptor | Mus musculus (house mouse) | Kd | 0.0006 | 0.0002 | 0.0887 | 0.5000 | AID257158 |
| Mu-type opioid receptor | Homo sapiens (human) | EC50 (µMol) | 0.0043 | 0.0000 | 0.3263 | 9.4000 | AID148339 |
| Delta-type opioid receptor | Homo sapiens (human) | EC50 (µMol) | 0.0001 | 0.0000 | 0.4332 | 8.3000 | AID148065 |
| Delta-type opioid receptor | Homo sapiens (human) | Kd | 0.0112 | 0.0004 | 0.5147 | 1.9800 | AID277681 |
| Kappa-type opioid receptor | Homo sapiens (human) | EC50 (µMol) | 0.0049 | 0.0000 | 0.2244 | 8.9900 | AID149987 |
| Nociceptin receptor | Homo sapiens (human) | EC50 (µMol) | 0.0039 | 0.0001 | 0.0089 | 0.0630 | AID450027 |
| Mu-type opioid receptor | Cavia porcellus (domestic guinea pig) | EC50 (µMol) | 0.0049 | 0.0000 | 0.0493 | 0.9320 | AID149987 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID148663 | Opioid receptor delta 1 antagonistic activity was measured by the displacement of DADLE in the mouse vas deferens at a concentration of 20 nM | 1990 | Journal of medicinal chemistry, Jun, Volume: 33, Issue:6 | Design of peptidomimetic delta opioid receptor antagonists using the message-address concept. |
| AID152209 | Selectivity ratio of Opioid receptor mu 1 to Opioid receptor delta 1 | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2 | 4'-Arylpyrrolomorphinans: effect of a pyrrolo-N-benzyl substituent in enhancing delta-opioid antagonist activity. |
| AID229267 | Ratio of IC50 in presence of antagonist to that of control IC50 value against kappa opioid receptor using ethylketazocine ligand in guinea pig ileal longitudinal muscle | 1994 | Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5 | Synthesis of naltrexone-derived delta-opioid antagonists. Role of conformation of the delta address moiety. |
| AID1237281 | Selectivity index, ratio of Ki for human KOR to Ki for human DOR | 2015 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15 | Naltrindole derivatives with fluorinated ethyl substituents on the 17-nitrogen as δ opioid receptor inverse agonists. |
| AID149016 | Compound was evaluated for the binding affinity to Opioid receptor mu using [3H]DAMGO as radioligand in guinea pig brain membrane | 1991 | Journal of medicinal chemistry, May, Volume: 34, Issue:5 | Role of spacer and address components in peptidomimetic delta opioid receptor antagonists related to 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. |
| AID148552 | Antagonist activity against kappa-opioid receptor in guinea pig ileum in the presence of ethylketazocine | 1994 | Journal of medicinal chemistry, Jun-10, Volume: 37, Issue:12 | Synthesis and delta-opioid receptor antagonist activity of a naltrindole analogue with a regioisomeric indole moiety. |
| AID148743 | Selectivity ratio towards Opioid receptor kappa 1 to Opioid receptor delta 1 | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2 | 4'-Arylpyrrolomorphinans: effect of a pyrrolo-N-benzyl substituent in enhancing delta-opioid antagonist activity. |
| AID310938 | Agonist activity at rat delta opioid receptor expressed in C6 cells assessed as stimulation of [35S]GTP-gamma-S binding relative to BW373U86 | 2007 | Journal of medicinal chemistry, Apr-19, Volume: 50, Issue:8 | Quantitative conformationally sampled pharmacophore for delta opioid ligands: reevaluation of hydrophobic moieties essential for biological activity. |
| AID148835 | Antagonist potency was determined as the ratio of [antagonist] to (IC50 ratio-1) for Opioid receptor kappa 1 | 1990 | Journal of medicinal chemistry, Jun, Volume: 33, Issue:6 | Design of peptidomimetic delta opioid receptor antagonists using the message-address concept. |
| AID149950 | Relative potency to that of [Leu5]- enkephalin | 1993 | Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21 | TIPP[psi]: a highly potent and stable pseudopeptide delta opioid receptor antagonist with extraordinary delta selectivity. |
| AID148242 | Binding affinity towards recombinant human Opioid receptor delta 1 transfected in to CHO cells for the displacement of [3H]Cl-DPDPE (delta) | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2 | 4'-Arylpyrrolomorphinans: effect of a pyrrolo-N-benzyl substituent in enhancing delta-opioid antagonist activity. |
| AID424036 | Selectivity ratio of Ki for mu opioid receptor in rat cerebellum membrane to Ki for delta opioid receptor in rat cerebellum membrane | 2009 | Bioorganic & medicinal chemistry letters, May-15, Volume: 19, Issue:10 | Design and synthesis of novel delta opioid receptor agonists and their pharmacologies. |
| AID689647 | Displacement of [3H]DAMGO from mu opioid receptor in mouse whole brain without cerebellum | 2012 | Bioorganic & medicinal chemistry, Oct-01, Volume: 20, Issue:19 | Synthesis of quinolinomorphinan derivatives as highly selective δ opioid receptor ligands. |
| AID133920 | Agonist vas deferens(MVD) | 1998 | Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14 | 14-Desoxy analogues of naltrindole and 7-spiroindanyloxymorphone: the role of the 14-hydroxy group at delta opioid receptors. |
| AID147999 | Binding affinity in recombinant human Opioid receptor kappa 1 transfected into chinese hamster ovary cells by displacing [3H]U-69593 radioligand | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 | Opioid binding and in vitro profiles of a series of 4-hdroxy-3-methoxyindolomorphinans. Transformation of a delta-selective ligand into a high affinity kappa-selective ligand by introduction of a 5,14-substituted bridge. |
| AID148813 | Antagonistic activity against Opioid receptor delta 1 using [D-Ala2,D-Leu5]enkephalin in mouse vas deferens preparation | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2 | Application of the message-address concept in the design of highly potent and selective non-peptide delta opioid receptor antagonists. |
| AID228132 | Ratio of mu/delta-opioid receptors Binding affinity | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 | Opioid binding and in vitro profiles of a series of 4-hdroxy-3-methoxyindolomorphinans. Transformation of a delta-selective ligand into a high affinity kappa-selective ligand by introduction of a 5,14-substituted bridge. |
| AID415717 | Selectivity ratio of Ki for mu opioid receptor to Ki for delta opioid receptor | 2009 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6 | 14-O-Heterocyclic-substituted naltrexone derivatives as non-peptide mu opioid receptor selective antagonists: design, synthesis, and biological studies. |
| AID148795 | Activity against Opioid receptor delta 1 on electrically stimulated mouse vas deferens using DADLE as agonist | 1997 | Journal of medicinal chemistry, Jun-20, Volume: 40, Issue:13 | Pyrrolomorphinans as delta opioid receptor antagonists. The role of steric hindrance in conferring selectivity. |
| AID232962 | Ke selectivity ratio (kappa/delta) of the compound | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6 | An approach to the design of receptor-type-selective non-peptide antagonists of peptidergic receptors: delta opioid antagonists. |
| AID603173 | Displacement of [125I]-IBNalA from DOR-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. |
| AID148316 | Binding affinity against Opioid receptor kappa 1 binding in ICR mouse brain membranes using the radioligand [3H]U-69593 | 1997 | Journal of medicinal chemistry, Jun-20, Volume: 40, Issue:13 | Pyrrolomorphinans as delta opioid receptor antagonists. The role of steric hindrance in conferring selectivity. |
| AID150852 | Binding affinity for human Opioid receptor mu 1 transfected into chinese hamster ovary cells by displacing [3H]DAMGO radioligand | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 | Opioid binding and in vitro profiles of a series of 4-hdroxy-3-methoxyindolomorphinans. Transformation of a delta-selective ligand into a high affinity kappa-selective ligand by introduction of a 5,14-substituted bridge. |
| AID148945 | Ratio of antagonistic activity against delta receptors in mouse vas deferens in presence and absence of delta agonist DL-II | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Novel deltorphin heptapeptide analogs with potent delta agonist, delta antagonist, or mixed mu antagonist/delta agonist properties. |
| AID1254732 | Antitrichomonal activity against Trichomonas vaginalis after 48 hrs by invert microscope analysis | 2015 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 25, Issue:21 | Investigation of 7-benzylidenenaltrexone derivatives as a novel structural antitrichomonal lead compound. |
| AID149192 | Binding affinity was measured by the displacement of [3H]- DADLE in guinea pig brain membrane of opioid receptor delta | 1990 | Journal of medicinal chemistry, Jun, Volume: 33, Issue:6 | Design of peptidomimetic delta opioid receptor antagonists using the message-address concept. |
| AID149283 | Compound was evaluated for binding affinity of Opioid receptor kappa 1 in guinea pig brain membranes | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6 | An approach to the design of receptor-type-selective non-peptide antagonists of peptidergic receptors: delta opioid antagonists. |
| AID1358124 | Displacement of [3H]diprenorphine from human DOR expressed in African green monkey COS1 cell membranes at 10 uM incubated for 1 hr by scintillation counting method | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Synthesis of 7β-hydroxy-8-ketone opioid derivatives with antagonist activity at mu- and delta-opioid receptors. |
| 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. |
| 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. |
| AID441378 | Agonist activity at rat delta opioid receptor expressed in rat C6 cells assessed as inhibition of forskolin-stimulated cAMP production after 30 mins by radioimmunoassay | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23 | Pentapeptides displaying mu opioid receptor agonist and delta opioid receptor partial agonist/antagonist properties. |
| AID150009 | Antagonist potency against mu opioid receptor was measured in guinea-pig ileal longitudinal muscle using PL-017 | 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. |
| AID1668233 | Displacement of [3H]DPDPE from human delta opioid receptor expressed in CHO cells | 2020 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 30, Issue:12 | Discovery of δ opioid receptor full agonists lacking a basic nitrogen atom and their antidepressant-like effects. |
| AID226819 | Selectivity ratio of mu receptor to the delta opioid receptor in smooth muscle (MVD/GPI) functional assay | 2001 | Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21 | Derivatives of 17-(2-methylallyl)-substituted noroxymorphone: variation of the delta address and its effects on affinity and selectivity for the delta opioid receptor. |
| AID1162886 | Displacement of [3H]U69593 from kappa opioid receptor (unknown origin) expressed in HEK293T cells after 1.5 hrs by radioligand binding assay | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | Michael acceptor approach to the design of new salvinorin A-based high affinity ligands for the kappa-opioid receptor. |
| AID416815 | Displacement of [3H]U69,593 from human kappa opioid receptor expressed in CHO cells after 60 mins by scintillation counting | 2009 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8 | Syntheses of novel high affinity ligands for opioid receptors. |
| 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. |
| AID429153 | Displacement of [3H]DAMGO from human mu opioid receptor expressed in CHO cells | 2009 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16 | Synthesis and opioid receptor activity of indolopropellanes. |
| AID1668236 | Selectivity ratio for Ki for displacement of [3H]DAMGO from human mu opioid receptor expressed in CHO cells to Ki for displacement of [3H]DPDPE from human DOR expressed in CHO cells | 2020 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 30, Issue:12 | Discovery of δ opioid receptor full agonists lacking a basic nitrogen atom and their antidepressant-like effects. |
| AID150840 | The antagonistic activity tested in [35S]-GTP-gamma S Recombinant Human Opioid receptor mu 1 transfected in to CHO cells for the displacement of [3H]DAMGO (mu) | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2 | 4'-Arylpyrrolomorphinans: effect of a pyrrolo-N-benzyl substituent in enhancing delta-opioid antagonist activity. |
| 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. |
| AID149676 | Binding affinity to delta opioid receptor was measured using [3H]DADLE | 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. |
| 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. |
| 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. |
| AID365604 | Binding affinity to guinea pig mu opioid receptor | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Structure-antitussive activity relationships of naltrindole derivatives. Identification of novel and potent antitussive agents. |
| AID151150 | Binding affinity against Opioid receptor mu 1 binding in ICR mouse brain membranes using the radioligand [3H][Ala2,Glyol5]enkephalin | 1997 | Journal of medicinal chemistry, Jun-20, Volume: 40, Issue:13 | Pyrrolomorphinans as delta opioid receptor antagonists. The role of steric hindrance in conferring selectivity. |
| AID239950 | Binding affinity against Opioid receptor kappa 1 from guinea pig brain membranes using [3H]U-69593 | 2005 | Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5 | 3D-QSAR comparative molecular field analysis on opioid receptor antagonists: pooling data from different studies. |
| AID138364 | Agonistic activity in Mouse Vas Deferens | 1999 | Journal of medicinal chemistry, May-06, Volume: 42, Issue:9 | delta Opioid affinity and selectivity of 4-hydroxy-3-methoxyindolomorphinan analogues related to naltrindole. |
| AID134202 | Antagonist potency (Ke) was evaluated | 1998 | Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14 | 14-Desoxy analogues of naltrindole and 7-spiroindanyloxymorphone: the role of the 14-hydroxy group at delta opioid receptors. |
| AID1237278 | Displacement of [3H]DPDPE from human DOR expressed in CHO cells | 2015 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15 | Naltrindole derivatives with fluorinated ethyl substituents on the 17-nitrogen as δ opioid receptor inverse agonists. |
| AID1237280 | Selectivity index, ratio of Ki for human MOR to Ki for human DOR | 2015 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15 | Naltrindole derivatives with fluorinated ethyl substituents on the 17-nitrogen as δ opioid receptor inverse agonists. |
| AID149135 | Binding affinity determined against Opioid receptor kappa 1 from a native receptor in guinea pig | 2003 | Journal of medicinal chemistry, Aug-28, Volume: 46, Issue:18 | Synthesis, biological evaluation, and receptor docking simulations of 2-[(acylamino)ethyl]-1,4-benzodiazepines as kappa-opioid receptor agonists endowed with antinociceptive and antiamnesic activity. |
| AID148950 | Ratio of antagonistic activity against delta receptors in mouse vas deferens in presence and absence of delta agonist leu-enkephalin | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Novel deltorphin heptapeptide analogs with potent delta agonist, delta antagonist, or mixed mu antagonist/delta agonist properties. |
| AID152387 | Displacement of [3H]- diprenorphine from mu-W318A-receptor expressed in HEK 293 | 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. |
| AID147894 | Ability to inhibit GTP-gamma-S binding to Opioid receptor mu 1 of guinea pig caudate. | 1999 | Journal of medicinal chemistry, May-06, Volume: 42, Issue:9 | delta Opioid affinity and selectivity of 4-hydroxy-3-methoxyindolomorphinan analogues related to naltrindole. |
| AID235723 | Relative affinity for guinea pig kappa1 and rat delta receptors | 1998 | Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15 | Synthesis, opioid receptor binding, and bioassay of naltrindole analogues substituted in the indolic benzene moiety. |
| AID141651 | Ability to inhibit binding of [3H]DAMGO to mu opioid receptor | 1999 | Bioorganic & medicinal chemistry letters, Dec-20, Volume: 9, Issue:24 | Delta opioid binding selectivity of 3-ether analogs of naltrindole. |
| AID270152 | Antagonist activity at human cloned mu opioid receptor expressed in CHO cells assessed as inhibition of DAMGO-stimulated [35S]GTP-gamma-S binding in presence of 10 uM GDP | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18 | Highly potent and selective phenylmorphan-based inverse agonists of the opioid delta receptor. |
| AID77783 | Tested for antagonist potency against kappa receptor using ethylketazocine ligand in guinea pig ileal longitudinal muscle at 100 nM concentration | 1994 | Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5 | Synthesis of naltrexone-derived delta-opioid antagonists. Role of conformation of the delta address moiety. |
| AID149023 | Selectivity for mu to delta opioid receptors was determined | 1992 | Journal of medicinal chemistry, Nov-13, Volume: 35, Issue:23 | Opioid agonist and antagonist activities of morphindoles related to naltrindole. |
| AID148011 | Binding affinity towards recombinant human Opioid receptor kappa 1 transfected in to CHO cells for the displacement of [3H]U-69593 | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2 | 4'-Arylpyrrolomorphinans: effect of a pyrrolo-N-benzyl substituent in enhancing delta-opioid antagonist activity. |
| AID151615 | Binding affinity to mu opioid receptor was measured using [3H]DAMGO | 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. |
| AID149207 | Opioid receptor delta antagonistic activity was measured by the displacement of DADLE in the mouse vas deferens at a concentration of 20 nM | 1990 | Journal of medicinal chemistry, Jun, Volume: 33, Issue:6 | Design of peptidomimetic delta opioid receptor antagonists using the message-address concept. |
| AID147978 | Binding affinity was measured by the displacement of [3H]- EK in guinea pig brain membrane of opioid receptor kappa | 1990 | Journal of medicinal chemistry, Jun, Volume: 33, Issue:6 | Design of peptidomimetic delta opioid receptor antagonists using the message-address concept. |
| AID150007 | Antagonism towards Opioid receptor mu 1 relative to PL-017 in guinea pig ileum (GPI) smooth muscle contraction assays; d = agonist effect was observed | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone]. |
| AID152068 | Displacement of [3H]DAMGO from Opioid receptor mu 1 | 2001 | Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21 | Derivatives of 17-(2-methylallyl)-substituted noroxymorphone: variation of the delta address and its effects on affinity and selectivity for the delta opioid receptor. |
| AID148808 | Antagonist potency measured as Ke = [antagonist]/(IC50 ratio-1) against delta opioid receptor from mouse vas deferens (MVD) using DPDPE | 1999 | Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18 | Synthesis, opioid receptor binding, and biological activities of naltrexone-derived pyrido- and pyrimidomorphinans. |
| AID148944 | Ratio of antagonistic activity against delta receptors in mouse vas deferens in presence and absence of delta agonist DADLE | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Novel deltorphin heptapeptide analogs with potent delta agonist, delta antagonist, or mixed mu antagonist/delta agonist properties. |
| AID365605 | Binding affinity to guinea pig kappa opioid receptor | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Structure-antitussive activity relationships of naltrindole derivatives. Identification of novel and potent antitussive agents. |
| AID1861726 | Binding affinity to MOR (unknown origin) assessed as inhibition constant by radioligand binding assay | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Design, synthesis and biological evaluation of novel aminopropylcarboxamide derivatives as sigma ligands. |
| AID149133 | Displacement of [3H]U-69593 from Opioid receptor kappa 1 of guinea pig brain membranes (pretreated with BIT and FIT to block mu and delta sites) | 1998 | Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15 | Synthesis, opioid receptor binding, and bioassay of naltrindole analogues substituted in the indolic benzene moiety. |
| AID134203 | Compound was tested for opioid agonist activity in the electrically stimulated mouse vas deferens(MVD) | 1998 | Journal of medicinal chemistry, Jul-30, Volume: 41, Issue:16 | Synthesis of 7-arylmorphinans. Probing the "address" requirements for selectivity at opioid delta receptors. |
| AID149367 | Evaluation for the ability of delta opioid to protect the [3H]-DAMGO binding site from alkylation | 1994 | Journal of medicinal chemistry, May-27, Volume: 37, Issue:11 | 14 alpha,14' beta-[Dithiobis[(2-oxo-2,1-ethanediyl)imino]]bis (7,8-dihydromorphinone) and 14 alpha,14' beta-[dithiobis[(2-oxo-2,1- ethanediyl)imino]]bis[7,8-dihydro-N-(cyclopropylmethyl)normorphinone]: chemistry and opioid binding properties. |
| AID148183 | The opioid receptor affinity(Ki) was evaluated by competition with [3H]DAMGO (mu) on guinea pig brain membranes | 1995 | Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3 | 7'-Substituted amino acid conjugates of naltrindole. Hydrophilic groups as determinants of selective antagonism of delta 1 opioid receptor-mediated antinociception in mice. |
| 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. |
| AID296739 | Antagonist activity at human delta 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 |
| AID450028 | Activity at NOP expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding relative to basal level | 2009 | Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18 | Synthesis and pharmacological evaluation of 6-naltrexamine analogs for alcohol cessation. |
| AID270154 | Antagonist activity at human cloned kappa opioid receptor expressed in CHO cells assessed as inhibition of U69593-stimulated [35S]GTPgammaS binding in presence of 10 uM GDP | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18 | Highly potent and selective phenylmorphan-based inverse agonists of the opioid delta receptor. |
| AID151605 | Displacement of [3H]DAMGO from Opioid receptor mu 1 of rat brain membranes | 1998 | Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15 | Synthesis, opioid receptor binding, and bioassay of naltrindole analogues substituted in the indolic benzene moiety. |
| AID150982 | Binding affinity towards recombinant human Opioid receptor mu 1 transfected in to CHO cells for the displacement of [3H]DAMGO (mu) | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2 | 4'-Arylpyrrolomorphinans: effect of a pyrrolo-N-benzyl substituent in enhancing delta-opioid antagonist activity. |
| AID1162885 | Displacement of [3H]DADLE from delta opioid receptor (unknown origin) expressed in HEK293T cells after 1.5 hrs by radioligand binding assay | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | Michael acceptor approach to the design of new salvinorin A-based high affinity ligands for the kappa-opioid receptor. |
| AID148702 | IC50 ratio was measured on ethylketazocine (Opioid receptor kappa 1) in the guinea pig ileal longitudinal muscle(GPI) preparation | 1995 | Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3 | 7'-Substituted amino acid conjugates of naltrindole. Hydrophilic groups as determinants of selective antagonism of delta 1 opioid receptor-mediated antinociception in mice. |
| AID148742 | Tested for binding activity against kappa opioid receptor using [3H]U-69593 ligand | 1994 | Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5 | Synthesis of naltrexone-derived delta-opioid antagonists. Role of conformation of the delta address moiety. |
| AID148999 | Opioid receptor mu antagonistic activity was measured by the displacement of morphine in the guinea pig ileum at a concentration of 200 nM | 1990 | Journal of medicinal chemistry, Jun, Volume: 33, Issue:6 | Design of peptidomimetic delta opioid receptor antagonists using the message-address concept. |
| AID1668234 | Displacement of [3H]DAMGO from human mu opioid receptor expressed in CHO cells | 2020 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 30, Issue:12 | Discovery of δ opioid receptor full agonists lacking a basic nitrogen atom and their antidepressant-like effects. |
| AID56440 | Ability to inhibit binding of SNC80 to delta opioid receptor | 1999 | Bioorganic & medicinal chemistry letters, Dec-20, Volume: 9, Issue:24 | Delta opioid binding selectivity of 3-ether analogs of naltrindole. |
| AID150011 | Antagonistic activity against Opioid receptor mu 1 receptor using morphine in guinea pig ileum preparation | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2 | Application of the message-address concept in the design of highly potent and selective non-peptide delta opioid receptor antagonists. |
| AID226612 | Selectivity ratio was measured between mu and delta opioid 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. |
| AID282132 | Activity at human recombinant kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay | 2004 | Journal of medicinal chemistry, Dec-16, Volume: 47, Issue:26 | Effects of substitution on the pyrrole N atom in derivatives of tetrahydronaltrindole, tetrahydrooxymorphindole, and a related 4,5-epoxyphenylpyrrolomorphinan. |
| AID233288 | Selectivity ratio is IC50 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. |
| AID282130 | Activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay | 2004 | Journal of medicinal chemistry, Dec-16, Volume: 47, Issue:26 | Effects of substitution on the pyrrole N atom in derivatives of tetrahydronaltrindole, tetrahydrooxymorphindole, and a related 4,5-epoxyphenylpyrrolomorphinan. |
| AID149573 | Antagonist potency was determined using ethylketazocine at kappa-opioid receptor in electrically stimulated guinea pig ileal longitudinal muscle (GPI); IC50 ratio | 1994 | Journal of medicinal chemistry, Jun-10, Volume: 37, Issue:12 | N-benzylnaltrindoles as long-acting delta-opioid receptor antagonists. |
| AID365582 | Antitussive activity in po dosed Sprague-Dawley rat assessed as reduction in number of capsaicin-induced coughs | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Structure-antitussive activity relationships of naltrindole derivatives. Identification of novel and potent antitussive agents. |
| AID147839 | Selectivity for kappa to delta opioid receptors was determined | 1992 | Journal of medicinal chemistry, Nov-13, Volume: 35, Issue:23 | Opioid agonist and antagonist activities of morphindoles related to naltrindole. |
| AID147965 | Opioid receptor kappa antagonistic activity was measured by the displacement of ethylketazocine in the guinea pig ileum at a concentration of 200 nM | 1990 | Journal of medicinal chemistry, Jun, Volume: 33, Issue:6 | Design of peptidomimetic delta opioid receptor antagonists using the message-address concept. |
| AID149659 | Binding affinity at opioid receptor delta 1 by displacement of [3H]DADLE in rat brain membrane | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone]. |
| AID231117 | Ratio of binding affinities of mu and delta opioid receptors | 1999 | Bioorganic & medicinal chemistry letters, Dec-20, Volume: 9, Issue:24 | Delta opioid binding selectivity of 3-ether analogs of naltrindole. |
| AID149123 | Binding affinity against kappa-opioid receptor in guinea pig brain membranes | 1994 | Journal of medicinal chemistry, Jun-10, Volume: 37, Issue:12 | Synthesis and delta-opioid receptor antagonist activity of a naltrindole analogue with a regioisomeric indole moiety. |
| AID235355 | Selectivity ratio (Ki value towards mu receptor compared to that of delta receptor). | 2002 | Journal of medicinal chemistry, Nov-21, Volume: 45, Issue:24 | Synthesis and biological evaluation of 14-alkoxymorphinans. 17. Highly delta opioid receptor selective 14-alkoxy-substituted indolo- and benzofuromorphinans. |
| AID148586 | 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. |
| AID148955 | The antagonist potencies mediated through sigma opioid receptors were expressed as Ke values calculated on DADLE(delta) in the mouse vas deferens(MVD) preparation | 1995 | Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3 | 7'-Substituted amino acid conjugates of naltrindole. Hydrophilic groups as determinants of selective antagonism of delta 1 opioid receptor-mediated antinociception in mice. |
| AID149614 | Agonistic activity for guinea pig caudate opioid receptor delta 1 in [35S]GTP-gamma-S, binding assay; g = not active as an agonist | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone]. |
| AID149641 | Ability to displace [3H]DADLE radioligand from Opioid receptor delta 1 | 1999 | Journal of medicinal chemistry, May-06, Volume: 42, Issue:9 | delta Opioid affinity and selectivity of 4-hydroxy-3-methoxyindolomorphinan analogues related to naltrindole. |
| AID226792 | Selectivity ratio was measured between kappa and delta opioid 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. |
| AID1237282 | Inverse agonist activity at human DOR expressed in CHO cell membranes by [35S]GTPgammaS binding assay | 2015 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15 | Naltrindole derivatives with fluorinated ethyl substituents on the 17-nitrogen as δ opioid receptor inverse agonists. |
| 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. |
| AID148317 | Binding affinity against Opioid receptor kappa 1 using [3H]-U-69,593 as radioligand | 1997 | Journal of medicinal chemistry, Sep-26, Volume: 40, Issue:20 | Discovery of a novel class of substituted pyrrolooctahydroisoquinolines as potent and selective delta opioid agonists, based on an extension of the message-address concept. |
| AID233684 | Selectivity ratio of the affinity for kappa and delta opioid receptors (Ki mu/Ki delta) | 1997 | Journal of medicinal chemistry, Sep-26, Volume: 40, Issue:20 | Discovery of a novel class of substituted pyrrolooctahydroisoquinolines as potent and selective delta opioid agonists, based on an extension of the message-address concept. |
| AID636092 | Displacement of [3H]DADLE from delta opioid receptor in rat cerebrum membranes | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2 | Synthesis of quinolinomorphinan-4-ol derivatives as δ opioid receptor agonists. |
| AID227054 | Competitive inhibition of Morphine on Guinea pig ileal longitudinal muscle for the opioid receptor mu at 200 nM | 1991 | Journal of medicinal chemistry, May, Volume: 34, Issue:5 | Role of spacer and address components in peptidomimetic delta opioid receptor antagonists related to naltrindole. |
| AID78084 | Partial agonist activity expressed as inhibition of contraction of guinea pig ileal longitudinal muscle myenteric plexus (GPI) at 1 uM conc. | 1998 | Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15 | Synthesis, opioid receptor binding, and bioassay of naltrindole analogues substituted in the indolic benzene moiety. |
| AID756069 | Selectivity ratio of Ki for mu opioid receptor (unknown origin) to Ki for delta opioid receptor (unknown origin) | 2013 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13 | Opioid receptor selectivity profile change via isosterism for 14-O-substituted naltrexone derivatives. |
| AID235328 | Selectivity ratio of kappa opioid receptor to delta opioid receptor | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2 | Application of the message-address concept in the design of highly potent and selective non-peptide delta opioid receptor antagonists. |
| AID148953 | Tested for antagonist potency against delta opioid receptor using DADLE ligand in mouse vas deferens at 100 nM concentration | 1994 | Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5 | Synthesis of naltrexone-derived delta-opioid antagonists. Role of conformation of the delta address moiety. |
| AID270160 | Inverse agonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTP-gamma-S binding in presence of 1 uM GDP | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18 | Highly potent and selective phenylmorphan-based inverse agonists of the opioid delta receptor. |
| AID624620 | Specific activity of expressed human recombinant UGT2B7H | 2000 | Annual review of pharmacology and toxicology, , Volume: 40 | Human UDP-glucuronosyltransferases: metabolism, expression, and disease. |
| AID148102 | The compound was evaluated for binding affinity against the opioid receptor kappa in guinea pig brain membranes using [3H]- U-69,593 | 1992 | Journal of medicinal chemistry, Nov-13, Volume: 35, Issue:23 | Opioid agonist and antagonist activities of morphindoles related to naltrindole. |
| AID424033 | Displacement of [3H]DAMGO from mu opioid receptor in rat cerebellum membrane | 2009 | Bioorganic & medicinal chemistry letters, May-15, Volume: 19, Issue:10 | Design and synthesis of novel delta opioid receptor agonists and their pharmacologies. |
| AID148584 | Displacement of [3H]diprenorphine from k-E297A-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. |
| 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. |
| AID224591 | Tested for binding affinity against mu opioid receptor fby displacing [3H]- DAMGO radioligand from rat brain membrane preparations | 1993 | Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21 | TIPP[psi]: a highly potent and stable pseudopeptide delta opioid receptor antagonist with extraordinary delta selectivity. |
| AID138352 | Inhibition of contraction (agonistic activity) of mouse vas deferens (MVD) at 1 uM concentration. | 1999 | Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18 | Synthesis, opioid receptor binding, and biological activities of naltrexone-derived pyrido- and pyrimidomorphinans. |
| AID233432 | Selectivity ratio is the ratio between delta and kappa receptor | 1994 | Journal of medicinal chemistry, Jun-10, Volume: 37, Issue:12 | N-benzylnaltrindoles as long-acting delta-opioid receptor antagonists. |
| AID235724 | Relative affinity for mu and delta receptors in rat brain membranes | 1998 | Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15 | Synthesis, opioid receptor binding, and bioassay of naltrindole analogues substituted in the indolic benzene moiety. |
| AID1237279 | Displacement of [3H]U-69,593 from human KOR expressed in CHO cells | 2015 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15 | Naltrindole derivatives with fluorinated ethyl substituents on the 17-nitrogen as δ opioid receptor inverse agonists. |
| AID109741 | Intracerebroventricular dose required to produce an equivalnet antagonism of DPDPE-induced antinociception. | 1995 | Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3 | 7'-Substituted amino acid conjugates of naltrindole. Hydrophilic groups as determinants of selective antagonism of delta 1 opioid receptor-mediated antinociception in mice. |
| AID147983 | Compound was evaluated for the binding affinity to opioid receptor kappa using [3H]-EK as radioligand in guinea pig brain membrane | 1991 | Journal of medicinal chemistry, May, Volume: 34, Issue:5 | Role of spacer and address components in peptidomimetic delta opioid receptor antagonists related to naltrindole. |
| AID227056 | Competitive inhibition of the DADLE on mouse vas deferens for the opioid receptor delta at 20 nM | 1991 | Journal of medicinal chemistry, May, Volume: 34, Issue:5 | Role of spacer and address components in peptidomimetic delta opioid receptor antagonists related to naltrindole. |
| AID365595 | Selectivity for delta opioid receptor over kappa opioid receptor in Hartley guinea pig brain membrane | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Structure-antitussive activity relationships of naltrindole derivatives. Identification of novel and potent antitussive agents. |
| AID235331 | Selectivity ratio of mu opioid receptor to delta opioid receptor | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2 | Application of the message-address concept in the design of highly potent and selective non-peptide delta opioid receptor antagonists. |
| AID148814 | Displacement of DPDPE from Opioid receptor delta 1 of mouse vas deferens (MVD)smooth muscle | 1998 | Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15 | Synthesis, opioid receptor binding, and bioassay of naltrindole analogues substituted in the indolic benzene moiety. |
| 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. |
| AID151151 | Binding affinity against Opioid receptor mu 1 using [3H][D-Ala2, MePhe4, Gly-ol5]-enkephalin as radioligand | 1997 | Journal of medicinal chemistry, Sep-26, Volume: 40, Issue:20 | Discovery of a novel class of substituted pyrrolooctahydroisoquinolines as potent and selective delta opioid agonists, based on an extension of the message-address concept. |
| AID141650 | Ability to displace [3H]DAMGO from mu opioid receptor | 1999 | Bioorganic & medicinal chemistry letters, Dec-20, Volume: 9, Issue:24 | Delta opioid binding selectivity of 3-ether analogs of naltrindole. |
| AID689651 | Selectivity ratio of Ki for kappa opioid receptor in guinea pig cerebellum to Ki for delta opioid receptor in mouse whole brain without cerebellum | 2012 | Bioorganic & medicinal chemistry, Oct-01, Volume: 20, Issue:19 | Synthesis of quinolinomorphinan derivatives as highly selective δ opioid receptor ligands. |
| AID148219 | The antagonistic activity tested in [35S]GTP-gamma-S, Recombinant Human Opioid receptor delta 1 transfected in to CHO cells for the displacement of [3H]Cl-DPDPE (delta) | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2 | 4'-Arylpyrrolomorphinans: effect of a pyrrolo-N-benzyl substituent in enhancing delta-opioid antagonist activity. |
| AID151588 | Ability to displace [3H]DAMGO radioligand from Opioid receptor mu 1 | 1999 | Journal of medicinal chemistry, May-06, Volume: 42, Issue:9 | delta Opioid affinity and selectivity of 4-hydroxy-3-methoxyindolomorphinan analogues related to naltrindole. |
| AID270157 | Agonist activity at delta opioid receptor at 31.6 uM | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18 | Highly potent and selective phenylmorphan-based inverse agonists of the opioid delta receptor. |
| AID149124 | Binding affinity at Opioid receptor kappa 1 by displacement of [3H]U-69593 in guinea pig brain membranes | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone]. |
| AID1629752 | Antagonist activity at mouse delta opioid receptor-1 expressed in CHO cell membranes assessed as inhibition of DPDPE-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. |
| 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. |
| AID150851 | Binding affinity determined against Opioid receptor mu 1 from human cloned receptor | 2003 | Journal of medicinal chemistry, Aug-28, Volume: 46, Issue:18 | Synthesis, biological evaluation, and receptor docking simulations of 2-[(acylamino)ethyl]-1,4-benzodiazepines as kappa-opioid receptor agonists endowed with antinociceptive and antiamnesic activity. |
| AID364674 | Antitussive activity in ip dosed Sprague-Dawley rat assessed as reduction of capsaicin-induced coughing for 3 mins administered 30 mins before capsaicin challenge relative to control | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | Design and synthesis of a metabolically stable and potent antitussive agent, a novel delta opioid receptor antagonist, TRK-851. |
| AID233878 | Selectivity ratio was determined from Ke value of Opioid receptor mu 1 and Opioid receptor delta 1 | 1990 | Journal of medicinal chemistry, Jun, Volume: 33, Issue:6 | Design of peptidomimetic delta opioid receptor antagonists using the message-address concept. |
| AID56439 | Ability to displace [3H]DADL from delta opioid receptor | 1999 | Bioorganic & medicinal chemistry letters, Dec-20, Volume: 9, Issue:24 | Delta opioid binding selectivity of 3-ether analogs of naltrindole. |
| AID747128 | Displacement of [3H]DADLE from delta opioid receptor (unknown origin) | 2013 | Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10 | Kappa-opioid receptor-selective dicarboxylic ester-derived salvinorin A ligands. |
| 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. |
| 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. |
| 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. |
| AID365593 | Displacement of [3H]DAMGO from kappa opioid receptor in Hartley guinea pig brain membrane | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Structure-antitussive activity relationships of naltrindole derivatives. Identification of novel and potent antitussive agents. |
| AID148253 | Evaluation for the ability of delta opioid to protect the [3H]DAMGO binding site from alkylation | 1994 | Journal of medicinal chemistry, May-27, Volume: 37, Issue:11 | 14 alpha,14' beta-[Dithiobis[(2-oxo-2,1-ethanediyl)imino]]bis (7,8-dihydromorphinone) and 14 alpha,14' beta-[dithiobis[(2-oxo-2,1- ethanediyl)imino]]bis[7,8-dihydro-N-(cyclopropylmethyl)normorphinone]: chemistry and opioid binding properties. |
| AID149550 | Binding affinity for Opioid receptor kappa 1 was determined by inhibition of binding of [3H]U-69593 (1.2-2.2 nM) to guinea pig brain membranes | 1999 | Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18 | Synthesis, opioid receptor binding, and biological activities of naltrexone-derived pyrido- and pyrimidomorphinans. |
| AID1861728 | Binding affinity to KOR (unknown origin) assessed as inhibition constant by radioligand binding assay | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Design, synthesis and biological evaluation of novel aminopropylcarboxamide derivatives as sigma ligands. |
| AID224713 | Tested for binding activity against mu opioid receptor using [3H]DAMGO ligand | 1994 | Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5 | Synthesis of naltrexone-derived delta-opioid antagonists. Role of conformation of the delta address moiety. |
| AID149223 | Agonist activity by the maximum response towards opioid receptor delta 1 induced contractions in mouse vas deferens (MVD) smooth muscle contraction assays | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone]. |
| AID148830 | Activity against Opioid receptor kappa 1 on electrically stimulated guinea pig ileum using ethylketazocine as the standard agonist. | 1997 | Journal of medicinal chemistry, Jun-20, Volume: 40, Issue:13 | Pyrrolomorphinans as delta opioid receptor antagonists. The role of steric hindrance in conferring selectivity. |
| AID95216 | Compound was tested for its ability to displace [3H]U-69593 from kappa receptor in guinea pig brain. | 1998 | Bioorganic & medicinal chemistry letters, Apr-07, Volume: 8, Issue:7 | Synthesis and biological activity of 3-substituted 3-desoxynaltrindole derivatives. |
| AID286281 | Displacement of [3H]U-69593 from kappa opioid receptor in guinea pig brain membranes | 2007 | Journal of medicinal chemistry, May-03, Volume: 50, Issue:9 | Indium-labeled macrocyclic conjugates of naltrindole: high-affinity radioligands for in vivo studies of peripheral delta opioid receptors. |
| AID282134 | Activity at human recombinant delta opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay | 2004 | Journal of medicinal chemistry, Dec-16, Volume: 47, Issue:26 | Effects of substitution on the pyrrole N atom in derivatives of tetrahydronaltrindole, tetrahydrooxymorphindole, and a related 4,5-epoxyphenylpyrrolomorphinan. |
| AID232963 | Ke selectivity ratio (mu/delta) of the compound | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6 | An approach to the design of receptor-type-selective non-peptide antagonists of peptidergic receptors: delta opioid antagonists. |
| AID747129 | Displacement of [3H]DAMGO from mu opioid receptor (unknown origin) | 2013 | Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10 | Kappa-opioid receptor-selective dicarboxylic ester-derived salvinorin A ligands. |
| AID149020 | The compound was evaluated for binding affinity against opioid receptor mu in guinea pig brain membranes using [3H]- DAMGO as ligand | 1992 | Journal of medicinal chemistry, Nov-13, Volume: 35, Issue:23 | Opioid agonist and antagonist activities of morphindoles related to naltrindole. |
| AID149475 | Opioid antagonist potency against PL-107 mu-opioid receptor from guinea pig ileum(GPI). | 1999 | Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18 | Synthesis, opioid receptor binding, and biological activities of naltrexone-derived pyrido- and pyrimidomorphinans. |
| AID2954 | Selectivity ratio of binding affinity towards mu to delta receptors of rat brain membranes | 1999 | Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18 | Synthesis, opioid receptor binding, and biological activities of naltrexone-derived pyrido- and pyrimidomorphinans. |
| 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. |
| AID239942 | Binding affinity against Opioid receptor mu 1 from rat brain membranes using [3H]DAMGO | 2005 | Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5 | 3D-QSAR comparative molecular field analysis on opioid receptor antagonists: pooling data from different studies. |
| AID148577 | Compound was evaluated for its ability to displace [3H]U-69593 in CHO cells expressing the cloned Opioid receptor kappa 1 | 2000 | Bioorganic & medicinal chemistry letters, Nov-06, Volume: 10, Issue:21 | N-Cyclohexylethyl-N-noroxymorphindole: a mu-opioid preferring analogue of naltrindole. |
| AID417159 | Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding relative to basal level | 2009 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8 | Syntheses of novel high affinity ligands for opioid receptors. |
| AID429161 | Displacement of [3H]p-Cl-DPDPE from rat delta opioid receptor expressed in rat C6 cells | 2009 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16 | Synthesis and opioid receptor activity of indolopropellanes. |
| AID149833 | Tested for the ratio of the binding affinities of Opioid receptor kappa 1/Opioid receptor delta 1 | 2001 | Bioorganic & medicinal chemistry letters, Apr-09, Volume: 11, Issue:7 | Selective delta-opioid receptor ligands: potential PET ligands based on naltrindole. |
| AID148850 | Displacement of [125I]OXY from Opioid receptor kappa 2b of guinea pig brain membranes (pretreated with BIT(mu) and FIT(delta) and in the presence of (-)U50,488) | 1998 | Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15 | Synthesis, opioid receptor binding, and bioassay of naltrindole analogues substituted in the indolic benzene moiety. |
| AID149005 | Antagonistic potency at opioid receptor mu (200 nM) (Ke =IC50 in the presence of antagonist divided by the control IC50 value) | 1991 | Journal of medicinal chemistry, May, Volume: 34, Issue:5 | Role of spacer and address components in peptidomimetic delta opioid receptor antagonists related to naltrindole. |
| AID751724 | Displacement of [3H]Naltrindole from human recombinant delta opioid receptor expressed in HEK293 cells at 10 uM after 60 mins relative to control | 2013 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6 | Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells. |
| 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. |
| AID149907 | Binding affinity was measured by the displacement of [3H]- DADLE in guinea pig brain membrane of Opioid receptor delta 1 | 1990 | Journal of medicinal chemistry, Jun, Volume: 33, Issue:6 | Design of peptidomimetic delta opioid receptor antagonists using the message-address concept. |
| AID233662 | Selectivity ratio of agonist stimulated [35S]GTP-gamma-S, binding in cloned human kappa-opioid receptor versus delta-opioid receptor | 2004 | Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2 | Discovery of the first N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphan to possess highly potent and selective opioid delta receptor antagonist activity. |
| 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. |
| AID689650 | Selectivity ratio of Ki for mu opioid receptor in mouse whole brain without cerebellum to Ki for delta opioid receptor in mouse whole brain without cerebellum | 2012 | Bioorganic & medicinal chemistry, Oct-01, Volume: 20, Issue:19 | Synthesis of quinolinomorphinan derivatives as highly selective δ opioid receptor ligands. |
| AID226812 | 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. |
| AID149720 | Agonistic activity towards Opioid receptor mu 1 was determined in [35S]GTP-gamma-S, binding assay in guinea pig caudate; g = not active as an agonist | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone]. |
| AID365603 | Binding affinity to guinea pig delta opioid receptor | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Structure-antitussive activity relationships of naltrindole derivatives. Identification of novel and potent antitussive agents. |
| AID233444 | Selectivity ratio measured as the kappa Ki to that of delta Ki values. | 1997 | Journal of medicinal chemistry, Jun-20, Volume: 40, Issue:13 | Pyrrolomorphinans as delta opioid receptor antagonists. The role of steric hindrance in conferring selectivity. |
| AID151909 | Binding affinity for Opioid receptor mu 1 was determined by inhibition of binding of [3H]DAMGO (1.4-3 nM) to rat brain membranes | 1999 | Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18 | Synthesis, opioid receptor binding, and biological activities of naltrexone-derived pyrido- and pyrimidomorphinans. |
| AID151601 | Binding affinity at Opioid receptor mu 1 by displacement of [3H]DAMGO in rat brain membrane | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone]. |
| AID227051 | Competitive inhibition of Ethylketazocine on Guinea pig ileal longitudinal muscle for the opioid receptor kappa at 200 nM | 1991 | Journal of medicinal chemistry, May, Volume: 34, Issue:5 | Role of spacer and address components in peptidomimetic delta opioid receptor antagonists related to naltrindole. |
| AID636097 | Selectivity ratio of Ki for mu opioid receptor in rat cerebrum membranes to Ki for delta opioid receptor in rat cerebrum membranes | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2 | Synthesis of quinolinomorphinan-4-ol derivatives as δ opioid receptor agonists. |
| AID231521 | Ratio of binding affinity to mu receptor to that of delta receptor | 2000 | Bioorganic & medicinal chemistry letters, Nov-06, Volume: 10, Issue:21 | N-Cyclohexylethyl-N-noroxymorphindole: a mu-opioid preferring analogue of naltrindole. |
| 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. |
| AID228131 | Ratio of kappa/delta-opioid receptors Binding affinity | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 | Opioid binding and in vitro profiles of a series of 4-hdroxy-3-methoxyindolomorphinans. Transformation of a delta-selective ligand into a high affinity kappa-selective ligand by introduction of a 5,14-substituted bridge. |
| AID149553 | The opioid receptor affinity(Ki) was evaluated by competition with 9 (Opioid receptor kappa 1) on guinea pig brain membranes | 1995 | Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3 | 7'-Substituted amino acid conjugates of naltrindole. Hydrophilic groups as determinants of selective antagonism of delta 1 opioid receptor-mediated antinociception in mice. |
| 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. |
| AID147986 | The antagonistic activity of compound was tested in [35S]GTP-gamma-S, Recombinant Human Opioid receptor kappa 1 transfected in to CHO cells for the displacement of [3H]U-69593 | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2 | 4'-Arylpyrrolomorphinans: effect of a pyrrolo-N-benzyl substituent in enhancing delta-opioid antagonist activity. |
| 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. |
| AID149664 | Displacement of [3H]DADLE from morphine-insensitive Opioid receptor delta 1 (presence of 50 nM morphine) of rat brain membranes | 1998 | Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15 | Synthesis, opioid receptor binding, and bioassay of naltrindole analogues substituted in the indolic benzene moiety. |
| AID689648 | Displacement of [3H]DPDPE from delta opioid receptor in mouse whole brain without cerebellum | 2012 | Bioorganic & medicinal chemistry, Oct-01, Volume: 20, Issue:19 | Synthesis of quinolinomorphinan derivatives as highly selective δ opioid receptor ligands. |
| AID233443 | Selectivity ratio measured as the delta IC50 to that of mu IC50 values. | 1997 | Journal of medicinal chemistry, Jun-20, Volume: 40, Issue:13 | Pyrrolomorphinans as delta opioid receptor antagonists. The role of steric hindrance in conferring selectivity. |
| AID148117 | Selectivity ratio is IC50 value of opioid receptor kappa to that of delta-opioid receptor | 1991 | Journal of medicinal chemistry, May, Volume: 34, Issue:5 | Role of spacer and address components in peptidomimetic delta opioid receptor antagonists related to naltrindole. |
| AID149073 | Binding affinity against Opioid receptor delta 1 receptor binding in ICR mouse brain membranes using the radioligand [3H]naltrindole | 1997 | Journal of medicinal chemistry, Jun-20, Volume: 40, Issue:13 | Pyrrolomorphinans as delta opioid receptor antagonists. The role of steric hindrance in conferring selectivity. |
| AID234754 | Selectivity as the ratio of Ki value towards kappa receptor to that of delta 1 receptor. | 1995 | Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3 | 7'-Substituted amino acid conjugates of naltrindole. Hydrophilic groups as determinants of selective antagonism of delta 1 opioid receptor-mediated antinociception in mice. |
| AID149880 | IC50 ratio was measured on Morphine(mu) in the guinea pig ileal longitudinal muscle(GPI) preparation | 1995 | Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3 | 7'-Substituted amino acid conjugates of naltrindole. Hydrophilic groups as determinants of selective antagonism of delta 1 opioid receptor-mediated antinociception in mice. |
| AID415718 | Selectivity ratio of Ki for kappa opioid receptor to Ki for delta opioid receptor | 2009 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6 | 14-O-Heterocyclic-substituted naltrexone derivatives as non-peptide mu opioid receptor selective antagonists: design, synthesis, and biological studies. |
| AID149549 | The ability of compound to inhibit [35S]GTP-delta-S binding in guinea pig caudate stimulated by U69,593 (Opioid receptor kappa 1) antagonist | 2002 | Journal of medicinal chemistry, Nov-21, Volume: 45, Issue:24 | Synthesis and biological evaluation of 14-alkoxymorphinans. 17. Highly delta opioid receptor selective 14-alkoxy-substituted indolo- and benzofuromorphinans. |
| AID149764 | Ability to inhibit GTP-gamma-S binding to Opioid receptor delta 1 of guinea pig caudate. | 1999 | Journal of medicinal chemistry, May-06, Volume: 42, Issue:9 | delta Opioid affinity and selectivity of 4-hydroxy-3-methoxyindolomorphinan analogues related to naltrindole. |
| AID148518 | Antagonist activity against delta-opioid receptor in mouse vas deferens in the presence of DADLE | 1994 | Journal of medicinal chemistry, Jun-10, Volume: 37, Issue:12 | Synthesis and delta-opioid receptor antagonist activity of a naltrindole analogue with a regioisomeric indole moiety. |
| AID1861723 | Binding affinity to sigma 1 receptor (unknown origin) assessed as inhibition constant by radioligand binding assay | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Design, synthesis and biological evaluation of novel aminopropylcarboxamide derivatives as sigma ligands. |
| AID1633377 | Antagonist activity at human delta opioid receptor expressed in CHO cells assessed as reduction in SNC80-induced inhibition of forskolin stimulated cAMP accumulation preincubated for 15 mins followed SNC80 and forskolin addition and measured after 10 mins | 2019 | ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4 | Novel Cyclic Biphalin Analogues by Ruthenium-Catalyzed Ring Closing Metathesis: |
| AID231404 | Antagonist activity against the delta1 opioid receptor using DPDPE as agonist at 0.4 nmol/kg (icv) was determined as ratio of ED50 of antagonist to the control (ED50 of control = 8.6 (6.5-11.1) nmol/kg) | 1995 | Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3 | 7'-Substituted amino acid conjugates of naltrindole. Hydrophilic groups as determinants of selective antagonism of delta 1 opioid receptor-mediated antinociception in mice. |
| AID149640 | Tested for antagonistic activity against delta opioid receptor from mouse vas deferens, using [Leu5]- enkephalin as agonist | 1993 | Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21 | TIPP[psi]: a highly potent and stable pseudopeptide delta opioid receptor antagonist with extraordinary delta selectivity. |
| AID149855 | Inhibitory activity against Opioid receptor mu 1 in an in vitro guinea pig ileum assay; '-' indicates inactive | 1997 | Journal of medicinal chemistry, Sep-12, Volume: 40, Issue:19 | Evolution of the Dmt-Tic pharmacophore: N-terminal methylated derivatives with extraordinary delta opioid antagonist activity. |
| AID226818 | Selectivity ratio for mu and delta opioid receptor binding | 2001 | Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21 | Derivatives of 17-(2-methylallyl)-substituted noroxymorphone: variation of the delta address and its effects on affinity and selectivity for the delta opioid receptor. |
| AID395147 | Ratio of Ki for delta opioid receptor in rat brain membrane to Ki for mu opioid receptor in rat brain membrane | 2008 | European journal of medicinal chemistry, Nov, Volume: 43, Issue:11 | Ligand binding to nucleic acids and proteins: Does selectivity increase with strength? |
| AID286284 | Lipophilicity, log D at pH7.4 | 2007 | Journal of medicinal chemistry, May-03, Volume: 50, Issue:9 | Indium-labeled macrocyclic conjugates of naltrindole: high-affinity radioligands for in vivo studies of peripheral delta opioid receptors. |
| AID56444 | Compound was tested for its ability to displace [3H]DADLE from delta receptor in rat brain. | 1998 | Bioorganic & medicinal chemistry letters, Apr-07, Volume: 8, Issue:7 | Synthesis and biological activity of 3-substituted 3-desoxynaltrindole derivatives. |
| AID429154 | Displacement of [3H]U50488 from human kappa opioid receptor expressed in CHO cells | 2009 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16 | Synthesis and opioid receptor activity of indolopropellanes. |
| AID552815 | Displacement of [3H]DADLE from delta opioid receptor expressed in HEK293 cells relative to DADLE | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1 | Synthesis and biological evaluation of new salvinorin A analogues incorporating natural amino acids. |
| AID148977 | Ability to displace [3H]U-69593 radioligand from Opioid receptor kappa 1 | 1999 | Journal of medicinal chemistry, May-06, Volume: 42, Issue:9 | delta Opioid affinity and selectivity of 4-hydroxy-3-methoxyindolomorphinan analogues related to naltrindole. |
| AID150029 | Compound was evaluated for antagonist potency in guinea pig ileum preparation using morphine (Opioid receptor mu 1) | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6 | An approach to the design of receptor-type-selective non-peptide antagonists of peptidergic receptors: delta opioid antagonists. |
| AID149105 | Displacement of DPDPE from Opioid receptor delta 1 of mouse vas deferens (MVD) smooth muscle | 1998 | Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15 | Synthesis, opioid receptor binding, and bioassay of naltrindole analogues substituted in the indolic benzene moiety. |
| AID148836 | Antagonistic activity against Opioid receptor kappa 1 using ethylketazocine in guinea pig ileum preparation | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2 | Application of the message-address concept in the design of highly potent and selective non-peptide delta opioid receptor antagonists. |
| AID149108 | Apparent binding affinity of compound was determined by antagonism towards Opioid receptor kappa 1 in [35S]GTP-gamma-S, binding assay in guinea pig caudate | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone]. |
| AID286279 | Displacement of [3H]NTI from delta opioid receptor in CD1 mouse brain membranes | 2007 | Journal of medicinal chemistry, May-03, Volume: 50, Issue:9 | Indium-labeled macrocyclic conjugates of naltrindole: high-affinity radioligands for in vivo studies of peripheral delta opioid receptors. |
| AID148780 | Antagonistic activity expressed as IC50 ratio against DADLE-Opioid receptor delta 1 in smooth muscle preparations | 1998 | Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14 | 14-Desoxy analogues of naltrindole and 7-spiroindanyloxymorphone: the role of the 14-hydroxy group at delta opioid receptors. |
| AID148962 | Compound was tested for opioid antagonist activity in the electrically stimulated GPI preparation, against Opioid receptor kappa 1 | 1998 | Journal of medicinal chemistry, Jul-30, Volume: 41, Issue:16 | Synthesis of 7-arylmorphinans. Probing the "address" requirements for selectivity at opioid delta receptors. |
| 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. |
| AID229373 | Ratio of iv dose to that of icv. | 1995 | Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3 | 7'-Substituted amino acid conjugates of naltrindole. Hydrophilic groups as determinants of selective antagonism of delta 1 opioid receptor-mediated antinociception in mice. |
| AID235719 | Selectivity Ratio of Ki of Kappa receptor/ Ki of Delta receptor | 1999 | Journal of medicinal chemistry, May-06, Volume: 42, Issue:9 | delta Opioid affinity and selectivity of 4-hydroxy-3-methoxyindolomorphinan analogues related to naltrindole. |
| AID79028 | Inhibition of contraction (agonistic activity) of guinea pig ileum(GPI) at 1 uM concentration. | 1999 | Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18 | Synthesis, opioid receptor binding, and biological activities of naltrexone-derived pyrido- and pyrimidomorphinans. |
| AID148961 | Compound was evaluated for antagonist potency in guinea pig ileum preparation using ethylketazocine (Opioid receptor kappa 1) | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6 | An approach to the design of receptor-type-selective non-peptide antagonists of peptidergic receptors: delta opioid antagonists. |
| AID226817 | Selectivity ratio between delta and mu opioid receptor in corresponding mouse vas-deferens and guinea-pig ileal longitudinal muscle | 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. |
| AID365596 | Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding at 1 uM relative to DPDPE | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Structure-antitussive activity relationships of naltrindole derivatives. Identification of novel and potent antitussive agents. |
| 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. |
| AID395145 | Binding affinity to delta opioid receptor in rat brain membrane | 2008 | European journal of medicinal chemistry, Nov, Volume: 43, Issue:11 | Ligand binding to nucleic acids and proteins: Does selectivity increase with strength? |
| AID73680 | Antagonism activity for the compound was determined by preincubating the muscle preparation with the test compound, ethylketazocine (EK) | 1998 | Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14 | 14-Desoxy analogues of naltrindole and 7-spiroindanyloxymorphone: the role of the 14-hydroxy group at delta opioid receptors. |
| 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. |
| AID756070 | Selectivity ratio of Ki for kappa receptor (unknown origin) to Ki for delta opioid receptor (unknown origin) | 2013 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13 | Opioid receptor selectivity profile change via isosterism for 14-O-substituted naltrexone derivatives. |
| AID1655288 | Displacement of [3H]DPDPE from DOR in rat brain membranes incubated for 45 mins by liquid scintillation counting | |||
| AID603172 | Displacement of [125I]-IBNtxA from DOR-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. |
| AID233433 | Selectivity ratio is the ratio between delta and mu receptor | 1994 | Journal of medicinal chemistry, Jun-10, Volume: 37, Issue:12 | N-benzylnaltrindoles as long-acting delta-opioid receptor antagonists. |
| AID224710 | Relative potency to that of [Leu5]- enkephalin | 1993 | Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21 | TIPP[psi]: a highly potent and stable pseudopeptide delta opioid receptor antagonist with extraordinary delta selectivity. |
| AID424035 | Displacement of [3H]U-69593 from kappa opioid receptor in guinea pig cerebellum | 2009 | Bioorganic & medicinal chemistry letters, May-15, Volume: 19, Issue:10 | Design and synthesis of novel delta opioid receptor agonists and their pharmacologies. |
| AID149103 | Antagonist potency was determined using D-Ala2, D-Leu5 enkephalin28 (DADLE) at delta-opioid receptor in mouse vas deferens (MVD); IC50 ratio | 1994 | Journal of medicinal chemistry, Jun-10, Volume: 37, Issue:12 | N-benzylnaltrindoles as long-acting delta-opioid receptor antagonists. |
| AID779515 | Selectivity ratio of Ki for guinea pig ileum MOR to Ki for mouse vas deferens DOR | 2013 | Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21 | Binding mode characterization of 6α- and 6β-N-heterocyclic substituted naltrexamine derivatives via docking in opioid receptor crystal structures and site-directed mutagenesis studies: application of the 'message-address' concept in development of mu opio |
| AID230637 | Ke (kappa/delta) ratio of the compound | 1994 | Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5 | Synthesis of naltrexone-derived delta-opioid antagonists. Role of conformation of the delta address moiety. |
| AID1237283 | Inverse agonist activity at human DOR expressed in CHO cell membranes by [35S]GTPgammaS binding assay relative to control | 2015 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15 | Naltrindole derivatives with fluorinated ethyl substituents on the 17-nitrogen as δ opioid receptor inverse agonists. |
| AID234730 | Selectivity as the ratio of IC50 value against delta receptor to that of mu receptor. | 1995 | Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3 | 7'-Substituted amino acid conjugates of naltrindole. Hydrophilic groups as determinants of selective antagonism of delta 1 opioid receptor-mediated antinociception in mice. |
| AID149279 | Binding affinity was measured by the displacement of [3H]- EK in guinea pig brain membrane of Opioid receptor kappa 1 | 1990 | Journal of medicinal chemistry, Jun, Volume: 33, Issue:6 | Design of peptidomimetic delta opioid receptor antagonists using the message-address concept. |
| AID235725 | Selectivity for mu receptor of guinea pig Ileum (GPI) and delta receptor of delta opioid receptor of mouse vas deferens (MVD) smooth muscle preparation | 1998 | Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15 | Synthesis, opioid receptor binding, and bioassay of naltrindole analogues substituted in the indolic benzene moiety. |
| 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. |
| AID234729 | Selectivity as the ratio of IC50 value against delta receptor to that of kappa receptor. | 1995 | Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3 | 7'-Substituted amino acid conjugates of naltrindole. Hydrophilic groups as determinants of selective antagonism of delta 1 opioid receptor-mediated antinociception in mice. |
| AID357092 | Antinociceptive effect in NY1DD transgenic mouse assessed as partial agonist response at 2.5 nmol 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. |
| AID148040 | Binding affinity was measured by the displacement of [3H]- DAMGO in guinea pig brain membrane of Opioid receptor mu 1 | 1990 | Journal of medicinal chemistry, Jun, Volume: 33, Issue:6 | Design of peptidomimetic delta opioid receptor antagonists using the message-address concept. |
| AID148229 | Binding affinity for human Opioid receptor delta 1 transfected into chinese hamster ovary cells by displacing [3H]CI-DPDPE radioligand | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 | Opioid binding and in vitro profiles of a series of 4-hdroxy-3-methoxyindolomorphinans. Transformation of a delta-selective ligand into a high affinity kappa-selective ligand by introduction of a 5,14-substituted bridge. |
| AID147892 | Ratio of antagonistic activity against mu receptors in guinea pig ileum in presence and absence of mu agonist dermorphin | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Novel deltorphin heptapeptide analogs with potent delta agonist, delta antagonist, or mixed mu antagonist/delta agonist properties. |
| AID148673 | Antagonist potency against delta opioid receptor in mouse vas deferens (MVD) using DPDPE | 1999 | Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18 | Synthesis, opioid receptor binding, and biological activities of naltrexone-derived pyrido- and pyrimidomorphinans. |
| AID109742 | Intravenous dose required to produce an equivalnet antagonism of DPDPE-induced antinociception. | 1995 | Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3 | 7'-Substituted amino acid conjugates of naltrindole. Hydrophilic groups as determinants of selective antagonism of delta 1 opioid receptor-mediated antinociception in mice. |
| AID417164 | Antagonist activity against human delta opioid receptor expressed in CHO cells assessed as inhibition of SNC80-stimulated [35S]GTPgammaS binding | 2009 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8 | Syntheses of novel high affinity ligands for opioid receptors. |
| AID132269 | The compound was evaluated for antinociceptive potency using abdominal stretch assay in mice. | 1992 | Journal of medicinal chemistry, Nov-13, Volume: 35, Issue:23 | Opioid agonist and antagonist activities of morphindoles related to naltrindole. |
| AID152385 | Displacement of [3H]- diprenorphine from mu-K303E-receptor expressed in HEK 293 | 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. |
| AID147998 | Binding affinity against opioid receptor kappa 1 from human cloned receptor | 2003 | Journal of medicinal chemistry, Aug-28, Volume: 46, Issue:18 | Synthesis, biological evaluation, and receptor docking simulations of 2-[(acylamino)ethyl]-1,4-benzodiazepines as kappa-opioid receptor agonists endowed with antinociceptive and antiamnesic activity. |
| AID395146 | Ratio of Ki for kappa opioid receptor in rat brain membrane to Ki for mu opioid receptor in rat brain membrane | 2008 | European journal of medicinal chemistry, Nov, Volume: 43, Issue:11 | Ligand binding to nucleic acids and proteins: Does selectivity increase with strength? |
| AID413922 | Antagonist activity at human delta opioid receptor expressed in CHO cells assessed as inhibition of SNC80-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 |
| AID365594 | Selectivity for delta opioid receptor over mu opioid receptor in Hartley guinea pig brain membrane | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Structure-antitussive activity relationships of naltrindole derivatives. Identification of novel and potent antitussive agents. |
| AID1358123 | Displacement of [3H]diprenorphine from human DOR expressed in African green monkey COS1 cell membranes at 1 uM incubated for 1 hr by scintillation counting method | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Synthesis of 7β-hydroxy-8-ketone opioid derivatives with antagonist activity at mu- and delta-opioid receptors. |
| AID138825 | Evaluation for the ability of mu opioid to protect the [3H]DAMGO binding site from alkylation | 1994 | Journal of medicinal chemistry, May-27, Volume: 37, Issue:11 | 14 alpha,14' beta-[Dithiobis[(2-oxo-2,1-ethanediyl)imino]]bis (7,8-dihydromorphinone) and 14 alpha,14' beta-[dithiobis[(2-oxo-2,1- ethanediyl)imino]]bis[7,8-dihydro-N-(cyclopropylmethyl)normorphinone]: chemistry and opioid binding properties. |
| AID751660 | Displacement of [3H]Naltrindole from human recombinant delta opioid receptor expressed in HEK293 cells after 60 mins | 2013 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6 | Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells. |
| 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. |
| AID416819 | Selectivity ratio of IC50 for human kappa opioid receptor to IC50 for human delta opioid receptor | 2009 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8 | Syntheses of novel high affinity ligands for opioid receptors. |
| AID148228 | Binding affinity determined against Opioid receptor delta 1 from human cloned receptor | 2003 | Journal of medicinal chemistry, Aug-28, Volume: 46, Issue:18 | Synthesis, biological evaluation, and receptor docking simulations of 2-[(acylamino)ethyl]-1,4-benzodiazepines as kappa-opioid receptor agonists endowed with antinociceptive and antiamnesic activity. |
| AID147891 | Ratio of antagonistic activity against mu receptors in guinea pig ileum in presence and absence of mu agonist DAGO | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Novel deltorphin heptapeptide analogs with potent delta agonist, delta antagonist, or mixed mu antagonist/delta agonist properties. |
| AID138525 | Partial agonist activity expressed as inhibition of contraction of mouse vas deferens (MVD) smooth muscle at 1 uM conc. | 1998 | Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15 | Synthesis, opioid receptor binding, and bioassay of naltrindole analogues substituted in the indolic benzene moiety. |
| AID148041 | Compound was evaluated for binding affinity at Opioid receptor mu 1 in guinea pig brain membranes | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6 | An approach to the design of receptor-type-selective non-peptide antagonists of peptidergic receptors: delta opioid antagonists. |
| AID233445 | Selectivity ratio measured as the mu Ki to that of delta Ki values. | 1997 | Journal of medicinal chemistry, Jun-20, Volume: 40, Issue:13 | Pyrrolomorphinans as delta opioid receptor antagonists. The role of steric hindrance in conferring selectivity. |
| AID232232 | Selectivity given as ratio of kappa receptor to delta receptor | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone]. |
| AID148694 | Opioid receptor kappa 1 antagonistic activity was measured by the displacement of ethylketazocine in the guinea pig ileum at a concentration of 200 nM | 1990 | Journal of medicinal chemistry, Jun, Volume: 33, Issue:6 | Design of peptidomimetic delta opioid receptor antagonists using the message-address concept. |
| AID149212 | Antagonistic potency at opioid receptor delta (20 nM) (Ke =IC50 in the presence of antagonist divided by the control IC50 value) | 1991 | Journal of medicinal chemistry, May, Volume: 34, Issue:5 | Role of spacer and address components in peptidomimetic delta opioid receptor antagonists related to naltrindole. |
| 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. |
| AID1861725 | Selectivity index, ratio of Ki for sigma 1 receptor (unknown origin) to Ki for sigma 2 receptor (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Design, synthesis and biological evaluation of novel aminopropylcarboxamide derivatives as sigma ligands. |
| AID138850 | Antagonist activity against mu-opioid receptor in guinea pig ileum in the presence of morphine | 1994 | Journal of medicinal chemistry, Jun-10, Volume: 37, Issue:12 | Synthesis and delta-opioid receptor antagonist activity of a naltrindole analogue with a regioisomeric indole moiety. |
| AID277681 | Antagonist activity against delta opioid receptor assessed as effect on deltorphin-2-induced calcium response in CHO cells by aequorin luminescence based calcium assay | 2007 | Journal of medicinal chemistry, Feb-08, Volume: 50, Issue:3 | Synthesis and characterization of potent and selective mu-opioid receptor antagonists, [Dmt(1), D-2-Nal(4)]endomorphin-1 (Antanal-1) and [Dmt(1), D-2-Nal(4)]endomorphin-2 (Antanal-2). |
| AID636093 | Displacement of [3H]U-69,593 from kappa opioid receptor in guinea pig cerebrum membranes | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2 | Synthesis of quinolinomorphinan-4-ol derivatives as δ opioid receptor agonists. |
| AID151896 | Binding affinity at mu opioid receptor 1 in rat brain membrane by [3H]DAMGO displacement. | 2002 | Journal of medicinal chemistry, Nov-21, Volume: 45, Issue:24 | Synthesis and biological evaluation of 14-alkoxymorphinans. 17. Highly delta opioid receptor selective 14-alkoxy-substituted indolo- and benzofuromorphinans. |
| AID244401 | Ratio of affinity against Opioid receptor kappa 1 to that of Opioid receptor delta 1 expressed as selectivity ratio | 2005 | Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5 | 3D-QSAR comparative molecular field analysis on opioid receptor antagonists: pooling data from different studies. |
| AID150041 | The ability of compound to inhibit [35S]GTP-delta-S binding in guinea pig caudate stimulated by SNC80 (Opioid receptor delta 1) antagonist | 2002 | Journal of medicinal chemistry, Nov-21, Volume: 45, Issue:24 | Synthesis and biological evaluation of 14-alkoxymorphinans. 17. Highly delta opioid receptor selective 14-alkoxy-substituted indolo- and benzofuromorphinans. |
| AID150043 | The compound was evaluated for binding affinity against Opioid receptor delta 1 in guinea pig brain membrane using [3H]- DPDPE as ligand | 1992 | Journal of medicinal chemistry, Nov-13, Volume: 35, Issue:23 | Opioid agonist and antagonist activities of morphindoles related to naltrindole. |
| 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. |
| AID282127 | Displacement of [3H]DAMGO from human recombinant mu opioid receptor expressed in CHO cells | 2004 | Journal of medicinal chemistry, Dec-16, Volume: 47, Issue:26 | Effects of substitution on the pyrrole N atom in derivatives of tetrahydronaltrindole, tetrahydrooxymorphindole, and a related 4,5-epoxyphenylpyrrolomorphinan. |
| AID270158 | Intrinsic activity at mu opioid receptor in presence of 1 uM GDP | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18 | Highly potent and selective phenylmorphan-based inverse agonists of the opioid delta receptor. |
| AID147820 | Tested for binding activity against delta1 opioid receptor using [3H]DPDPE ligand | 1994 | Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5 | Synthesis of naltrexone-derived delta-opioid antagonists. Role of conformation of the delta address moiety. |
| AID1861727 | Binding affinity to DOR (unknown origin) assessed as inhibition constant by radioligand binding assay | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Design, synthesis and biological evaluation of novel aminopropylcarboxamide derivatives as sigma ligands. |
| AID365581 | Antitussive activity in ip dosed Sprague-Dawley rat assessed as reduction in number of capsaicin-induced coughs | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Structure-antitussive activity relationships of naltrindole derivatives. Identification of novel and potent antitussive agents. |
| AID257161 | Displacement of endomorphin-2 from mu opioid receptor in guinea pig ileum | 2005 | Journal of medicinal chemistry, Dec-15, Volume: 48, Issue:25 | Potent Dmt-Tic pharmacophoric delta- and mu-opioid receptor antagonists. |
| AID233663 | Selectivity ratio of agonist stimulated [35S]GTP-gamma-S, binding in cloned human mu-opioid receptor versus delta-opioid receptor | 2004 | Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2 | Discovery of the first N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphan to possess highly potent and selective opioid delta receptor antagonist activity. |
| AID149472 | Antagonistic activity expressed as IC50 ratio in Opioid receptor mu 1 in electrically stimulated guinea pig ileum(GPI) | 1998 | Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14 | 14-Desoxy analogues of naltrindole and 7-spiroindanyloxymorphone: the role of the 14-hydroxy group at delta opioid receptors. |
| AID270159 | Intrinsic activity at kappa opioid receptor in presence of 1 uM GDP | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18 | Highly potent and selective phenylmorphan-based inverse agonists of the opioid delta receptor. |
| AID149086 | 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. |
| AID141500 | Tested for antagonist potency against mu opioid receptor using morphine ligand in guinea pig ileal longitudinal muscle at 100 nM concentration | 1994 | Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5 | Synthesis of naltrexone-derived delta-opioid antagonists. Role of conformation of the delta address moiety. |
| AID689649 | Displacement of [3H]U-69,593 from kappa opioid receptor in guinea pig cerebellum | 2012 | Bioorganic & medicinal chemistry, Oct-01, Volume: 20, Issue:19 | Synthesis of quinolinomorphinan derivatives as highly selective δ opioid receptor ligands. |
| AID149665 | Displacement of [3H]DADLE from morphine-sensitive Opioid receptor delta 1 (presence of 300 nM DELT-II) of rat brain membranes | 1998 | Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15 | Synthesis, opioid receptor binding, and bioassay of naltrindole analogues substituted in the indolic benzene moiety. |
| AID147935 | Binding affinity against delta-opioid receptor in guinea pig brain membranes | 1994 | Journal of medicinal chemistry, Jun-10, Volume: 37, Issue:12 | Synthesis and delta-opioid receptor antagonist activity of a naltrindole analogue with a regioisomeric indole moiety. |
| 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. |
| AID149196 | Compound was evaluated for the binding affinity to opioid receptor delta using [3H]DADLE as radioligand in guinea pig brain membrane | 1991 | Journal of medicinal chemistry, May, Volume: 34, Issue:5 | Role of spacer and address components in peptidomimetic delta opioid receptor antagonists related to naltrindole. |
| 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. |
| AID149800 | Compound was evaluated for its ability to displace [3H]p-CI-DPDPE in C6 glioma cells expressing the cloned Opioid receptor delta 1 | 2000 | Bioorganic & medicinal chemistry letters, Nov-06, Volume: 10, Issue:21 | N-Cyclohexylethyl-N-noroxymorphindole: a mu-opioid preferring analogue of naltrindole. |
| AID416813 | Displacement of [3H]DAMGO from human mu opioid receptor expressed in CHO cells after 60 mins by scintillation counting | 2009 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8 | Syntheses of novel high affinity ligands for opioid receptors. |
| AID147876 | Ability to inhibit agonist-stimulated (U69,593) [35S]GTP-gamma-S, binding, using cloned human Opioid receptor kappa 1 expressed in CHO cells | 2004 | Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2 | Discovery of the first N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphan to possess highly potent and selective opioid delta receptor antagonist activity. |
| AID148711 | Displacement of [3H]U-69593 from Opioid receptor kappa 1 | 2001 | Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21 | Derivatives of 17-(2-methylallyl)-substituted noroxymorphone: variation of the delta address and its effects on affinity and selectivity for the delta opioid receptor. |
| AID149085 | 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. |
| 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. |
| AID149666 | Displacement of [3H]DADLE from Opioid receptor delta 1 of rat brain membranes (DAMGO quenching mu receptor) | 1998 | Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15 | Synthesis, opioid receptor binding, and bioassay of naltrindole analogues substituted in the indolic benzene moiety. |
| AID148809 | Antagonist potency against delta opioid receptor was measured in mouse vas-deferens using DPDPE | 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. |
| AID149848 | Selectivity ratio of binding affinity towards kappa of guinea pig brain membrane to delta receptors of rat brain membranes | 1999 | Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18 | Synthesis, opioid receptor binding, and biological activities of naltrexone-derived pyrido- and pyrimidomorphinans. |
| AID1861724 | Binding affinity to sigma 2 receptor (unknown origin) assessed as inhibition constant by radioligand binding assay | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Design, synthesis and biological evaluation of novel aminopropylcarboxamide derivatives as sigma ligands. |
| 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 | |||
| AID286283 | Selectivity for mouse brain delta opioid receptor over guinea pig brain kappa opioid receptor | 2007 | Journal of medicinal chemistry, May-03, Volume: 50, Issue:9 | Indium-labeled macrocyclic conjugates of naltrindole: high-affinity radioligands for in vivo studies of peripheral delta opioid receptors. |
| AID148339 | Effective concentration agonistic activity towards Opioid receptor mu 1 | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 | Opioid binding and in vitro profiles of a series of 4-hdroxy-3-methoxyindolomorphinans. Transformation of a delta-selective ligand into a high affinity kappa-selective ligand by introduction of a 5,14-substituted bridge. |
| AID149921 | Binding affinity to Opioid receptor delta 1 using [3H]DPDPE as a radioligand in guinea pig | 2001 | Bioorganic & medicinal chemistry letters, Apr-09, Volume: 11, Issue:7 | Selective delta-opioid receptor ligands: potential PET ligands based on naltrindole. |
| AID150089 | Displacement of [3H]DADLE from Opioid receptor delta 1 | 2001 | Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21 | Derivatives of 17-(2-methylallyl)-substituted noroxymorphone: variation of the delta address and its effects on affinity and selectivity for the delta opioid receptor. |
| AID149473 | Antagonist potency against mu opioid receptor in guinea pig ileum (GPI) using PL-107 | 1999 | Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18 | Synthesis, opioid receptor binding, and biological activities of naltrexone-derived pyrido- and pyrimidomorphinans. |
| AID95213 | Ability to inhibit binding of U-69,593 to kappa opioid receptor | 1999 | Bioorganic & medicinal chemistry letters, Dec-20, Volume: 9, Issue:24 | Delta opioid binding selectivity of 3-ether analogs of naltrindole. |
| AID148198 | Antagonist activity against Opioid receptor mu 1 iin a guinea pig ileum assay | 1997 | Journal of medicinal chemistry, Sep-12, Volume: 40, Issue:19 | Evolution of the Dmt-Tic pharmacophore: N-terminal methylated derivatives with extraordinary delta opioid antagonist activity. |
| AID150047 | The opioid receptor affinity(Ki) was evaluated by competition with [3H]-DPDPE (delta 1) on guinea pig brain membranes | 1995 | Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3 | 7'-Substituted amino acid conjugates of naltrindole. Hydrophilic groups as determinants of selective antagonism of delta 1 opioid receptor-mediated antinociception in mice. |
| 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. |
| AID79061 | Agonistic activity in Guinea Pig Ileum | 1999 | Journal of medicinal chemistry, May-06, Volume: 42, Issue:9 | delta Opioid affinity and selectivity of 4-hydroxy-3-methoxyindolomorphinan analogues related to naltrindole. |
| AID226790 | Selectivity ratio for kappa and delta opioid receptor binding | 2001 | Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21 | Derivatives of 17-(2-methylallyl)-substituted noroxymorphone: variation of the delta address and its effects on affinity and selectivity for the delta opioid receptor. |
| AID149024 | Selectivity ratio is IC50 value of mu-opioid receptor to that of delta-opioid receptor | 1991 | Journal of medicinal chemistry, May, Volume: 34, Issue:5 | Role of spacer and address components in peptidomimetic delta opioid receptor antagonists related to naltrindole. |
| AID365606 | Selectivity for Hartley guinea pig delta opioid receptor over Hartley guinea pig mu opioid receptor | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Structure-antitussive activity relationships of naltrindole derivatives. Identification of novel and potent antitussive agents. |
| AID286282 | Selectivity for mouse brain delta opioid receptor over guinea pig brain mu opioid receptor | 2007 | Journal of medicinal chemistry, May-03, Volume: 50, Issue:9 | Indium-labeled macrocyclic conjugates of naltrindole: high-affinity radioligands for in vivo studies of peripheral delta opioid receptors. |
| AID239944 | Binding affinity against Opioid receptor delta 1 from rat brain membranes using [3H]DADLE | 2005 | Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5 | 3D-QSAR comparative molecular field analysis on opioid receptor antagonists: pooling data from different studies. |
| AID450027 | Activity at NOP expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding | 2009 | Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18 | Synthesis and pharmacological evaluation of 6-naltrexamine analogs for alcohol cessation. |
| AID148949 | Ratio of antagonistic activity against delta receptors in mouse vas deferens in presence and absence of delta agonist deltorphin | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Novel deltorphin heptapeptide analogs with potent delta agonist, delta antagonist, or mixed mu antagonist/delta agonist properties. |
| AID78077 | Agonist activity (ability to decrease the twitch height of the electrically stimulated smooth muscle) in electrically stimulated guinea pig ileum(GPI) | 1998 | Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14 | 14-Desoxy analogues of naltrindole and 7-spiroindanyloxymorphone: the role of the 14-hydroxy group at delta opioid receptors. |
| 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. |
| 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. |
| 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. |
| AID149639 | Tested for antagonistic activity against delta opioid receptor from mouse vas deferens, using [D-Ala2] Deltorphin 1 as agonist | 1993 | Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21 | TIPP[psi]: a highly potent and stable pseudopeptide delta opioid receptor antagonist with extraordinary delta selectivity. |
| AID395144 | Binding affinity to kappa opioid receptor in rat brain membrane | 2008 | European journal of medicinal chemistry, Nov, Volume: 43, Issue:11 | Ligand binding to nucleic acids and proteins: Does selectivity increase with strength? |
| AID270155 | Selectivity for human cloned delta opioid receptor over mu opioid receptor | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18 | Highly potent and selective phenylmorphan-based inverse agonists of the opioid delta receptor. |
| AID636091 | Displacement of [3H]DAMGO from mu opioid receptor in rat cerebrum membranes | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2 | Synthesis of quinolinomorphinan-4-ol derivatives as δ opioid receptor agonists. |
| AID149987 | Agonistic activity towards Opioid receptor kappa 1 | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 | Opioid binding and in vitro profiles of a series of 4-hdroxy-3-methoxyindolomorphinans. Transformation of a delta-selective ligand into a high affinity kappa-selective ligand by introduction of a 5,14-substituted bridge. |
| AID148947 | Ratio of antagonistic activity against delta receptors in mouse vas deferens in presence and absence of delta agonist DPDPE | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Novel deltorphin heptapeptide analogs with potent delta agonist, delta antagonist, or mixed mu antagonist/delta agonist properties. |
| AID233289 | Selectivity ratio is IC50 value of delta-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. |
| AID149227 | Antagonist activity against Opioid receptor delta 1 in mouse vas deferens assay | 1997 | Journal of medicinal chemistry, Sep-12, Volume: 40, Issue:19 | Evolution of the Dmt-Tic pharmacophore: N-terminal methylated derivatives with extraordinary delta opioid antagonist activity. |
| AID365607 | Selectivity for Hartley guinea pig delta opioid receptor over Hartley guinea pig kappa opioid receptor | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Structure-antitussive activity relationships of naltrindole derivatives. Identification of novel and potent antitussive agents. |
| AID148979 | Ability to inhibit GTP-gamma-S binding to Opioid receptor kappa 1 of guinea pig caudate. | 1999 | Journal of medicinal chemistry, May-06, Volume: 42, Issue:9 | delta Opioid affinity and selectivity of 4-hydroxy-3-methoxyindolomorphinan analogues related to naltrindole. |
| AID234755 | Selectivity as the ratio of Ki value towards mu receptor to that of delta 1 receptor. | 1995 | Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3 | 7'-Substituted amino acid conjugates of naltrindole. Hydrophilic groups as determinants of selective antagonism of delta 1 opioid receptor-mediated antinociception in mice. |
| AID147898 | Apparent binding affinity of compound was determined by antagonism towards Opioid receptor mu 1 in [35S]GTP-gamma-S, binding assay in guinea pig caudate | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone]. |
| 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. |
| AID429152 | Displacement of [3H]naltrindole from human delta opioid receptor expressed in CHO cells | 2009 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16 | Synthesis and opioid receptor activity of indolopropellanes. |
| AID282128 | Displacement of [3H]U-69593 from human recombinant kappa opioid receptor expressed in CHO cells | 2004 | Journal of medicinal chemistry, Dec-16, Volume: 47, Issue:26 | Effects of substitution on the pyrrole N atom in derivatives of tetrahydronaltrindole, tetrahydrooxymorphindole, and a related 4,5-epoxyphenylpyrrolomorphinan. |
| AID296544 | Displacement of [3H]diprenorphine from human recombinant delta 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. |
| AID365597 | Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding at 1 uM relative to DAMGO | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Structure-antitussive activity relationships of naltrindole derivatives. Identification of novel and potent antitussive agents. |
| AID150010 | Antagonist potency was determined as the ratio of [antagonist] to (IC50 ratio-1) for Opioid receptor mu 1 | 1990 | Journal of medicinal chemistry, Jun, Volume: 33, Issue:6 | Design of peptidomimetic delta opioid receptor antagonists using the message-address concept. |
| AID747126 | Displacement of [3H]U69593 from kappa opioid receptor (unknown origin) | 2013 | Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10 | Kappa-opioid receptor-selective dicarboxylic ester-derived salvinorin A ligands. |
| AID148051 | Binding affinity to Opioid receptor mu 1 by using [3H]DAMGO as a radioligand from guinea pig | 2001 | Bioorganic & medicinal chemistry letters, Apr-09, Volume: 11, Issue:7 | Selective delta-opioid receptor ligands: potential PET ligands based on naltrindole. |
| AID149542 | Tested for antagonistic activity against delta delta opioid receptor from mouse vas deferens, using DPDPE as agonist | 1993 | Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21 | TIPP[psi]: a highly potent and stable pseudopeptide delta opioid receptor antagonist with extraordinary delta selectivity. |
| AID424034 | Displacement of [3H]DADLE from delta opioid receptor in rat cerebellum membrane | 2009 | Bioorganic & medicinal chemistry letters, May-15, Volume: 19, Issue:10 | Design and synthesis of novel delta opioid receptor agonists and their pharmacologies. |
| AID680022 | TP_TRANSPORTER: inhibition of Deltorphin II uptake (Deltorphin II: 50 uM, Naltrindole: 1500 uM) in Xenopus laevis oocytes | 2000 | The Journal of pharmacology and experimental therapeutics, Jul, Volume: 294, Issue:1 | Organic anion-transporting polypeptides mediate transport of opioid peptides across blood-brain barrier. |
| AID233705 | Selectivity ratio was determined from Ke value of Opioid receptor kappa 1 and Opioid receptor delta 1 | 1990 | Journal of medicinal chemistry, Jun, Volume: 33, Issue:6 | Design of peptidomimetic delta opioid receptor antagonists using the message-address concept. |
| AID229268 | Ratio of IC50 in presence of antagonist to that of control IC50 value against mu opioid receptor using morphine ligand in guinea pig ileal longitudinal muscle | 1994 | Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5 | Synthesis of naltrexone-derived delta-opioid antagonists. Role of conformation of the delta address moiety. |
| AID148810 | Antagonist potency was determined as the ratio of [antagonist] to (IC50 ratio-1) for opioid receptor delta 1 | 1990 | Journal of medicinal chemistry, Jun, Volume: 33, Issue:6 | Design of peptidomimetic delta opioid receptor antagonists using the message-address concept. |
| AID244400 | Ratio of affinity against Opioid receptor mu 1 to that of Opioid receptor delta 1 expressed as selectivity ratio | 2005 | Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5 | 3D-QSAR comparative molecular field analysis on opioid receptor antagonists: pooling data from different studies. |
| AID148798 | Antagonism of delta receptor using DPDPE in mouse vas deferens (MVD) smooth muscle contraction assays | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone]. |
| AID149417 | Binding affinity to Opioid receptor kappa 1 by using [3H]U-69593 as a radioligand from guinea pig | 2001 | Bioorganic & medicinal chemistry letters, Apr-09, Volume: 11, Issue:7 | Selective delta-opioid receptor ligands: potential PET ligands based on naltrindole. |
| AID95212 | Ability to displace [3H]U-69593 from kappa opioid receptor | 1999 | Bioorganic & medicinal chemistry letters, Dec-20, Volume: 9, Issue:24 | Delta opioid binding selectivity of 3-ether analogs of naltrindole. |
| AID1162884 | Displacement of [3H]DAMGO from mu opioid receptor (unknown origin) expressed in HEK293T cells after 1.5 hrs by radioligand binding assay | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | Michael acceptor approach to the design of new salvinorin A-based high affinity ligands for the kappa-opioid receptor. |
| AID148180 | The ability of compound to inhibit [35S]GTP-delta-S binding in guinea pig caudate stimulated by DAMGO (Opioid receptor mu 1) antagonist | 2002 | Journal of medicinal chemistry, Nov-21, Volume: 45, Issue:24 | Synthesis and biological evaluation of 14-alkoxymorphinans. 17. Highly delta opioid receptor selective 14-alkoxy-substituted indolo- and benzofuromorphinans. |
| AID636098 | Selectivity ratio of Ki for kappa opioid receptor in guinea pig cerebrum membranes to Ki for delta opioid receptor in rat cerebrum membranes | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2 | Synthesis of quinolinomorphinan-4-ol derivatives as δ opioid receptor agonists. |
| AID1237277 | Displacement of [3H]DAMGO from human MOR expressed in CHO cells | 2015 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15 | Naltrindole derivatives with fluorinated ethyl substituents on the 17-nitrogen as δ opioid receptor inverse agonists. |
| AID150831 | Ability to inhibit agonist-stimulated (DAMGO) [35S]GTP-gamma-S, binding, using cloned human Opioid receptor mu 1 expressed in CHO cells | 2004 | Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2 | Discovery of the first N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphan to possess highly potent and selective opioid delta receptor antagonist activity. |
| AID416814 | Displacement of [3H]naltrindole from human delta opioid receptor expressed in CHO cells after 3 hrs by scintillation counting | 2009 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8 | Syntheses of novel high affinity ligands for opioid receptors. |
| AID147914 | Binding affinity of compound was determined against Opioid receptor mu 1 from native receptor in guinea pig | 2003 | Journal of medicinal chemistry, Aug-28, Volume: 46, Issue:18 | Synthesis, biological evaluation, and receptor docking simulations of 2-[(acylamino)ethyl]-1,4-benzodiazepines as kappa-opioid receptor agonists endowed with antinociceptive and antiamnesic activity. |
| 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. |
| AID365592 | Displacement of [3H]DAMGO from mu opioid receptor in Hartley guinea pig brain membrane | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Structure-antitussive activity relationships of naltrindole derivatives. Identification of novel and potent antitussive agents. |
| AID149873 | Opioid receptor mu 1 antagonistic activity was measured by the displacement of morphine in the guinea pig ileum at a concentration of 200 nM | 1990 | Journal of medicinal chemistry, Jun, Volume: 33, Issue:6 | Design of peptidomimetic delta opioid receptor antagonists using the message-address concept. |
| AID148065 | Agonistic activity towards Opioid receptor delta 1 | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 | Opioid binding and in vitro profiles of a series of 4-hdroxy-3-methoxyindolomorphinans. Transformation of a delta-selective ligand into a high affinity kappa-selective ligand by introduction of a 5,14-substituted bridge. |
| AID233442 | Selectivity ratio measured as the delta IC50 to that of kappa IC50 values. | 1997 | Journal of medicinal chemistry, Jun-20, Volume: 40, Issue:13 | Pyrrolomorphinans as delta opioid receptor antagonists. The role of steric hindrance in conferring selectivity. |
| AID235352 | Selectivity ratio (Ki value towards kappa receptor compared to that of delta receptor). | 2002 | Journal of medicinal chemistry, Nov-21, Volume: 45, Issue:24 | Synthesis and biological evaluation of 14-alkoxymorphinans. 17. Highly delta opioid receptor selective 14-alkoxy-substituted indolo- and benzofuromorphinans. |
| AID224570 | Binding affinity against mu-opioid receptor in guinea pig brain membranes | 1994 | Journal of medicinal chemistry, Jun-10, Volume: 37, Issue:12 | Synthesis and delta-opioid receptor antagonist activity of a naltrindole analogue with a regioisomeric indole moiety. |
| AID147971 | Antagonistic potency at opioid receptor kappa (200 nM) (Ke =IC50 in the presence of antagonist divided by the control IC50 value) | 1991 | Journal of medicinal chemistry, May, Volume: 34, Issue:5 | Role of spacer and address components in peptidomimetic delta opioid receptor antagonists related to naltrindole. |
| AID229269 | Ratio of IC50 in presence of antagonist to that of control IC50 value in delta opioid receptor using DADLE ligand in mouse vas deferens | 1994 | Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5 | Synthesis of naltrexone-derived delta-opioid antagonists. Role of conformation of the delta address moiety. |
| AID149026 | Selectivity ratio is Ki value of mu-opioid receptor to that of delta-opioid receptor | 1991 | Journal of medicinal chemistry, May, Volume: 34, Issue:5 | Role of spacer and address components in peptidomimetic delta opioid receptor antagonists related to naltrindole. |
| AID230638 | Ke (mu/delta) ratio of the compound | 1994 | Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5 | Synthesis of naltrexone-derived delta-opioid antagonists. Role of conformation of the delta address moiety. |
| AID282146 | Antagonism of 1'-benzyl-6,7-didehydro-3,14-dihydroxy-4,5alpha-epoxy-17-methyl-4',5',6',7'-tetrahydroindolo[2',3':6,7]morphinan-induced antinociceptive activity in mouse at 30 mg/kg, sc | 2004 | Journal of medicinal chemistry, Dec-16, Volume: 47, Issue:26 | Effects of substitution on the pyrrole N atom in derivatives of tetrahydronaltrindole, tetrahydrooxymorphindole, and a related 4,5-epoxyphenylpyrrolomorphinan. |
| 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. |
| AID141759 | Compound was tested for its ability to displace [3H]DAMGO from mu receptor in rat brain. | 1998 | Bioorganic & medicinal chemistry letters, Apr-07, Volume: 8, Issue:7 | Synthesis and biological activity of 3-substituted 3-desoxynaltrindole derivatives. |
| AID148098 | Ability to inhibit agonist-stimulated (DPDPE) [35S]GTP-gamma-S, binding, using cloned human opioid receptor delta 1 expressed in CHO cells | 2004 | Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2 | Discovery of the first N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphan to possess highly potent and selective opioid delta receptor antagonist activity. |
| AID1543759 | Displacement of [3H]DPDPE from DOR in rat brain membranes incubated for 45 mins by liquid scintillation counting | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | (2S)-N-2-methoxy-2-phenylethyl-6,7-benzomorphan compound (2S-LP2): Discovery of a biased mu/delta opioid receptor agonist. |
| AID148373 | [3H]-Cl-DPDPE competition binding assay using human cloned opioid receptor delta 1 | 2004 | Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2 | Discovery of the first N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphan to possess highly potent and selective opioid delta receptor antagonist activity. |
| AID148115 | Selectivity ratio is IC50 value of opioid receptor kappa to that of opioid receptor delta | 1991 | Journal of medicinal chemistry, May, Volume: 34, Issue:5 | Role of spacer and address components in peptidomimetic delta opioid receptor antagonists related to naltrindole. |
| 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. |
| 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. |
| AID286280 | Displacement of [3H]DAMGO from mu opioid receptor in guinea pig brain membranes | 2007 | Journal of medicinal chemistry, May-03, Volume: 50, Issue:9 | Indium-labeled macrocyclic conjugates of naltrindole: high-affinity radioligands for in vivo studies of peripheral delta opioid receptors. |
| AID148785 | IC50 ratio was measured on DADLE (delta) in the mouse vas deferens (MVD) preparation | 1995 | Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3 | 7'-Substituted amino acid conjugates of naltrindole. Hydrophilic groups as determinants of selective antagonism of delta 1 opioid receptor-mediated antinociception in mice. |
| AID1877934 | Displacement of [3H]-(2-D-Ala)[Tyrosy1-3,5-]-DELTORPHIN II from Sprague-Dawley rat brain membrane delta opioid receptor incubated for 45 mins by liquid scintillation counting analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Dual Sigma-1 receptor antagonists and hydrogen sulfide-releasing compounds for pain treatment: Design, synthesis, and pharmacological evaluation. |
| AID779516 | Selectivity ratio of Ki for guinea pig ileum KOR to Ki for mouse vas deferens DOR | 2013 | Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21 | Binding mode characterization of 6α- and 6β-N-heterocyclic substituted naltrexamine derivatives via docking in opioid receptor crystal structures and site-directed mutagenesis studies: application of the 'message-address' concept in development of mu opio |
| AID77770 | Compound was tested for opioid agonist activity in the electrically stimulated guinea pig ileal longitudinal muscle(GPI) | 1998 | Journal of medicinal chemistry, Jul-30, Volume: 41, Issue:16 | Synthesis of 7-arylmorphinans. Probing the "address" requirements for selectivity at opioid delta receptors. |
| AID149939 | Tested for binding affinity against delta opioid receptor by displacing [3H]- DSLET radioligand from rat brain membrane preparations | 1993 | Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21 | TIPP[psi]: a highly potent and stable pseudopeptide delta opioid receptor antagonist with extraordinary delta selectivity. |
| AID282129 | Displacement of [3H]Cl-DPDPE from human recombinant delta opioid receptor expressed in CHO cells | 2004 | Journal of medicinal chemistry, Dec-16, Volume: 47, Issue:26 | Effects of substitution on the pyrrole N atom in derivatives of tetrahydronaltrindole, tetrahydrooxymorphindole, and a related 4,5-epoxyphenylpyrrolomorphinan. |
| 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. |
| 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. |
| AID257158 | Displacement of deltorphin-II from delta opioid receptor in mouse vas deferens | 2005 | Journal of medicinal chemistry, Dec-15, Volume: 48, Issue:25 | Potent Dmt-Tic pharmacophoric delta- and mu-opioid receptor antagonists. |
| AID395148 | Ratio of Ki for mu opioid receptor in rat brain membrane to Ki for delta opioid receptor in rat brain membrane | 2008 | European journal of medicinal chemistry, Nov, Volume: 43, Issue:11 | Ligand binding to nucleic acids and proteins: Does selectivity increase with strength? |
| AID148546 | Agonistic activity towards Opioid receptor kappa 1 was determined in [35S]GTP-gamma-S, binding assay in guinea pig caudate; g = not active as an agonist | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone]. |
| AID149257 | Binding affinity for kappa opioid receptor was measured using [3H]U-69593 | 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. |
| AID270153 | Antagonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTP-gamma-S binding in presence of 10 uM GDP | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18 | Highly potent and selective phenylmorphan-based inverse agonists of the opioid delta receptor. |
| AID151756 | Compound was evaluated for its ability to displace [3H]DAMGO in C6 glioma cells expressing the cloned Opioid receptor mu 1 | 2000 | Bioorganic & medicinal chemistry letters, Nov-06, Volume: 10, Issue:21 | N-Cyclohexylethyl-N-noroxymorphindole: a mu-opioid preferring analogue of naltrindole. |
| AID229715 | GPI/MVD ratio is based on Ke (antilog of pA2 value of antagonistic activity of compound for delta opioid receptor) and IC50 values | 1997 | Journal of medicinal chemistry, Sep-12, Volume: 40, Issue:19 | Evolution of the Dmt-Tic pharmacophore: N-terminal methylated derivatives with extraordinary delta opioid antagonist activity. |
| AID1162887 | Inhibition of human kappa opioid receptor expressed in HEK293T cells assessed as inhibition of cAMP production after 30 mins | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | Michael acceptor approach to the design of new salvinorin A-based high affinity ligands for the kappa-opioid receptor. |
| AID270156 | Selectivity for human cloned delta opioid receptor over kappa opioid receptor | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18 | Highly potent and selective phenylmorphan-based inverse agonists of the opioid delta receptor. |
| AID624621 | Specific activity of expressed human recombinant UGT2B7Y | 2000 | Annual review of pharmacology and toxicology, , Volume: 40 | Human UDP-glucuronosyltransferases: metabolism, expression, and disease. |
| 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. |
| AID229070 | Antagonist activity against the delta1 opioid receptor using DPDPE as agonist at 12.5 umol/kg (i.v.) was determined as ratio of ED50 of antagonist to the control (ED50 of control = 8.6 (6.5-11.1) nmol/kg) | 1995 | Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3 | 7'-Substituted amino acid conjugates of naltrindole. Hydrophilic groups as determinants of selective antagonism of delta 1 opioid receptor-mediated antinociception in mice. |
| AID149944 | Binding affinity for Opioid receptor delta 1 was determined by inhibition of binding of [3H]DADLE (1.3-2.0 nM) to rat brain membranes | 1999 | Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18 | Synthesis, opioid receptor binding, and biological activities of naltrexone-derived pyrido- and pyrimidomorphinans. |
| AID365598 | Agonist activity at human kappa opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding at 1 uM relative to U69,593 | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Structure-antitussive activity relationships of naltrindole derivatives. Identification of novel and potent antitussive agents. |
| AID1668237 | Selectivity ratio for Ki for displacement of [3H]U69593 from human kappa opioid receptor expressed in CHO cells to Ki for displacement of [3H]DPDPE from human DOR expressed in CHO cells | 2020 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 30, Issue:12 | Discovery of δ opioid receptor full agonists lacking a basic nitrogen atom and their antidepressant-like effects. |
| AID365591 | Displacement of [3H]NTI from delta opioid receptor in Hartley guinea pig brain membrane | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Structure-antitussive activity relationships of naltrindole derivatives. Identification of novel and potent antitussive agents. |
| AID148930 | Compound was evaluated for antagonist potency in the mouse vas deferens preparation using [D-Ala2,D-Leu5]enkephalin (Opioid receptor delta 1) | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6 | An approach to the design of receptor-type-selective non-peptide antagonists of peptidergic receptors: delta opioid antagonists. |
| AID149074 | Binding affinity against Opioid receptor delta 1 using [3H][D-Ala2, D-Leu5]-enkephalin as radioligand | 1997 | Journal of medicinal chemistry, Sep-26, Volume: 40, Issue:20 | Discovery of a novel class of substituted pyrrolooctahydroisoquinolines as potent and selective delta opioid agonists, based on an extension of the message-address concept. |
| AID395143 | Binding affinity to mu opioid receptor in rat brain membrane | 2008 | European journal of medicinal chemistry, Nov, Volume: 43, Issue:11 | Ligand binding to nucleic acids and proteins: Does selectivity increase with strength? |
| AID1668235 | Displacement of [3H]U69593 from human kappa opioid receptor expressed in CHO cells | 2020 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 30, Issue:12 | Discovery of δ opioid receptor full agonists lacking a basic nitrogen atom and their antidepressant-like effects. |
| 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. |
| 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. |
| AID235720 | Selectivity Ratio of Ki of Mu receptor/ Ki of Delta receptor | 1999 | Journal of medicinal chemistry, May-06, Volume: 42, Issue:9 | delta Opioid affinity and selectivity of 4-hydroxy-3-methoxyindolomorphinan analogues related to naltrindole. |
| AID149910 | Compound was evaluated for binding affinity at Opioid receptor delta 1 in guinea pig brain membranes | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6 | An approach to the design of receptor-type-selective non-peptide antagonists of peptidergic receptors: delta opioid antagonists. |
| AID149766 | Apparent antagonist activity determined by measuring the ability to inhibit stimulation of [35S]GTP-gamma-S, binding to opioid receptor delta 1 in guinea pig caudate membranes | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone]. |
| AID149782 | Binding affinity of compound was determined against Opioid receptor delta 1 from a native receptor in guinea pig | 2003 | Journal of medicinal chemistry, Aug-28, Volume: 46, Issue:18 | Synthesis, biological evaluation, and receptor docking simulations of 2-[(acylamino)ethyl]-1,4-benzodiazepines as kappa-opioid receptor agonists endowed with antinociceptive and antiamnesic activity. |
| AID232233 | Selectivity given as ratio of mu receptor to delta receptor | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone]. |
| AID149544 | Binding affinity at kappa opioid receptor 1 in guinea pig brain by [3H]U-69593 displacement. | 2002 | Journal of medicinal chemistry, Nov-21, Volume: 45, Issue:24 | Synthesis and biological evaluation of 14-alkoxymorphinans. 17. Highly delta opioid receptor selective 14-alkoxy-substituted indolo- and benzofuromorphinans. |
| AID149936 | Binding affinity at delta opioid receptor 1 in rat brain membrane by [3H]DADLE displacement. | 2002 | Journal of medicinal chemistry, Nov-21, Volume: 45, Issue:24 | Synthesis and biological evaluation of 14-alkoxymorphinans. 17. Highly delta opioid receptor selective 14-alkoxy-substituted indolo- and benzofuromorphinans. |
| 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. |
| AID233685 | Selectivity ratio of the affinity for mu and delta opioid receptors (Ki mu/Ki delta) | 1997 | Journal of medicinal chemistry, Sep-26, Volume: 40, Issue:20 | Discovery of a novel class of substituted pyrrolooctahydroisoquinolines as potent and selective delta opioid agonists, based on an extension of the message-address concept. |
| AID141516 | Antagonist potency using morphine at mu-opioid receptor in electrically stimulated guinea pig ileal longitudinal muscle (GPI); IC50 ratio | 1994 | Journal of medicinal chemistry, Jun-10, Volume: 37, Issue:12 | N-benzylnaltrindoles as long-acting delta-opioid receptor antagonists. |
| AID77769 | Binding affinity of compound was measured on electrically stimulated guinea pig ileal longitudinal muscle myenteric plexus (GPI) preparation using PL017 as standard antagonist | 1998 | Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15 | Synthesis, opioid receptor binding, and bioassay of naltrindole analogues substituted in the indolic benzene moiety. |
| AID149468 | Compound was tested for antagonist activity against Opioid receptor mu 1 on electrically stimulated guinea pig ileal longitudinal muscle myenteric plexus (GPI) using PL017 as antagonist ligand. IC50 ratio = IC50(agonist)/IC50 (control) | 1998 | Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15 | Synthesis, opioid receptor binding, and bioassay of naltrindole analogues substituted in the indolic benzene moiety. |
| AID416818 | Selectivity ratio of IC50 for human mu opioid receptor to IC50 for human delta opioid receptor | 2009 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8 | Syntheses of novel high affinity ligands for opioid receptors. |
| AID150002 | Activity against mu receptor on electrically stimulated guinea pig ileum using morphine as the standard agonist (Opioid receptor mu 1) | 1997 | Journal of medicinal chemistry, Jun-20, Volume: 40, Issue:13 | Pyrrolomorphinans as delta opioid receptor antagonists. The role of steric hindrance in conferring selectivity. |
| AID424037 | Selectivity ratio of Ki for kappa opioid receptor in guinea pig cerebellum to Ki for delta opioid receptor in rat cerebellum membrane | 2009 | Bioorganic & medicinal chemistry letters, May-15, Volume: 19, Issue:10 | Design and synthesis of novel delta opioid receptor agonists and their pharmacologies. |
| 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. |
| AID148187 | Tested for the ratio of the binding affinities of Opioid receptor mu 1/Opioid receptor delta 1 | 2001 | Bioorganic & medicinal chemistry letters, Apr-09, Volume: 11, Issue:7 | Selective delta-opioid receptor ligands: potential PET ligands based on naltrindole. |
| AID1346406 | Rat delta receptor (Opioid receptors) | 1992 | Life sciences, , Volume: 50, Issue:16 | Characterization of [3H]naltrindole binding to delta opioid receptors in rat brain. |
| 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. |
| 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. |
| AID1346373 | Mouse delta receptor (Opioid receptors) | 1994 | Molecular pharmacology, Feb, Volume: 45, Issue:2 | Pharmacological characterization of the cloned kappa-, delta-, and mu-opioid receptors. |
| 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. |
| 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. |
| 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. |
| AID1346361 | Human delta receptor (Opioid receptors) | 1988 | European journal of pharmacology, Jan-27, Volume: 146, Issue:1 | Naltrindole, a highly selective and potent non-peptide delta opioid receptor antagonist. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 4 (0.51) | 18.7374 |
| 1990's | 350 (44.59) | 18.2507 |
| 2000's | 273 (34.78) | 29.6817 |
| 2010's | 143 (18.22) | 24.3611 |
| 2020's | 15 (1.91) | 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 (31.69) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 4 (0.50%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 797 (99.50%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||