epibatidine: a powerful, though toxic, pain killer produced by the poison arrow frog, Epipedobates tricolor; structure given in first source; more potent than morphine but acts at nicotine rather than opiate receptors [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 105084 |
| MeSH ID | M0220392 |
| PubMed CID | 1204 |
| CHEMBL ID | 6623 |
| CHEBI ID | 91678 |
| SCHEMBL ID | 316978 |
| MeSH ID | M0220392 |
| PubMed CID | 854023 |
| CHEMBL ID | 298826 |
| SCHEMBL ID | 2500147 |
| MeSH ID | M0220392 |
| Synonym |
|---|
| PDSP2_000458 |
| epibatidine |
| (-)-epibatidine |
| epibatidine, (+/-) |
| 2-(6-chloro-pyridin-3-yl)-7-azonia-bicyclo[2.2.1]heptane |
| ()-2-(6-chloro-pyridin-3-yl)-7-aza-bicyclo[2.2.1]heptane |
| 2-(6-chloro-pyridin-3-yl)-7-aza-bicyclo[2.2.1]heptane(epibatidine) |
| 2-(6-chloropyridin-3-yl)-7-aza-bicyclo[2.2.1]heptane |
| exo-2-(6-chloropyridin-3-yl)-7-aza-bicyclo[2.2.1]heptane |
| 2-(6-chloro-pyridin-3-yl)-5-methyl-7-aza-bicyclo[2.2.1]heptane |
| (2r,4s)-2-(6-chloro-pyridin-3-yl)-7-aza-bicyclo[2.2.1]heptane |
| (+)-2-(6-chloro-pyridin-3-yl)-7-aza-bicyclo[2.2.1]heptane |
| (-)-2-(6-chloro-pyridin-3-yl)-7-aza-bicyclo[2.2.1]heptane |
| (r)-2-(6-chloro-pyridin-3-yl)-7-methyl-7-aza-bicyclo[2.2.1]heptane |
| bdbm50049757 |
| (2r,4s)-2-(6-chloropyridin-3-yl)-7-aza-bicyclo[2.2.1]heptane |
| 2-(6-chloro-pyridin-3-yl)-7-aza-bicyclo[2.2.1]heptane (epibatidine) |
| epibatidine-(+) |
| 2-(6-chloro-pyridin-3-yl)-7-aza-bicyclo[2.2.1]heptane |
| epibatidine-(-) |
| BRD-A39268308-001-02-0 |
| BIO2_000462 |
| BIO2_000942 |
| IDI1_002217 |
| BSPBIO_001263 |
| NCGC00024730-03 |
| NCGC00024730-04 |
| KBIOSS_000603 |
| KBIO3_001065 |
| KBIO2_003171 |
| KBIO2_000603 |
| KBIOGR_000603 |
| KBIO3_001066 |
| KBIO2_005739 |
| (+/-)-epibatidine |
| NCGC00024730-02 |
| NCGC00024730-05 |
| HMS1990O05 |
| (1r,2r,4s)-epibatidine |
| CHEMBL6623 , |
| HMS1792O05 |
| HMS1362O05 |
| (2r)-2-(6-chloropyridin-3-yl)-7-aza-bicyclo[2.2.1]heptane hydrochloride |
| (r)-2-(6-chloro-pyridin-3-yl)-7-aza-bicyclo[2.2.1]heptane |
| rac-(2r)-2-(6-chloropyridin-3-yl)-7-aza-bicyclo[2.2.1]heptane |
| 2-(6-chloro-pyridin-3-yl)-7-aza-bicyclo[2.2.1]heptane(+/-) epibatidine |
| A807623 |
| FT-0643316 |
| [125i]epibatidine |
| [3h]epibatidine |
| 2-(6-chloropyridin-3-yl)-7-azabicyclo[2.2.1]heptane |
| gtpl3976 |
| gtpl3977 |
| CCG-208204 |
| SCHEMBL316978 |
| AKOS023808322 |
| 208/210 epibatidine |
| (+/-)-exo-2-(6-chloro-3-pyridinyl)-7-azabicyclo[2.2.1.]heptane |
| HMS3403O05 |
| SR-01000597620-1 |
| SR-01000597620-3 |
| sr-01000597620 |
| CHEBI:91678 |
| J-007356 |
| ()-epibatidine |
| epibatidine (+/-) |
| 3-(6-chloro-3-pyridinyl)-7-azabicyclo[2.2.1]heptane |
| Q27163500 |
| Q27077200 |
| cmi 545 |
| 7-azabicyclo[2.2.1]heptane, 2-(6-chloro-3-pyridinyl)-, (1r,2r,4s)-rel- |
| DTXSID30861409 |
| 7-azabicyclo(2.2.1)heptane, 2-(6-chloro-3-pyridinyl)-, exo- |
| 7-azabicyclo(2.2.1)heptane, 2-(6-chloro-3-pyridinyl)-, (1r,2r,4s)- |
| cmi-488 |
| cmi-477 |
| cmi-545 |
| 140111-52-0 |
| (2r)-2-(6-chloropyridin-3-yl)-7-azabicyclo[2.2.1]heptane |
| EPJ , |
| (1r,2r,4s)-2-(6-chloro-pyridin-3-yl)-7-aza-bicyclo[2.2.1]heptane |
| bdbm50143314 |
| DB07720 |
| CHEMBL298826 , |
| m6k314f1xx , |
| unii-m6k314f1xx |
| SCHEMBL2500147 |
| (1r,2r,4s)-2-(6-chloropyridin-3-yl)-7-azabicyclo[2.2.1]heptane |
| 7-azabicyclo(2.2.1)heptane, 2-(6-chloro-3-pyridinyl)-, (1r-exo)- |
| alkaloid 208/210 from dendrobates |
| epibatidine [mi] |
| (1r-exo)-2-(6-chloro-3-pyridinyl)-7-azabicyclo(2.2.1)heptane |
| DTXSID00894067 |
| 7-azabicyclo[2.2.1]heptane, 2-(6-chloro-3-pyridinyl)-, (1r,2r,4s)- |
Epibatidine is a potent but nonselective nAChR agonist.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Epibatidine is a potent but nonselective nAChR agonist. " | ( Epibatidine structure-activity relationships. Carroll, FI, 2004) | 3.21 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "The present study directly compared the antinociceptive and toxic effects of the neuronal nicotinic receptor agonist ABT-594 ((R)-5-(2-azetidinylmethoxy)-2-chloropyridine) with (-)-nicotine and (+)-epibatidine." | ( Analgesic and toxic effects of ABT-594 resemble epibatidine and nicotine in rats. Boyce, S; Hill, RG; Rupniak, NMJ; Russell, MGN; Shepheard, SL; Webb, JK, 2000) | 0.31 |
| " This study examines the hypothesis for the first time that the neonicotinoid insecticides and their imine metabolites and analogs display analgesic (antinociceptive) activity or adverse toxic effects associated with their action on binding to the alpha 4 beta 2 nicotinic acetylcholine receptor (AChR) subtype." | ( Analgesic and toxic effects of neonicotinoid insecticides in mice. Casida, JE; Cowan, A; Tomizawa, M, 2001) | 0.31 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " The nicotinic agonists were given acutely and repeatedly either alone or in combination with a dopamine uptake inhibitor, nomifensine." | ( Comparison of the effects of nicotine and epibatidine given in combination with nomifensine on rotational behaviour in rats. Ahtee, L; Janhunen, S; Tuominen, RK, 2005) | 0.33 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " Furthermore, the compounds are tertiary amines, implying some advantages in terms of bioavailability pertinent to future in vivo pharmacological studies." | ( Carbamoylcholine homologs: novel and potent agonists at neuronal nicotinic acetylcholine receptors. Bräuner-Osborne, H; Falch, E; Frølund, B; Jensen, AA; Krogsgaard-Larsen, P; Mikkelsen, I, 2003) | 0.32 |
The dose-response curve of epibatidine to increase the dopamine output in the caudate-putamen was bell-shaped and clearly differed from that in the accumbens. As anticipated, likely alpha4beta2-nAChR [125I] binding sites increased with treatment (estimated dosage for one-half maximal increase was 0.5 mg/kg)
| Excerpt | Relevance | Reference |
|---|---|---|
| " However, a significant shift in (-)-epibatidine's dose-response curve was obtained in animals that received (-)-epibatidine." | ( Tolerance to the antinociceptive effect of epibatidine after acute and chronic administration in mice. Damaj, MI; Martin, BR, 1996) | 0.29 |
| " Dose-response curves for agonist-induced ileum contraction indicate that RJR-2429 is equipotent with nicotine, having an EC30 of approximately 2 microM." | ( The heterocyclic substituted pyridine derivative (+/-)-2-(-3-pyridinyl)-1-azabicyclo[2.2.2]octane (RJR-2429): a selective ligand at nicotinic acetylcholine receptors. Bencherif, M; Bhatti, BS; Caldwell, WS; Crooks, P; Fowler, K; Lippiello, PM; Lovette, ME; Reeves, L; Schmitt, JD, 1998) | 0.3 |
| " F3 (30 nM) rapidly and reversibly blocked inward currents generated by pulse applications of nicotine, shifting the dose-response curve to the right in a parallel fashion without changing the maximum response." | ( Antagonism of nicotinic receptors of rat chromaffin cells by N,N, N-trimethyl-1-(4-trans-stilbenoxy)-2-propylammonium iodide: a patch clamp and ligand binding study. Clementi, F; Di Angelantonio, S; Gotti, C; Moretti, M; Nistri, A, 2000) | 0.31 |
| " Moreover, dose-related inhibition of brain ChE was similar between age groups, and similar reductions in both QNB and epibatidine binding were noted between the age groups after repeated dosing, even though by the end of the dosing period young animals (juveniles) were still about 3 times more sensitive than adults, based on acute lethality." | ( Comparative cholinergic neurotoxicity of oral chlorpyrifos exposures in preweanling and adult rats. Olivier, K; Pope, CN; Won, YK; Zheng, Q, 2000) | 0.31 |
| " This dosage of nicotine administered during pregnancy to same rats was shown to result in increased vertical activity in the male offspring [Tizabi Y, Russell LT, Nespor SM, Perry DC, Grunberg NE." | ( Prenatal nicotine exposure is associated with an increase in [125I]epibatidine binding in discrete cortical regions in rats. Perry, DC; Tizabi, Y, 2000) | 0.31 |
| " To test this hypothesis, we injected nicotine intraperitoneally in alpha7 mutant mice and found that the dose-response curve for nicotine-induced seizures was similar in the alpha7 +/+, alpha7 +/- and alpha7 -/- mice." | ( Absence of alpha7-containing neuronal nicotinic acetylcholine receptors does not prevent nicotine-induced seizures. Bassetto, L; Broide, R; De Biasi, M; Franceschini, D; Gotti, C; Paylor, R; Salas, R, 2002) | 0.31 |
| " In addition, nicotine in low dosage (10 microM) rescued the decreased rates of cell viability and inhibited the production of lipid peroxidation resulted from H(2)O(2) and Abeta in the cultured cells." | ( Dual effects of nicotine on oxidative stress and neuroprotection in PC12 cells. Guan, ZZ; Nordberg, A; Yu, WF, 2003) | 0.32 |
| " Similarly to what has been reported concerning nicotine, the dose-response curve of epibatidine to increase the dopamine output in the caudate-putamen was bell-shaped and clearly differed from that in the accumbens." | ( Comparison of the effects of nicotine and epibatidine on the striatal extracellular dopamine. Ahtee, L; Janhunen, S, 2004) | 0.32 |
| " The dose-response relations for Delta F agreed well with those for epibatidine-induced currents, but were shifted approximately 100-fold to the left of those for ACh-induced currents." | ( A fluorophore attached to nicotinic acetylcholine receptor beta M2 detects productive binding of agonist to the alpha delta site. Auyeung, VC; Bezanilla, F; Chanda, B; Dahan, DS; Dibas, MI; Dougherty, DA; Lester, HA; Petersson, EJ, 2004) | 0.32 |
| " An intermittent nicotine dosing regimen designed to resemble nicotine intake in a smoker was administered from GD1-20." | ( Vaccination against nicotine does not prevent nicotine-induced changes in fetal nicotinic receptor binding and c-fos mRNA expression in rats. Chen, Y; Dufek, MB; Keyler, DE; Le, C; LeSage, MG; Leslie, FM; Pentel, PR, ) | 0.13 |
| " Although Dscam is not the sole gene in the DSCR contributing to enhanced refinement in trisomy, Dscam dosage clearly regulates cell spacing and dendritic fasciculation in a specific class of retinal ganglion cells." | ( The Down syndrome critical region regulates retinogeniculate refinement. Barres, BA; Blank, M; Burgess, RW; Feller, MB; Fuerst, PG; Garner, CC; Huberman, AD; Kirkby, L; Nouri, N; Stevens, B; Warrier, D, 2011) | 0.37 |
| " In the present work we studied the in vivo effect of a classic chronic dosing schedule of MDMA in rats, alone or combined with a chronic schedule of NIC, on the density of nAChR and on serotonin reuptake transporters." | ( 3,4-Methylenedioxy-methamphetamine induces in vivo regional up-regulation of central nicotinic receptors in rats and potentiates the regulatory effects of nicotine on these receptors. Camarasa, J; Escubedo, E; Garcia-Ratés, S; Pubill, D, 2013) | 0.39 |
| " This study examined dose-response relationships for murine α6β2*-nicotinic acetylcholine receptor (nAChR) down-regulation by chronic nicotine treatment." | ( α6β2*-subtype nicotinic acetylcholine receptors are more sensitive than α4β2*-subtype receptors to regulation by chronic nicotine administration. Grady, SR; Marks, MJ; McIntosh, JM; Paley, MA; Salminen, O; Wageman, CR; Whiteaker, P, 2014) | 0.4 |
| Class | Description |
|---|---|
| alkaloid | Any of the naturally occurring, basic nitrogen compounds (mostly heterocyclic) occurring mostly in the plant kingdom, but also found in bacteria, fungi, and animals. By extension, certain neutral compounds biogenetically related to basic alkaloids are also classed as alkaloids. Amino acids, peptides, proteins, nucleotides, nucleic acids, amino sugars and antibiotics are not normally regarded as alkaloids. Compounds in which the nitrogen is exocyclic (dopamine, mescaline, serotonin, etc.) are usually classed as amines rather than alkaloids. |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Chain A, TYROSYL-DNA PHOSPHODIESTERASE | Homo sapiens (human) | Potency | 31.6228 | 0.0040 | 23.8416 | 100.0000 | AID485290 |
| aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 40.0749 | 0.0112 | 12.4002 | 100.0000 | AID1030 |
| regulator of G-protein signaling 4 | Homo sapiens (human) | Potency | 29.9349 | 0.5318 | 15.4358 | 37.6858 | AID504845 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 17.7828 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
| 15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1 | Homo sapiens (human) | Potency | 35.4813 | 0.0018 | 15.6638 | 39.8107 | AID894 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Acetylcholine receptor subunit alpha | Homo sapiens (human) | EC50 (µMol) | 0.0001 | 0.0001 | 3.3370 | 10.0000 | AID246397 |
| Acetylcholine receptor subunit alpha | Tetronarce californica (Pacific electric ray) | EC50 (µMol) | 0.2000 | 0.2000 | 0.2000 | 0.2000 | AID219638 |
| Acetylcholine receptor subunit beta | Tetronarce californica (Pacific electric ray) | EC50 (µMol) | 0.2000 | 0.2000 | 0.2000 | 0.2000 | AID219638 |
| Acetylcholine receptor subunit gamma | Tetronarce californica (Pacific electric ray) | EC50 (µMol) | 0.2000 | 0.2000 | 0.2000 | 0.2000 | AID219638 |
| Acetylcholine receptor subunit delta | Tetronarce californica (Pacific electric ray) | EC50 (µMol) | 0.2000 | 0.1000 | 0.1667 | 0.2000 | AID145357; AID219638 |
| Neuronal acetylcholine receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | EC50 (µMol) | 0.1427 | 0.0000 | 1.0116 | 10.0000 | AID1410542; AID145657; AID146157; AID146158; AID240159; AID246719; AID536867 |
| Neuronal acetylcholine receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Kd | 0.0002 | 0.0000 | 0.0001 | 0.0003 | AID146000; AID146150 |
| Acetylcholine receptor subunit gamma | Homo sapiens (human) | EC50 (µMol) | 0.0001 | 0.0001 | 0.0055 | 0.0110 | AID246397 |
| Neuronal acetylcholine receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | EC50 (µMol) | 0.0274 | 0.0140 | 2.2724 | 10.0000 | AID145657; AID146297; AID146316; AID146321; AID146477 |
| Neuronal acetylcholine receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Kd | 0.0001 | 0.0000 | 0.0001 | 0.0001 | AID146452; AID146768; AID238150 |
| Acetylcholine receptor subunit beta | Homo sapiens (human) | EC50 (µMol) | 0.0001 | 0.0001 | 0.0055 | 0.0110 | AID246397 |
| Neuronal acetylcholine receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | EC50 (µMol) | 0.1000 | 0.1000 | 2.1040 | 10.0000 | AID145657 |
| Neuronal acetylcholine receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Kd | 0.0000 | 0.0000 | 0.0001 | 0.0001 | AID145858; AID145986 |
| Neuronal acetylcholine receptor subunit beta-2 | Rattus norvegicus (Norway rat) | EC50 (µMol) | 0.0274 | 0.0140 | 2.3104 | 10.0000 | AID145657; AID146297; AID146316; AID146321; AID146477 |
| Neuronal acetylcholine receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Kd | 0.0000 | 0.0000 | 0.0000 | 0.0001 | AID145858; AID146000; AID146452; AID238150 |
| Neuronal acetylcholine receptor subunit beta-3 | Rattus norvegicus (Norway rat) | EC50 (µMol) | 0.1000 | 0.0460 | 1.7610 | 10.0000 | AID145657 |
| Neuronal acetylcholine receptor subunit beta-4 | Rattus norvegicus (Norway rat) | EC50 (µMol) | 0.1427 | 0.0000 | 1.0101 | 10.0000 | AID1410542; AID145657; AID146157; AID146158; AID240159; AID246719; AID536867 |
| Neuronal acetylcholine receptor subunit beta-4 | Rattus norvegicus (Norway rat) | Kd | 0.0002 | 0.0001 | 0.0001 | 0.0003 | AID145986; AID146150; AID146768 |
| Neuronal acetylcholine receptor subunit beta-2 | Homo sapiens (human) | EC50 (µMol) | 0.0356 | 0.0000 | 1.5172 | 9.4000 | AID1410544; AID146297; AID246575; AID291934; AID302773; AID417951; AID675880 |
| Neuronal acetylcholine receptor subunit beta-2 | Homo sapiens (human) | Kd | 0.0000 | 0.0000 | 0.0000 | 0.0000 | AID238148 |
| Neuronal acetylcholine receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | EC50 (µMol) | 0.1000 | 0.1000 | 2.1040 | 10.0000 | AID145657 |
| Adenosine receptor A2a | Rattus norvegicus (Norway rat) | EC50 (µMol) | 0.0000 | 0.0000 | 0.1156 | 0.7200 | AID246575 |
| Neuronal acetylcholine receptor subunit beta-4 | Homo sapiens (human) | EC50 (µMol) | 0.0172 | 0.0070 | 3.4540 | 10.0000 | AID145356; AID146165; AID282345; AID302774; AID417953 |
| Neuronal acetylcholine receptor subunit beta-4 | Homo sapiens (human) | Kd | 0.0003 | 0.0003 | 0.0003 | 0.0003 | AID238149 |
| Neuronal acetylcholine receptor subunit alpha-3 | Homo sapiens (human) | EC50 (µMol) | 0.0158 | 0.0070 | 2.2587 | 9.4000 | AID145356; AID146165; AID225721; AID282345; AID302774; AID417953 |
| Neuronal acetylcholine receptor subunit alpha-3 | Homo sapiens (human) | Kd | 0.0002 | 0.0000 | 0.0002 | 0.0003 | AID238148; AID238149 |
| Neuronal acetylcholine receptor subunit alpha-7 | Homo sapiens (human) | EC50 (µMol) | 3.5000 | 0.1280 | 2.8018 | 8.9000 | AID146779 |
| Neuronal acetylcholine receptor subunit alpha-7 | Homo sapiens (human) | Kd | 0.0037 | 0.0011 | 0.0404 | 0.1580 | AID238082; AID689290 |
| Neuronal acetylcholine receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | EC50 (µMol) | 0.1000 | 0.0460 | 1.7610 | 10.0000 | AID145657 |
| Neuronal acetylcholine receptor subunit alpha-9 | Rattus norvegicus (Norway rat) | EC50 (µMol) | 0.1000 | 0.1000 | 2.1040 | 10.0000 | AID145657 |
| Neuronal acetylcholine receptor subunit alpha-4 | Homo sapiens (human) | EC50 (µMol) | 0.0356 | 0.0000 | 1.6186 | 9.4000 | AID1410544; AID146297; AID246575; AID291934; AID302773; AID417951; AID675880 |
| Neuronal acetylcholine receptor subunit alpha-7 | Rattus norvegicus (Norway rat) | EC50 (µMol) | 0.7000 | 0.0002 | 1.8481 | 10.0000 | AID145657; AID146798 |
| Acetylcholine receptor subunit delta | Homo sapiens (human) | EC50 (µMol) | 0.0001 | 0.0001 | 0.0055 | 0.0110 | AID246397 |
| Neuronal acetylcholine receptor subunit alpha-10 | Rattus norvegicus (Norway rat) | EC50 (µMol) | 0.1000 | 0.1000 | 2.1040 | 10.0000 | AID145657 |
| Transporter | Rattus norvegicus (Norway rat) | Kd | 0.0000 | 0.0000 | 0.0000 | 0.0000 | AID145858 |
| Neuronal acetylcholine receptor subunit beta-2 | Homo sapiens (human) | Kd | 0.0000 | 0.0000 | 0.0000 | 0.0000 | AID1275134 |
| Neuronal acetylcholine receptor subunit beta-4 | Homo sapiens (human) | Kd | 0.0003 | 0.0003 | 0.0003 | 0.0003 | AID1275133 |
| Neuronal acetylcholine receptor subunit alpha-3 | Homo sapiens (human) | Kd | 0.0003 | 0.0000 | 0.0002 | 0.0003 | AID1275133 |
| Neuronal acetylcholine receptor subunit alpha-4 | Homo sapiens (human) | Kd | 0.0000 | 0.0000 | 0.0000 | 0.0000 | AID1275134 |
| Acetylcholine-binding protein | Lymnaea stagnalis (great pond snail) | Kd | 0.0014 | 0.0001 | 0.5316 | 3.6308 | AID1799850 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Neuronal acetylcholine receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Affinity | 0.0005 | 0.0005 | 0.1103 | 0.2200 | AID243385 |
| Neuronal acetylcholine receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | K app | 0.0000 | 0.0000 | 0.0031 | 0.0062 | AID145677 |
| Muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | Kapp | 6.4750 | 0.0005 | 1.6511 | 6.9000 | AID1682111; AID1682112 |
| Neuronal acetylcholine receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Affinity | 0.0000 | 0.0000 | 0.0001 | 0.0001 | AID243384 |
| Neuronal acetylcholine receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | K app | 0.0000 | 0.0000 | 0.0031 | 0.0062 | AID145677 |
| Neuronal acetylcholine receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | K app | 0.0000 | 0.0000 | 0.0031 | 0.0062 | AID145677 |
| Neuronal acetylcholine receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Affinity | 0.0000 | 0.0000 | 0.0001 | 0.0001 | AID243384 |
| Neuronal acetylcholine receptor subunit beta-2 | Rattus norvegicus (Norway rat) | K app | 0.0000 | 0.0000 | 0.0031 | 0.0062 | AID145677 |
| Neuronal acetylcholine receptor subunit beta-3 | Rattus norvegicus (Norway rat) | K app | 0.0000 | 0.0000 | 0.0031 | 0.0062 | AID145677 |
| Neuronal acetylcholine receptor subunit beta-4 | Rattus norvegicus (Norway rat) | Affinity | 0.0005 | 0.0005 | 0.1103 | 0.2200 | AID243385 |
| Neuronal acetylcholine receptor subunit beta-4 | Rattus norvegicus (Norway rat) | K app | 0.0000 | 0.0000 | 0.0031 | 0.0062 | AID145677 |
| Neuronal acetylcholine receptor subunit beta-2 | Homo sapiens (human) | Activity | 0.0050 | 0.0050 | 0.0050 | 0.0050 | AID146464 |
| Neuronal acetylcholine receptor subunit beta-2 | Homo sapiens (human) | ED50 | 0.0170 | 0.0170 | 2.0085 | 4.0000 | AID1682121 |
| Neuronal acetylcholine receptor subunit beta-2 | Homo sapiens (human) | INH | 0.0001 | 0.0001 | 0.0001 | 0.0001 | AID452525 |
| Neuronal acetylcholine receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | K app | 0.0000 | 0.0000 | 0.0031 | 0.0062 | AID145677 |
| Neuronal acetylcholine receptor subunit beta-4 | Homo sapiens (human) | Activity | 0.0050 | 0.0050 | 0.0050 | 0.0050 | AID146155 |
| Neuronal acetylcholine receptor subunit beta-4 | Homo sapiens (human) | ED50 | 0.0190 | 0.0190 | 0.0190 | 0.0190 | AID1682118 |
| Neuronal acetylcholine receptor subunit beta-4 | Homo sapiens (human) | INH | 0.0003 | 0.0003 | 0.0003 | 0.0003 | AID452526 |
| Neuronal acetylcholine receptor subunit alpha-3 | Homo sapiens (human) | Activity | 0.0050 | 0.0050 | 0.0050 | 0.0050 | AID146155 |
| Neuronal acetylcholine receptor subunit alpha-3 | Homo sapiens (human) | ED50 | 0.0190 | 0.0190 | 0.0190 | 0.0190 | AID1682118 |
| Neuronal acetylcholine receptor subunit alpha-3 | Homo sapiens (human) | INH | 0.0003 | 0.0003 | 0.0003 | 0.0003 | AID452526 |
| Neuronal acetylcholine receptor subunit alpha-7 | Homo sapiens (human) | ED50 | 1.1000 | 1.1000 | 1.1000 | 1.1000 | AID1682117 |
| Neuronal acetylcholine receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | K app | 0.0000 | 0.0000 | 0.0031 | 0.0062 | AID145677 |
| Neuronal acetylcholine receptor subunit alpha-9 | Rattus norvegicus (Norway rat) | K app | 0.0000 | 0.0000 | 0.0031 | 0.0062 | AID145677 |
| Neuronal acetylcholine receptor subunit alpha-4 | Homo sapiens (human) | Activity | 0.0050 | 0.0050 | 0.0050 | 0.0050 | AID146464 |
| Neuronal acetylcholine receptor subunit alpha-4 | Homo sapiens (human) | ED50 | 0.0170 | 0.0170 | 2.0085 | 4.0000 | AID1682121 |
| Neuronal acetylcholine receptor subunit alpha-4 | Homo sapiens (human) | INH | 0.0001 | 0.0001 | 0.0001 | 0.0001 | AID452525 |
| Neuronal acetylcholine receptor subunit alpha-7 | Rattus norvegicus (Norway rat) | Activity | 0.5000 | 0.5000 | 0.5000 | 0.5000 | AID146792 |
| Neuronal acetylcholine receptor subunit alpha-7 | Rattus norvegicus (Norway rat) | K app | 0.0000 | 0.0000 | 0.0031 | 0.0062 | AID145677 |
| Neuronal acetylcholine receptor subunit alpha-10 | Rattus norvegicus (Norway rat) | K app | 0.0000 | 0.0000 | 0.0031 | 0.0062 | AID145677 |
| Transporter | Rattus norvegicus (Norway rat) | K app | 0.0000 | 0.0000 | 0.0031 | 0.0062 | AID145677 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID239324 | Inhibition of [3H]epibatidine binding to Nicotinic acetylcholine receptor alpha2-beta2 | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Novel pyridyl ring C5 substituted analogues of epibatidine and 3-(1-methyl-2(S)-pyrrolidinylmethoxy)pyridine (A-84543) as highly selective agents for neuronal nicotinic acetylcholine receptors containing beta2 subunits. |
| AID229712 | Functional / binding potency ratio for nAChR subtype alpha4-beta2 (rat brain) | 1997 | Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26 | Neuronal nicotinic acetylcholine receptors as targets for drug discovery. |
| AID238082 | Dissociation constant for nicotinic acetylcholine receptor alpha 7 from human neuroblastoma SH-SY5Y cells; n=3 | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4 | 6'-Methylpyrido[3,4-b]norhomotropane: synthesis and outstanding potency in relation to the alpha4beta2 nicotinic receptor pharmacophore model. |
| AID231911 | Ratio between the binding affinities towards rat alpha2-beta4 and alpha2-beta2 nACh receptor using [3H]-EB as radioligand | 2004 | Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8 | Pharmacology of the agonist binding sites of rat neuronal nicotinic receptor subtypes expressed in HEK 293 cells. |
| AID246575 | Change in membrane potential in K-177 cells expressing acetylcholine central neuronal receptor alpha4-beta2 subunits | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4 | Halogenated and isosteric cytisine derivatives with increased affinity and functional activity at nicotinic acetylcholine receptors. |
| AID374844 | Binding affinity to Aplysia californica AchBP A107M, M116L, Y195F mutant expressed in HEK293S cells by scintillation proximity assay | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID1101292 | Inhibition of [3H]nicotine binding to alpha3 nicotinic acetylcholine receptor in Homo sapiens (human) SH-SY5Y cells co-expressing beta2beta4alpha5 Nicotinic acetylcholine receptor subunits | 2000 | Journal of agricultural and food chemistry, Dec, Volume: 48, Issue:12 | Neonicotinoid insecticides: molecular features conferring selectivity for insect versus mammalian nicotinic receptors. |
| AID146309 | Binding affinity to alpha4 beta-2 receptor subtype from mouse fibroblast M10 cells was measured using [3 H]nicotine | 2003 | Bioorganic & medicinal chemistry letters, Feb-10, Volume: 13, Issue:3 | 5-Azidoepibatidine: an exceptionally potent photoaffinity ligand for neuronal alpha 4 beta 2 and alpha 7 nicotinic acetylcholine receptors. |
| AID14401 | Biodistribution in rat thalamus, expressed as percent I.D./g tissue | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | Synthesis and nicotinic acetylcholine receptor in vivo binding properties of 2-fluoro-3-[2(S)-2-azetidinylmethoxy]pyridine: a new positron emission tomography ligand for nicotinic receptors. |
| AID264241 | Selectivity for rat alpha-4-beta-2 nACHR over alpha3beta4 nACHR expressed in human HEK293 cells | 2006 | Journal of medicinal chemistry, May-04, Volume: 49, Issue:9 | Synthesis and pharmacological evaluation of novel 9- and 10-substituted cytisine derivatives. Nicotinic ligands of enhanced subtype selectivity. |
| AID1101298 | Inhibition of [3H]IMI binding to Drosophila melanogaster neuronal acetylcholine receptor | 2000 | Journal of agricultural and food chemistry, Dec, Volume: 48, Issue:12 | Neonicotinoid insecticides: molecular features conferring selectivity for insect versus mammalian nicotinic receptors. |
| AID145982 | Binding affinity towards rat alpha2-beta2 neuronal nAChR expressed in Xenopus oocytes using [3H]epibatidine as radioligand | 2004 | Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8 | Epibatidine structure-activity relationships. |
| AID113223 | Analgesic efficacy is expressed as percentage of that morphine, done on mouse. | 1998 | Journal of medicinal chemistry, Feb-26, Volume: 41, Issue:5 | Mono- and disubstituted-3,8-diazabicyclo[3.2.1]octane derivatives as analgesics structurally related to epibatidine: synthesis, activity, and modeling. |
| AID374879 | Binding affinity to Aplysia californica AchBP V108M, M116L, Y195F mutant expressed in HEK293S cells assessed as specific photoincorporation at 46 pmol by scintillation counting | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID1682121 | Agonist activity at human alpha4beta2 nAChR expressed in human K177 cell membrane assessed as increase in 86-rubidium efflux incubated for 5 mins by gamma counting method | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Pyridine alkaloids with activity in the central nervous system. |
| AID1682120 | Displacement of [125I]alpha-bungarotoxin from Torpedo californica electroplax alpha1beta1deltagamma nACHR incubated for 1 hr by gamma counter method | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Pyridine alkaloids with activity in the central nervous system. |
| AID239611 | Displacement of [3H]epibatidine from Alpha3 Beta4 Nicotinic acetylcholine receptor of rat brain homogenates | 2005 | Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16 | Ligand selectivity for the acetylcholine binding site of the rat alpha4beta2 and alpha3beta4 nicotinic subtypes investigated by molecular docking. |
| AID146321 | Functional potency for Nicotinic acetylcholine receptor alpha4-beta2 (rat brain) | 1997 | Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26 | Neuronal nicotinic acetylcholine receptors as targets for drug discovery. |
| AID225721 | Functional activation of human sympathetic ganglionic type nAChRs in IMR-32 cells containing alpha-3 subtype | 1998 | Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4 | Identification and initial structure-activity relationships of (R)-5-(2-azetidinylmethoxy)-2-chloropyridine (ABT-594), a potent, orally active, non-opiate analgesic agent acting via neuronal nicotinic acetylcholine receptors. |
| AID1074611 | Agonist activity at rat alpha7 nAChR expressed in Xenopus laevis oocytes assessed as stimulation of acetylcholine-induced current at 100 uM by two-electrode voltage clamp electrophysiological analysis relative to acetylcholine | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3 | Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2'-fluoro-3'-(substituted pyridinyl)-7-deschloroepibatidine analogues. |
| AID1682117 | Agonist activity at human alpha7 nAChR (unknown origin) | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Pyridine alkaloids with activity in the central nervous system. |
| AID238146 | Dissociation constant against Nicotinic acetylcholine receptor alpha2-beta2 | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Novel pyridyl ring C5 substituted analogues of epibatidine and 3-(1-methyl-2(S)-pyrrolidinylmethoxy)pyridine (A-84543) as highly selective agents for neuronal nicotinic acetylcholine receptors containing beta2 subunits. |
| AID375124 | Binding affinity to Aplysia californica AchBP I118M, M116L mutant expressed in HEK293S cells assessed as specific photoincorporation at 46 pmol by scintillation counting relative to wild type | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID341257 | Displacement of [3H]epibatidine from nAChR in rat cerebral cortex membrane | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Discovery of (-)-7-methyl-2-exo-[3'-(6-[18F]fluoropyridin-2-yl)-5'-pyridinyl]-7-azabicyclo[2.2.1]heptane, a radiolabeled antagonist for cerebral nicotinic acetylcholine receptor (alpha4beta2-nAChR) with optimal positron emission tomography imaging propert |
| AID427648 | Displacement of [3H]epibatidine from rat alpha2beta2 nicotinic receptor expressed in human HEK293 cells by liquid scintillation counting | 2009 | Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13 | Synthesis and biological evaluation of novel carbon-11 labeled pyridyl ethers: candidate ligands for in vivo imaging of alpha4beta2 nicotinic acetylcholine receptors (alpha4beta2-nAChRs) in the brain with positron emission tomography. |
| AID146631 | Functional potency measured as maximum stimulation at rat Nicotinic acetylcholine receptor alpha4-beta2 expressed in Xenopus oocytes | 2004 | Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8 | Epibatidine structure-activity relationships. |
| AID113222 | Analgesic efficacy is expressed as percentage of that epibatidine, done on mouse. | 1998 | Journal of medicinal chemistry, Feb-26, Volume: 41, Issue:5 | Mono- and disubstituted-3,8-diazabicyclo[3.2.1]octane derivatives as analgesics structurally related to epibatidine: synthesis, activity, and modeling. |
| AID1682112 | Displacement of [3H]-NMS from rat cerebral cortex muscarinic M1 receptor incubated for 60 mins by liquid scintillation spectrometry | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Pyridine alkaloids with activity in the central nervous system. |
| AID1410536 | Displacement of [3H]epibatidine from alpha7 nAChR (unknown origin) expressed in HEK cell membranes after 4 hrs by liquid scintillation counting method | 2018 | Journal of natural products, 04-27, Volume: 81, Issue:4 | Absolute Configuration and Pharmacology of the Poison Frog Alkaloid Phantasmidine. |
| AID374869 | Binding affinity to Aplysia californica AchBP M116L mutant expressed in HEK293S cells assessed as specific photoincorporation at 46 pmol by scintillation counting | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID1682115 | Displacement of [3H]-(-)-nicotine from rat cerebral cortex nAChR incubated for 60 mins by liquid scintillation spectrometry | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Pyridine alkaloids with activity in the central nervous system. |
| AID145989 | Binding affinity towards rat Nicotinic acetylcholine receptor alpha2-beta4 expressed in Xenopus oocytes using [3H]epibatidine as radioligand | 2004 | Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8 | Epibatidine structure-activity relationships. |
| AID341262 | Displacement of [3H]epibatidine from rat alpha3beta4 nAChR expressed in HEK293 cells | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Discovery of (-)-7-methyl-2-exo-[3'-(6-[18F]fluoropyridin-2-yl)-5'-pyridinyl]-7-azabicyclo[2.2.1]heptane, a radiolabeled antagonist for cerebral nicotinic acetylcholine receptor (alpha4beta2-nAChR) with optimal positron emission tomography imaging propert |
| AID488647 | Displacement of (+/-)-[3H]epibatidine from alpha4beta2 nAChR in rat cortical membrane | 2010 | Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12 | Novel tricyclic Delta(2)-isoxazoline and 3-oxo-2-methyl-isoxazolidine derivatives: synthesis and binding affinity at neuronal nicotinic acetylcholine receptor subtypes. |
| AID374882 | Binding affinity to Aplysia californica AchBP I118M, M116L mutant expressed in HEK293S cells assessed as specific photoincorporation at 46 pmol by scintillation counting | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID146630 | in vitro binding affinity by inhibiting [3H]cytisine binding in rat brain tissue at Nicotinic acetylcholine receptor alpha4-beta2 | 2002 | Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14 | Synthesis and biological evaluation at nicotinic acetylcholine receptors of N-arylalkyl- and N-aryl-7-azabicyclo[2.2.1]heptanes. |
| AID264234 | Displacement of [3H]epibatidine from rat alpha-2-beta-2 nACHR expressed in human HEK293 cells | 2006 | Journal of medicinal chemistry, May-04, Volume: 49, Issue:9 | Synthesis and pharmacological evaluation of novel 9- and 10-substituted cytisine derivatives. Nicotinic ligands of enhanced subtype selectivity. |
| AID242876 | Maximal response against Nicotinic acetylcholine receptor alpha3-beta4 | 2005 | Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15 | Neuronal nicotinic acetylcholine receptors: structural revelations, target identifications, and therapeutic inspirations. |
| AID374848 | Binding affinity to Aplysia californica AchBP V108M, M116L mutant expressed in HEK293S cells by scintillation proximity assay | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID146163 | Binding affinity towards rat Nicotinic acetylcholine receptor alpha3-beta4 expressed in Xenopus oocytes using [3H]epibatidine as radioligand | 2004 | Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8 | Epibatidine structure-activity relationships. |
| AID146484 | Binding affinity towards Nicotinic acetylcholine receptor alpha4-beta2 using [3H]epibatidine | 2004 | Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8 | Synthesis and pharmacological characterization of bivalent ligands of epibatidine at neuronal nicotinic acetylcholine receptors. |
| AID1410534 | Displacement of [3H]epibatidine from alpha3beta4 nAChR (unknown origin) expressed in HEK cell membranes after 4 hrs by liquid scintillation counting method | 2018 | Journal of natural products, 04-27, Volume: 81, Issue:4 | Absolute Configuration and Pharmacology of the Poison Frog Alkaloid Phantasmidine. |
| AID1410542 | Agonist activity at rat alpha3beta4 nAChR by cell-based rubidium flux assay | 2018 | Journal of natural products, 04-27, Volume: 81, Issue:4 | Absolute Configuration and Pharmacology of the Poison Frog Alkaloid Phantasmidine. |
| AID1359525 | Displacement of [3H]epibatidine from human alpha3beta4 nAChR expressed in HEK293 cell membranes | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Pyridinyl- and pyridazinyl-3,6-diazabicyclo[3.1.1]heptane-anilines: Novel selective ligands with subnanomolar affinity for α |
| AID146149 | Binding affinity to Nicotinic acetylcholine receptor alpha3-beta4 using +/-[3H]epibatidine as radioligand in pig adrenal gland | 2002 | Journal of medicinal chemistry, Feb-28, Volume: 45, Issue:5 | Synthesis and nicotinic binding studies on enantiopure diazine analogues of the novel (2-chloro-5-pyridyl)-9-azabicyclo[4.2.1]non-2-ene UB-165. |
| AID374881 | Binding affinity to Aplysia californica AchBP S114M, M116L, Y195F mutant expressed in HEK293S cells assessed as specific photoincorporation at 46 pmol by scintillation counting | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID1101291 | Inhibition of [3H]nicotine binding to alpha4 nicotinic acetylcholine receptor in Mus musculus (mouse) M10 cells co-expressing beta2 nicotinic acetylcholine receptor subunits | 2000 | Journal of agricultural and food chemistry, Dec, Volume: 48, Issue:12 | Neonicotinoid insecticides: molecular features conferring selectivity for insect versus mammalian nicotinic receptors. |
| AID242878 | Maximal response against Nicotinic acetylcholine receptor alpha4-beta4 | 2005 | Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15 | Neuronal nicotinic acetylcholine receptors: structural revelations, target identifications, and therapeutic inspirations. |
| AID427650 | Displacement of [3H]epibatidine from rat alpha3beta2 nicotinic receptor expressed in human HEK293 cells by liquid scintillation counting | 2009 | Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13 | Synthesis and biological evaluation of novel carbon-11 labeled pyridyl ethers: candidate ligands for in vivo imaging of alpha4beta2 nicotinic acetylcholine receptors (alpha4beta2-nAChRs) in the brain with positron emission tomography. |
| AID374856 | Binding affinity to Aplysia californica AchBP S114M, M116L, Y195F mutant expressed in HEK293S cells by scintillation proximity assay | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID240159 | Effective concentration against alpha3-beta4 nicotinic acetylcholine receptor (nAChR) expressed in IMR32 cell | 2005 | Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16 | Ligand selectivity for the acetylcholine binding site of the rat alpha4beta2 and alpha3beta4 nicotinic subtypes investigated by molecular docking. |
| AID427655 | Selectivity ratio of Ki for rat alpha3beta4 nicotinic receptor to Ki for rat alpha4beta2 nicotinic receptor | 2009 | Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13 | Synthesis and biological evaluation of novel carbon-11 labeled pyridyl ethers: candidate ligands for in vivo imaging of alpha4beta2 nicotinic acetylcholine receptors (alpha4beta2-nAChRs) in the brain with positron emission tomography. |
| AID322347 | Antinociceptive activity in sc dosed mouse assessed as inhibition of nicotin induced hypothermia | 2008 | Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2 | Synthesis, nicotinic acetylcholine receptor binding, and pharmacological properties of 3'-(substituted phenyl)deschloroepibatidine analogs. |
| AID1682113 | Displacement of [3H]-Cytisine from rat cerebral cortex nAChR at 10 uM by radioligand binding assay relative to control | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Pyridine alkaloids with activity in the central nervous system. |
| AID146775 | Binding affinity against nicotinic acetylcholine receptor alpha4-beta4 using [3H]epibatidine as radioligand expressed in HEK293 cells or tsA cells | 2004 | Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1 | Synthesis and nicotinic receptor activity of a hydroxylated tropane. |
| AID146162 | Binding affinity towards rat Nicotinic acetylcholine receptor alpha3-beta4 expressed in HEK293 cells using [3H]EB as radioligand | 2004 | Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8 | Pharmacology of the agonist binding sites of rat neuronal nicotinic receptor subtypes expressed in HEK 293 cells. |
| AID239302 | Inhibition of [3H]epibatidine binding to Nicotinic acetylcholine receptor alpha4-beta4 | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Novel pyridyl ring C5 substituted analogues of epibatidine and 3-(1-methyl-2(S)-pyrrolidinylmethoxy)pyridine (A-84543) as highly selective agents for neuronal nicotinic acetylcholine receptors containing beta2 subunits. |
| AID1682114 | Displacement of [3H]-Pirenzepine from rat cerebral cortex Muscarinic M1 receptor at 10 uM by radioligand binding assay relative to control | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Pyridine alkaloids with activity in the central nervous system. |
| AID374878 | Binding affinity to Aplysia californica AchBP V108M, M116L mutant expressed in HEK293S cells assessed as specific photoincorporation at 46 pmol by scintillation counting | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID697852 | Inhibition of electric eel AChE at 2 mg/ml by Ellman's method | 2012 | Bioorganic & medicinal chemistry, Nov-15, Volume: 20, Issue:22 | Exploration of natural compounds as sources of new bifunctional scaffolds targeting cholinesterases and beta amyloid aggregation: the case of chelerythrine. |
| AID145685 | Binding affinity towards rat forebrain nicotinic acetylcholine receptor using [3H]EB as radioligand | 2004 | Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8 | Pharmacology of the agonist binding sites of rat neuronal nicotinic receptor subtypes expressed in HEK 293 cells. |
| AID239325 | Inhibition of [3H]epibatidine binding to Nicotinic acetylcholine receptor alpha2-beta4 | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Novel pyridyl ring C5 substituted analogues of epibatidine and 3-(1-methyl-2(S)-pyrrolidinylmethoxy)pyridine (A-84543) as highly selective agents for neuronal nicotinic acetylcholine receptors containing beta2 subunits. |
| AID1682118 | Agonist activity at human alpha3beta4 nAChR expressed in mouse/rat hybrid F11 cells assessed as increase in rubidium-86 efflux | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Pyridine alkaloids with activity in the central nervous system. |
| AID145343 | Binding affinity to Drosophila nicotinic receptor was measured using [3H]imidacloprid as radioligand | 2003 | Bioorganic & medicinal chemistry letters, Feb-10, Volume: 13, Issue:3 | 5-Azidoepibatidine: an exceptionally potent photoaffinity ligand for neuronal alpha 4 beta 2 and alpha 7 nicotinic acetylcholine receptors. |
| AID94460 | Ability to stimulate Rb+ efflux from human K177 cell preparations containing human alpha4-beta2 receptors | 1996 | Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4 | Novel 3-Pyridyl ethers with subnanomolar affinity for central neuronal nicotinic acetylcholine receptors. |
| AID264236 | Displacement of [3H]epibatidine from rat alpha-3-beta-2 nACHR expressed in human HEK293 cells | 2006 | Journal of medicinal chemistry, May-04, Volume: 49, Issue:9 | Synthesis and pharmacological evaluation of novel 9- and 10-substituted cytisine derivatives. Nicotinic ligands of enhanced subtype selectivity. |
| AID1682124 | Displacement of [3H]cytisine from rat brain nAChR using radiolabelled compound | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Pyridine alkaloids with activity in the central nervous system. |
| AID318725 | Displacement of [3H]ACE from Aplysia AChBP expressed in HEK293S cells by scintillation proximity assay | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-22, Volume: 104, Issue:21 | Mapping the elusive neonicotinoid binding site. |
| AID239384 | Inhibition of [3H]epibatidine binding to rat Nicotinic acetylcholine receptor alpha4-beta2 | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Novel pyridyl ring C5 substituted analogues of epibatidine and 3-(1-methyl-2(S)-pyrrolidinylmethoxy)pyridine (A-84543) as highly selective agents for neuronal nicotinic acetylcholine receptors containing beta2 subunits. |
| AID145663 | Binding affinity towards nicotinic acetylcholine receptor using [125I]alpha-bungarotoxin as radioligand in rat forebrain homogenates | 2003 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21 | Rigidified acetylcholine mimics: conformational requirements for binding to neuronal nicotinic receptors. |
| AID145345 | Potency to displace [3H]IMI binding to Nicotinic acetylcholine receptor from Drosophila head membranes | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Structural features of azidopyridinyl neonicotinoid probes conferring high affinity and selectivity for mammalian alpha4beta2 and Drosophila nicotinic receptors. |
| AID1101295 | Inhibition of [3H]alpha-BGT binding to alpha1 nicotinic acetylcholine receptor in Homo sapiens (human) TE671 cells co-expressing gammaalpha1deltabeta1 nicotinic acetylcholine receptor subunits | 2000 | Journal of agricultural and food chemistry, Dec, Volume: 48, Issue:12 | Neonicotinoid insecticides: molecular features conferring selectivity for insect versus mammalian nicotinic receptors. |
| AID374876 | Binding affinity to Aplysia californica AchBP A107M, M116L, Y195F mutant expressed in HEK293S cells assessed as specific photoincorporation at 46 pmol by scintillation counting | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID246719 | Effective concentration in KXalpha-3-beta-4R2 cells expressing rat nicotinic acetylcholine receptor alpha3-beta4 subunits | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4 | Halogenated and isosteric cytisine derivatives with increased affinity and functional activity at nicotinic acetylcholine receptors. |
| AID145986 | Tested for binding affinity against Nicotinic acetylcholine receptor alpha2-beta4 | 2003 | Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6 | Synthesis, nicotinic acetylcholine receptor binding affinities, and molecular modeling of constrained epibatidine analogues. |
| AID145988 | Binding affinity towards Nicotinic acetylcholine receptor alpha2-beta4 using [3H]epibatidine | 2004 | Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8 | Synthesis and pharmacological characterization of bivalent ligands of epibatidine at neuronal nicotinic acetylcholine receptors. |
| AID146001 | Tested for binding affinity against Nicotinic acetylcholine receptor alpha3-beta2 | 2003 | Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6 | Synthesis, nicotinic acetylcholine receptor binding affinities, and molecular modeling of constrained epibatidine analogues. |
| AID242872 | Maximal response against Nicotinic acetylcholine receptor alpha 7 | 2005 | Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15 | Neuronal nicotinic acetylcholine receptors: structural revelations, target identifications, and therapeutic inspirations. |
| AID1410535 | Displacement of [3H]epibatidine from alpha4beta2 nAChR (unknown origin) expressed in HEK cell membranes after 4 hrs by liquid scintillation counting method | 2018 | Journal of natural products, 04-27, Volume: 81, Issue:4 | Absolute Configuration and Pharmacology of the Poison Frog Alkaloid Phantasmidine. |
| AID1410537 | Selectivity ratio of Ki for displacement of [3H]epibatidine from alpha3beta4 nAChR (unknown origin) expressed in HEK cell membranes to Ki for displacement of [3H]epibatidine from alpha4beta2 nAChR (unknown origin) expressed in HEK cell membranes | 2018 | Journal of natural products, 04-27, Volume: 81, Issue:4 | Absolute Configuration and Pharmacology of the Poison Frog Alkaloid Phantasmidine. |
| AID146314 | Affinity at alpha4-beta2 nACh receptors in rat brain (minus cerebellum) homogenates. | 2003 | Bioorganic & medicinal chemistry letters, Feb-24, Volume: 13, Issue:4 | Binding of nicotine and homoazanicotine analogues at neuronal nicotinic acetylcholinergic (nACh) receptors. |
| AID146297 | Compound was evaluated for functional potencies and efficacies at human Nicotinic acetylcholine receptor alpha4-beta2 | 1997 | Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26 | Neuronal nicotinic acetylcholine receptors as targets for drug discovery. |
| AID94458 | Cholinergic interactions was measured with FLIPR device on K177l cells and given as Intrinsic activity | 1998 | Journal of medicinal chemistry, Feb-26, Volume: 41, Issue:5 | Mono- and disubstituted-3,8-diazabicyclo[3.2.1]octane derivatives as analgesics structurally related to epibatidine: synthesis, activity, and modeling. |
| AID1682128 | Displacement of [3H] dihydromorphine from guinea pig brain opioid receptor | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Pyridine alkaloids with activity in the central nervous system. |
| AID375119 | Binding affinity to Aplysia californica AchBP V108M mutant expressed in HEK293S cells assessed as specific photoincorporation at 46 pmol by scintillation counting relative to wild type | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID397990 | Displacement of [3H]A585539 from alpha7 nicotinic acetylcholine receptor in rat brain minus cerebellum membrane | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Octahydropyrrolo[3,4-c]pyrrole: a diamine scaffold for construction of either alpha4beta2 or alpha7-selective nicotinic acetylcholine receptor (nAChR) ligands. Substitutions that switch subtype selectivity. |
| AID146779 | Compound was evaluated for functional potencies and efficacies at human Nicotinic acetylcholine receptor alpha7 | 1997 | Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26 | Neuronal nicotinic acetylcholine receptors as targets for drug discovery. |
| AID1682130 | Antinociceptive activity in naloxone treated mouse assessed as induction of Straub-tail response | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Pyridine alkaloids with activity in the central nervous system. |
| AID1410538 | Potency index, ratio of epibatidine Ki to racemic phantasmidine Ki for displacement of [3H]epibatidine from alpha3beta4 nAChR (unknown origin) expressed in HEK cell membranes | 2018 | Journal of natural products, 04-27, Volume: 81, Issue:4 | Absolute Configuration and Pharmacology of the Poison Frog Alkaloid Phantasmidine. |
| AID146167 | Binding affinity against nicotinic acetylcholine receptor alpha3-beta4 using [3H]epibatidine as radioligand expressed in HEK293 cells or tsA cells | 2004 | Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1 | Synthesis and nicotinic receptor activity of a hydroxylated tropane. |
| AID1682111 | Displacement of [3H]-oxo-M from rat cerebral cortex muscarinic M1 receptor incubated for 40 mins by liquid scintillation spectrometry | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Pyridine alkaloids with activity in the central nervous system. |
| AID246840 | Effective dose to induce hypothermia in mouse was determined | 2005 | Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4 | Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 3'-substituted deschloroepibatidine analogues. Novel nicotinic antagonists. |
| AID146316 | Compound was evaluated for functional potencies and efficacies at rat Nicotinic acetylcholine receptor alpha4-beta2 | 1997 | Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26 | Neuronal nicotinic acetylcholine receptors as targets for drug discovery. |
| AID374870 | Binding affinity to Aplysia californica AchBP Y195F mutant expressed in HEK293S cells assessed as specific photoincorporation at 46 pmol by scintillation counting | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID375121 | Binding affinity to Aplysia californica AchBP V108M, M116L, Y195F mutant expressed in HEK293S cells assessed as specific photoincorporation at 46 pmol by scintillation counting relative to wild type | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID146770 | Functional potency measured as stimulation at rat Nicotinic acetylcholine receptor alpha4-beta4 expressed in Xenopus oocytes | 2004 | Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8 | Epibatidine structure-activity relationships. |
| AID1682127 | Antinociceptive activity against mecamylamine-treated mouse | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Pyridine alkaloids with activity in the central nervous system. |
| AID374858 | Binding affinity to Aplysia californica AchBP I118M mutant expressed in HEK293S cells by scintillation proximity assay | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID146617 | Inhibition of [3H]epibatidine binding to Nicotinic acetylcholine receptor alpha4-beta2 from rat membranes | 2004 | Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8 | Epibatidine structure-activity relationships. |
| AID374880 | Binding affinity to Aplysia californica AchBP S114M, M116L mutant expressed in HEK293S cells assessed as specific photoincorporation at 46 pmol by scintillation counting | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID375117 | Binding affinity to Aplysia californica AchBP A107M, M116L mutant expressed in HEK293S cells assessed as specific photoincorporation at 46 pmol by scintillation counting relative to wild type | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID146486 | Binding affinity towards rat Nicotinic acetylcholine receptor alpha4-beta2 expressed in HEK293 cells using [3H]EB as radioligand | 2004 | Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8 | Pharmacology of the agonist binding sites of rat neuronal nicotinic receptor subtypes expressed in HEK 293 cells. |
| AID226266 | Compound was evaluated for the functional selectivity for alpha4-beta2 (rat brain)/ vs alpha-7 (rat brain) | 1997 | Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26 | Neuronal nicotinic acetylcholine receptors as targets for drug discovery. |
| AID374860 | Binding affinity to Aplysia californica AchBP I118M, M116L mutant expressed in HEK293S cells by scintillation proximity assay | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID145858 | Tested for binding affinity against Nicotinic acetylcholine receptor alpha2-beta2 | 2003 | Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6 | Synthesis, nicotinic acetylcholine receptor binding affinities, and molecular modeling of constrained epibatidine analogues. |
| AID276250 | Displacement of [3H]epibatidine from human recombinant alpha-3-beta-4 nAChR in HEK293 cells by SPA assay | 2006 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21 | Epibatidine isomers and analogues: structure-activity relationships. |
| AID147090 | Binding affinity towards nicotinic acetylcholine receptor alpha7 - 5-hydroxytryptamine 3 receptor was determined in transfected HEK cells (alpha7) using [125I]-alpha-BgTx as radioligand | 2003 | Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6 | Syntheses and biological properties of cysteine-reactive epibatidine derivatives. |
| AID208871 | Cholinergic interactions was measured with FLIPR device on TE671 cells and given as Effective dose | 1998 | Journal of medicinal chemistry, Feb-26, Volume: 41, Issue:5 | Mono- and disubstituted-3,8-diazabicyclo[3.2.1]octane derivatives as analgesics structurally related to epibatidine: synthesis, activity, and modeling. |
| AID253369 | Lethal dose against rodents; Range = 7-67 nmol/kg | 2005 | Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16 | Ligand selectivity for the acetylcholine binding site of the rat alpha4beta2 and alpha3beta4 nicotinic subtypes investigated by molecular docking. |
| AID374874 | Binding affinity to Aplysia californica AchBP A107M mutant expressed in HEK293S cells assessed as specific photoincorporation at 46 pmol by scintillation counting | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID146792 | Agonistic activity against rat nicotinic acetylcholine receptor alpha-7 expressed in Xenopus oocytes | 2001 | Journal of medicinal chemistry, Jan-04, Volume: 44, Issue:1 | exo-2-(Pyridazin-4-yl)-7-azabicyclo[2.2.1]heptanes: syntheses and nicotinic acetylcholine receptor agonist activity of potent pyridazine analogues of (+/-)-epibatidine. |
| AID264240 | Displacement of [3H]epibatidine from rat forebrain alpha4beta2 nACHR | 2006 | Journal of medicinal chemistry, May-04, Volume: 49, Issue:9 | Synthesis and pharmacological evaluation of novel 9- and 10-substituted cytisine derivatives. Nicotinic ligands of enhanced subtype selectivity. |
| AID242891 | Maximal response against Nicotinic acetylcholine receptor alpha2-beta4 expressed in HEK293 cells | 2005 | Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15 | Neuronal nicotinic acetylcholine receptors: structural revelations, target identifications, and therapeutic inspirations. |
| AID91541 | Cholinergic interactions was measured with FLIPR device on cells of IMR-32 human neuroblastoma clonal line and given as Intrinsic activity | 1998 | Journal of medicinal chemistry, Feb-26, Volume: 41, Issue:5 | Mono- and disubstituted-3,8-diazabicyclo[3.2.1]octane derivatives as analgesics structurally related to epibatidine: synthesis, activity, and modeling. |
| AID231914 | Ratio between the binding affinities towards rat alpha3-beta4 and forebrain nACh receptor using [3H]EB as radioligand | 2004 | Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8 | Pharmacology of the agonist binding sites of rat neuronal nicotinic receptor subtypes expressed in HEK 293 cells. |
| AID417954 | Agonist activity at human recombinant alpha3beta4 nAChR expressed in human IMR32 cells assessed as calcium dynamics by FLIPR assay relative to nicotine | 2009 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6 | Preparation and characterization of N-(3-pyridinyl) spirocyclic diamines as ligands for nicotinic acetylcholine receptors. |
| AID229789 | Ratio of Ki (binding affinity) relative to activation potency | 2002 | Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15 | Synthesis and pharmacological characterization of novel analogues of the nicotinic acetylcholine receptor agonist (+/-)-UB-165. |
| AID302773 | Agonist activity at recombinant human alpha-4-beta-2 nAChR expressed in HEK293 cells assessed as induction of calcium influx by FLIPR assay | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22 | Synthesis and structure-activity relationship studies of 3,6-diazabicyclo[3.2.0]heptanes as novel alpha4beta2 nicotinic acetylcholine receptor selective agonists. |
| AID375125 | Binding affinity to Aplysia californica AchBP I118M, M116L, Y195F mutant expressed in HEK293S cells assessed as specific photoincorporation at 46 pmol by scintillation counting relative to wild type | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID465077 | Agonist activity at human alpha3beta4 nAChR in human IMR32 cells assessed as membrane depolarization after 1 hr by HPLC based fluorescence assay | 2010 | Journal of natural products, Mar-26, Volume: 73, Issue:3 | Phantasmidine: an epibatidine congener from the ecuadorian poison frog Epipedobates anthonyi. |
| AID225722 | Intrinsic activity against human sympathetic ganglionic type nAChRs in IMR-32 cells containing alpha-3 subtype | 1998 | Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4 | Identification and initial structure-activity relationships of (R)-5-(2-azetidinylmethoxy)-2-chloropyridine (ABT-594), a potent, orally active, non-opiate analgesic agent acting via neuronal nicotinic acetylcholine receptors. |
| AID1092034 | Binding affinity to freshwater snail Lymnaea stagnalis AChBP assessed as [3H]EPI binding by radioligand binding assay | 2011 | Journal of agricultural and food chemistry, Apr-13, Volume: 59, Issue:7 | Unique neonicotinoid binding conformations conferring selective receptor interactions. |
| AID375120 | Binding affinity to Aplysia californica AchBP V108M, M116L mutant expressed in HEK293S cells assessed as specific photoincorporation at 46 pmol by scintillation counting relative to wild type | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID239326 | Inhibition of [3H]epibatidine binding to Nicotinic acetylcholine receptor alpha3-beta2 | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Novel pyridyl ring C5 substituted analogues of epibatidine and 3-(1-methyl-2(S)-pyrrolidinylmethoxy)pyridine (A-84543) as highly selective agents for neuronal nicotinic acetylcholine receptors containing beta2 subunits. |
| AID1074609 | Antagonist activity at rat alpha3beta4 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of acetylcholine-induced current at 100 uM by two-electrode voltage clamp electrophysiological analysis relative to acetylcholine | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3 | Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2'-fluoro-3'-(substituted pyridinyl)-7-deschloroepibatidine analogues. |
| AID225720 | Binding affinity towards rat alpha2-beta4 nACh receptor expressed in HEK293 cells using [3H]EB as radioligand | 2004 | Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8 | Pharmacology of the agonist binding sites of rat neuronal nicotinic receptor subtypes expressed in HEK 293 cells. |
| AID417951 | Agonist activity at human recombinant alpha4beta2 nAChR expressed in human IMR32 cells assessed as calcium dynamics by FLIPR assay | 2009 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6 | Preparation and characterization of N-(3-pyridinyl) spirocyclic diamines as ligands for nicotinic acetylcholine receptors. |
| AID231912 | Ratio between the binding affinities towards rat alpha3-beta4 and alpha3-beta2 nACh receptor using [3H]EB as radioligand | 2004 | Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8 | Pharmacology of the agonist binding sites of rat neuronal nicotinic receptor subtypes expressed in HEK 293 cells. |
| AID1682122 | Displacement of [3H]cytisine from human alpha4beta2 nAChR expressed in human K177 cell membrane incubated for 75 mins by liquid scintillation spectroscopy | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Pyridine alkaloids with activity in the central nervous system. |
| AID374884 | Binding affinity to Aplysia californica AchBP M116Y mutant expressed in HEK293S cells assessed as specific photoincorporation at 46 pmol by scintillation counting | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID146635 | Binding affinity at heteropentameric Nicotinic acetylcholine receptor alpha4-beta2 subtype using [3H]bungarotoxin as radioligand | 1999 | Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16 | Molecular recognition in nicotinic acetylcholine receptors: the importance of pi-cation interactions. |
| AID146935 | Binding affinity to subtype Nicotinic acetylcholine receptor alpha-7 using [125I]-alpha-BTX as radioligand in rat brain | 2002 | Journal of medicinal chemistry, Feb-28, Volume: 45, Issue:5 | Synthesis and nicotinic binding studies on enantiopure diazine analogues of the novel (2-chloro-5-pyridyl)-9-azabicyclo[4.2.1]non-2-ene UB-165. |
| AID751661 | Displacement of [I125]Epibatidine from nAChR in human IMR32 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. |
| AID141666 | In vitro displacement of [3H]oxotremorine-M from muscarinic acetylcholine receptor in rat brain cortex | 1999 | Journal of medicinal chemistry, Dec-02, Volume: 42, Issue:24 | Improving the nicotinic pharmacophore with a series of (Isoxazole)methylene-1-azacyclic compounds: synthesis, structure-activity relationship, and molecular modeling. |
| AID427652 | Displacement of [3H]epibatidine from rat alpha4beta2 nicotinic receptor expressed in human HEK293 cells by liquid scintillation counting | 2009 | Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13 | Synthesis and biological evaluation of novel carbon-11 labeled pyridyl ethers: candidate ligands for in vivo imaging of alpha4beta2 nicotinic acetylcholine receptors (alpha4beta2-nAChRs) in the brain with positron emission tomography. |
| AID145668 | In vitro displacement of [3H]methylcarbamylcholine from nicotinic acetylcholine receptor in rat brain cortex | 1999 | Journal of medicinal chemistry, Dec-02, Volume: 42, Issue:24 | Improving the nicotinic pharmacophore with a series of (Isoxazole)methylene-1-azacyclic compounds: synthesis, structure-activity relationship, and molecular modeling. |
| AID94462 | Ability to stimulate Rb+ efflux from human IMR-32 cell preparations containing human alpha3-betaX receptors | 1996 | Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4 | Novel 3-Pyridyl ethers with subnanomolar affinity for central neuronal nicotinic acetylcholine receptors. |
| AID219640 | Binding potency for nAChR subtype Alpha-1-beta-1-delta gamma(torpedo) | 1997 | Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26 | Neuronal nicotinic acetylcholine receptors as targets for drug discovery. |
| AID675880 | Agonist activity at alpha4beta 2 nAChR | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10 | Synthesis and nicotinic receptor activity of chemical space analogues of N-(3R)-1-azabicyclo[2.2.2]oct-3-yl-4-chlorobenzamide (PNU-282,987) and 1,4-diazabicyclo[3.2.2]nonane-4-carboxylic acid 4-bromophenyl ester (SSR180711). |
| AID14400 | Biodistribution in rat superior coliculus, expressed as percent I.D./g tissue | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | Synthesis and nicotinic acetylcholine receptor in vivo binding properties of 2-fluoro-3-[2(S)-2-azetidinylmethoxy]pyridine: a new positron emission tomography ligand for nicotinic receptors. |
| AID231915 | Ratio between the binding affinities towards rat alpha4-beta4 and alpha4-beta2 nACh receptor using [3H]EB as radioligand | 2004 | Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8 | Pharmacology of the agonist binding sites of rat neuronal nicotinic receptor subtypes expressed in HEK 293 cells. |
| AID427651 | Displacement of [3H]epibatidine from rat alpha3beta4 nicotinic receptor expressed in human HEK293 cells by liquid scintillation counting | 2009 | Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13 | Synthesis and biological evaluation of novel carbon-11 labeled pyridyl ethers: candidate ligands for in vivo imaging of alpha4beta2 nicotinic acetylcholine receptors (alpha4beta2-nAChRs) in the brain with positron emission tomography. |
| AID94457 | Cholinergic interactions was measured with FLIPR device on K177l cells and given as EC50. | 1998 | Journal of medicinal chemistry, Feb-26, Volume: 41, Issue:5 | Mono- and disubstituted-3,8-diazabicyclo[3.2.1]octane derivatives as analgesics structurally related to epibatidine: synthesis, activity, and modeling. |
| AID146459 | Cholinergic interactions was measured as displaced [3H]cystine from Nicotinic acetylcholine receptor alpha4-beta2 in rat brain membranes | 1998 | Journal of medicinal chemistry, Feb-26, Volume: 41, Issue:5 | Mono- and disubstituted-3,8-diazabicyclo[3.2.1]octane derivatives as analgesics structurally related to epibatidine: synthesis, activity, and modeling. |
| AID146772 | Binding affinity towards rat Nicotinic acetylcholine receptor alpha4-beta4 expressed in HEK293 cells using [3H]EB as radioligand | 2004 | Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8 | Pharmacology of the agonist binding sites of rat neuronal nicotinic receptor subtypes expressed in HEK 293 cells. |
| AID374872 | Binding affinity to Aplysia californica AchBP I106M, M116L mutant expressed in HEK293S cells assessed as specific photoincorporation at 46 pmol by scintillation counting | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID374868 | Binding affinity to wild type Aplysia californica AchBP expressed in HEK293S cells assessed as specific photoincorporation at 46 pmol by scintillation counting | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID371854 | Binding affinity to wild type Aplysia californica AchBP expressed in HEK293S cells by scintillation proximity assay | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID254466 | In vitro binding affinity towards rat Nicotinic acetylcholine receptor alpha4-beta4 using 0.5 nM [3H]epibatidine | 2005 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 15, Issue:19 | Epibatidine analogues as selective ligands for the alpha(x)beta2-containing subtypes of nicotinic acetylcholine receptors. |
| AID145983 | Binding affinity towards rat nicotinic acetylcholine receptor alpha2-beta2 expressed in HEK293 cells using [3H]EB as radioligand | 2004 | Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8 | Pharmacology of the agonist binding sites of rat neuronal nicotinic receptor subtypes expressed in HEK 293 cells. |
| AID1074613 | Agonist activity at rat alpha4beta2 nAChR expressed in Xenopus laevis oocytes assessed as stimulation of acetylcholine-induced current at 100 uM by two-electrode voltage clamp electrophysiological analysis relative to acetylcholine | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3 | Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2'-fluoro-3'-(substituted pyridinyl)-7-deschloroepibatidine analogues. |
| AID208878 | Cholinergic interactions was measured with FLIPR device on TE671 cells and given as Intrinsic activity | 1998 | Journal of medicinal chemistry, Feb-26, Volume: 41, Issue:5 | Mono- and disubstituted-3,8-diazabicyclo[3.2.1]octane derivatives as analgesics structurally related to epibatidine: synthesis, activity, and modeling. |
| AID227722 | Compound was evaluated for the binding selectivity for alpha4-beta2 (rat brain)/ vs alpha-7 (rat brain) | 1997 | Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26 | Neuronal nicotinic acetylcholine receptors as targets for drug discovery. |
| AID375118 | Binding affinity to Aplysia californica AchBP A107M, M116L, Y195F mutant expressed in HEK293S cells assessed as specific photoincorporation at 46 pmol by scintillation counting relative to wild type | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID374834 | Binding affinity to Aplysia californica AchBP M116L,Y195F mutant expressed in HEK293S cells by scintillation proximity assay | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID374838 | Binding affinity to Aplysia californica AchBP I106M, M116L, Y195F mutant expressed in HEK293S cells by scintillation proximity assay | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID145657 | Compound was evaluated for functional potencies and efficacies at rat Nicotinic acetylcholine receptor subtype PC12 (ganglionic) | 1997 | Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26 | Neuronal nicotinic acetylcholine receptors as targets for drug discovery. |
| AID145666 | Binding affinity towards nicotinic acetylcholine receptor using [3H]-cytisine as radioligand in rat forebrain homogenates | 2003 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21 | Rigidified acetylcholine mimics: conformational requirements for binding to neuronal nicotinic receptors. |
| AID1682110 | Selectivity ratio of displacement of [3H]-NMS from rat cerebral cortex muscarinic M1 receptor to displacement of [3H]-oxo-M from rat cerebral cortex muscarinic M1 receptor | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Pyridine alkaloids with activity in the central nervous system. |
| AID1410544 | Agonist activity at human alpha4beta2 nAChR by cell-based rubidium flux assay | 2018 | Journal of natural products, 04-27, Volume: 81, Issue:4 | Absolute Configuration and Pharmacology of the Poison Frog Alkaloid Phantasmidine. |
| AID374873 | Binding affinity to Aplysia californica AchBP I106M, M116L, Y195F mutant expressed in HEK293S cells assessed as specific photoincorporation at 46 pmol by scintillation counting | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID1092035 | Binding affinity to salt water mollusc Aplysia californica AChBP Y55W mutant assessed as [3H]acetamiprid binding by radioligand binding assay | 2011 | Journal of agricultural and food chemistry, Apr-13, Volume: 59, Issue:7 | Unique neonicotinoid binding conformations conferring selective receptor interactions. |
| AID1682116 | Agonist activity at Torpedo alpha1beta1deltagamma nACHR | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Pyridine alkaloids with activity in the central nervous system. |
| AID254462 | In vitro binding affinity towards rat Nicotinic acetylcholine receptor alpha2-beta4 using 0.5 nM [3H]epibatidine | 2005 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 15, Issue:19 | Epibatidine analogues as selective ligands for the alpha(x)beta2-containing subtypes of nicotinic acetylcholine receptors. |
| AID238151 | Dissociation constant against Nicotinic acetylcholine receptor alpha4-beta4 | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Novel pyridyl ring C5 substituted analogues of epibatidine and 3-(1-methyl-2(S)-pyrrolidinylmethoxy)pyridine (A-84543) as highly selective agents for neuronal nicotinic acetylcholine receptors containing beta2 subunits. |
| AID465078 | Agonist activity at human alpha3beta4 nAChR in human SH-SY5Y cells assessed as membrane depolarization after 1 hr by HPLC based fluorescence assay | 2010 | Journal of natural products, Mar-26, Volume: 73, Issue:3 | Phantasmidine: an epibatidine congener from the ecuadorian poison frog Epipedobates anthonyi. |
| AID361547 | Displacement of [3H]nicotine from alpha4beta2 nAChR in rat cortical membrane | 2008 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 18, Issue:16 | Epiboxidine and novel-related analogues: a convenient synthetic approach and estimation of their affinity at neuronal nicotinic acetylcholine receptor subtypes. |
| AID302775 | Agonist activity at recombinant human alpha-4-beta-2 nAChR expressed in HEK293 cells assessed as induction of calcium influx by FLIPR assay relative to nicotine | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22 | Synthesis and structure-activity relationship studies of 3,6-diazabicyclo[3.2.0]heptanes as novel alpha4beta2 nicotinic acetylcholine receptor selective agonists. |
| AID177747 | Agonist activity against alpha beta Nicotinic acetylcholine receptor (nAChR) in male rat cerebral cortex in antinociceptive assay in tail flick test | 2002 | Journal of medicinal chemistry, Oct-10, Volume: 45, Issue:21 | Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2-exo-2-(2',3'-disubstituted 5'-pyridinyl)-7-azabicyclo[2.2.1]heptanes: epibatidine analogues. |
| AID229713 | Functional / binding potency ratio for nAChR subtype Alpha7 (rat brain) | 1997 | Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26 | Neuronal nicotinic acetylcholine receptors as targets for drug discovery. |
| AID239381 | Inhibition of [125I]-iodo-MLA binding to Nicotinic acetylcholine receptor alpha-7 in rat cerebral cortex | 2005 | Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4 | Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 3'-substituted deschloroepibatidine analogues. Novel nicotinic antagonists. |
| AID264237 | Displacement of [3H]epibatidine from rat alpha3beta4 nACHR expressed in human HEK293 cells | 2006 | Journal of medicinal chemistry, May-04, Volume: 49, Issue:9 | Synthesis and pharmacological evaluation of novel 9- and 10-substituted cytisine derivatives. Nicotinic ligands of enhanced subtype selectivity. |
| AID264238 | Displacement of [3H]epibatidine from rat alpha-4-beta-2 nACHR expressed in human HEK293 cells | 2006 | Journal of medicinal chemistry, May-04, Volume: 49, Issue:9 | Synthesis and pharmacological evaluation of novel 9- and 10-substituted cytisine derivatives. Nicotinic ligands of enhanced subtype selectivity. |
| AID146150 | Tested for binding affinity against Nicotinic acetylcholine receptor alpha3-beta4 | 2003 | Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6 | Synthesis, nicotinic acetylcholine receptor binding affinities, and molecular modeling of constrained epibatidine analogues. |
| AID1682125 | Selectivity ratio of antinociceptive activity against mecamylamine-treated mouse to antinociceptive activity in mouse | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Pyridine alkaloids with activity in the central nervous system. |
| AID264235 | Displacement of [3H]epibatidine from rat alpha-2-beta-4 nACHR expressed in human HEK293 cells | 2006 | Journal of medicinal chemistry, May-04, Volume: 49, Issue:9 | Synthesis and pharmacological evaluation of novel 9- and 10-substituted cytisine derivatives. Nicotinic ligands of enhanced subtype selectivity. |
| AID276253 | Selectivity for human alpha-4-beta-2 nAChR over human alpha3beta4 nAChR | 2006 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21 | Epibatidine isomers and analogues: structure-activity relationships. |
| AID374850 | Binding affinity to Aplysia californica AchBP V108M, M116L, Y195F mutant expressed in HEK293S cells by scintillation proximity assay | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID35535 | Inhibition of [3H]epibatidine binding at the alpha beta nicotinic AChR in male rat cerebral cortex | 2001 | Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24 | Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2-exo-2-(2'-substituted-3'-phenyl-5'-pyridinyl)-7-azabicyclo[2.2.1]heptanes. Novel nicotinic antagonist. |
| AID374854 | Binding affinity to Aplysia californica AchBP S114M, M116L mutant expressed in HEK293S cells by scintillation proximity assay | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID239634 | Binding affinity for nicotinic acetylcholine receptor alpha 7 from human neuroblastoma SH-SY5Y cells; n=3 | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4 | 6'-Methylpyrido[3,4-b]norhomotropane: synthesis and outstanding potency in relation to the alpha4beta2 nicotinic receptor pharmacophore model. |
| AID318726 | Displacement of [3H]EPI from Aplysia AChBP expressed in HEK293S cells by scintillation proximity assay | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-22, Volume: 104, Issue:21 | Mapping the elusive neonicotinoid binding site. |
| AID282345 | Agonist activity at alpha-3-beta-4 nAChR in KXalpha-3-beta-4R2 cells by rubidium efflux assay | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Coaxing a pyridine nucleus to give up its aromaticity: synthesis and pharmacological characterization of novel conformationally restricted analogues of nicotine and anabasine. |
| AID14399 | Biodistribution in rat cerebellum, expressed as percent I.D./g tissue | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | Synthesis and nicotinic acetylcholine receptor in vivo binding properties of 2-fluoro-3-[2(S)-2-azetidinylmethoxy]pyridine: a new positron emission tomography ligand for nicotinic receptors. |
| AID145990 | Binding affinity against nicotinic acetylcholine receptor alpha2-beta4 using [3H]epibatidine as radioligand expressed in HEK293 cells or tsA cells | 2004 | Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1 | Synthesis and nicotinic receptor activity of a hydroxylated tropane. |
| AID145682 | Binding affinity against Nicotinic Acetylcholine Receptor was determined by measuring the displacement of [3H]cytisine from a preparation of whole rat brain. | 1996 | Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4 | Novel 3-Pyridyl ethers with subnanomolar affinity for central neuronal nicotinic acetylcholine receptors. |
| AID238147 | Dissociation constant against Nicotinic acetylcholine receptor alpha2-beta4 | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Novel pyridyl ring C5 substituted analogues of epibatidine and 3-(1-methyl-2(S)-pyrrolidinylmethoxy)pyridine (A-84543) as highly selective agents for neuronal nicotinic acetylcholine receptors containing beta2 subunits. |
| AID374862 | Binding affinity to Aplysia californica AchBP I118M, M116L, Y195F mutant expressed in HEK293S cells by scintillation proximity assay | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID146165 | Agonistic potency against nicotinic acetylcholine receptor alpha3-beta4 | 2004 | Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1 | Synthesis and nicotinic receptor activity of a hydroxylated tropane. |
| AID246898 | Effective dose to induce antinociception in mouse determined in hotplate test | 2005 | Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4 | Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 3'-substituted deschloroepibatidine analogues. Novel nicotinic antagonists. |
| AID276249 | Displacement of [3H]epibatidine from human recombinant alpha4beta2 nAChR in HEK293 cells by SPA assay | 2006 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21 | Epibatidine isomers and analogues: structure-activity relationships. |
| AID1074612 | Agonist activity at rat alpha3beta4 nAChR expressed in Xenopus laevis oocytes assessed as stimulation of acetylcholine-induced current at 100 uM by two-electrode voltage clamp electrophysiological analysis relative to acetylcholine | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3 | Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2'-fluoro-3'-(substituted pyridinyl)-7-deschloroepibatidine analogues. |
| AID640184 | Selectivity ratio of Ki for displacement of [3H]epibatidine from nAChR alpha4beta2 receptor on rat cortical membrane homogenate to Ki for displacement of [3H]bungarotoxin from nAChR alpha7 receptor on rat cortical membrane homogenate | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2 | Synthesis and binding affinity at α4β2 and α7 nicotinic acetylcholine receptors of new analogs of epibatidine and epiboxidine containing the 7-azabicyclo[2.2.1]hept-2-ene ring system. |
| AID374885 | Binding affinity to Aplysia californica AchBP M116Y, Y195F mutant expressed in HEK293S cells assessed as specific photoincorporation at 46 pmol by scintillation counting | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID341260 | Displacement of [3H]epibatidine from rat alpha2beta4 nAChR expressed in HEK293 cells | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Discovery of (-)-7-methyl-2-exo-[3'-(6-[18F]fluoropyridin-2-yl)-5'-pyridinyl]-7-azabicyclo[2.2.1]heptane, a radiolabeled antagonist for cerebral nicotinic acetylcholine receptor (alpha4beta2-nAChR) with optimal positron emission tomography imaging propert |
| AID145357 | Compound was evaluated for functional potencies and efficacies at human Nicotinic acetylcholine receptor subtype TE671 (muscle) | 1997 | Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26 | Neuronal nicotinic acetylcholine receptors as targets for drug discovery. |
| AID146610 | Binding affinity towards rat Nicotinic acetylcholine receptor alpha4-beta2 expressed in Xenopus oocytes using [3H]epibatidine as radioligand | 2004 | Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8 | Epibatidine structure-activity relationships. |
| AID536864 | Displacement of [3H]epibatidine from alpha7 nAChR in rat brain membranes after 2 hrs | 2010 | Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22 | Novel α3β4 nicotinic acetylcholine receptor-selective ligands. Discovery, structure-activity studies, and pharmacological evaluation. |
| AID640179 | Displacement of [3H]epibatidine from nAChR alpha4beta2 receptor on rat cortical membrane homogenate by beta-counting | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2 | Synthesis and binding affinity at α4β2 and α7 nicotinic acetylcholine receptors of new analogs of epibatidine and epiboxidine containing the 7-azabicyclo[2.2.1]hept-2-ene ring system. |
| AID146787 | Binding affinity to alpha-7 receptor subtype from human neuroblastoma SH-SY5Y cells was measured using [125I]-alpha-bungarotoxin as radioligand | 2003 | Bioorganic & medicinal chemistry letters, Feb-10, Volume: 13, Issue:3 | 5-Azidoepibatidine: an exceptionally potent photoaffinity ligand for neuronal alpha 4 beta 2 and alpha 7 nicotinic acetylcholine receptors. |
| AID254465 | In vitro binding affinity towards rat Nicotinic acetylcholine receptor alpha4-beta2 using 0.5 nM [3H]epibatidine | 2005 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 15, Issue:19 | Epibatidine analogues as selective ligands for the alpha(x)beta2-containing subtypes of nicotinic acetylcholine receptors. |
| AID751726 | Displacement of [I125]Epibatidine from nAChR in human IMR32 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. |
| AID536862 | Displacement of [3H]epibatidine from rat alpha3beta4 nAChR expressed in HEK292 cells after 3 hrs | 2010 | Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22 | Novel α3β4 nicotinic acetylcholine receptor-selective ligands. Discovery, structure-activity studies, and pharmacological evaluation. |
| AID229710 | Functional / binding potency ratio for nAChR subtype Alpha1-beta1 delta-gamma-torpedo) | 1997 | Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26 | Neuronal nicotinic acetylcholine receptors as targets for drug discovery. |
| AID374875 | Binding affinity to Aplysia californica AchBP A107M, M116L mutant expressed in HEK293S cells assessed as specific photoincorporation at 46 pmol by scintillation counting | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID239383 | Inhibition of [3H]epibatidine binding to rat Nicotinic acetylcholine receptor alpha3-beta4 | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Novel pyridyl ring C5 substituted analogues of epibatidine and 3-(1-methyl-2(S)-pyrrolidinylmethoxy)pyridine (A-84543) as highly selective agents for neuronal nicotinic acetylcholine receptors containing beta2 subunits. |
| AID251197 | Percentage efficacy in K-177 cells expressing acetylcholine central neuronal receptor type alpha-4 beta2 subunits as change in membrane potential | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4 | Halogenated and isosteric cytisine derivatives with increased affinity and functional activity at nicotinic acetylcholine receptors. |
| AID375126 | Binding affinity to Aplysia californica AchBP M116Y mutant expressed in HEK293S cells assessed as specific photoincorporation at 46 pmol by scintillation counting relative to wild type | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID146157 | Activation potency at Nicotinic acetylcholine receptor alpha3beta4, expressed as concentration required to achieve a half maximal activation | 2002 | Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15 | Synthesis and pharmacological characterization of novel analogues of the nicotinic acetylcholine receptor agonist (+/-)-UB-165. |
| AID1359522 | Displacement of [3H]epibatidine from alpha4beta2 nAChR in rat cortex membranes | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Pyridinyl- and pyridazinyl-3,6-diazabicyclo[3.1.1]heptane-anilines: Novel selective ligands with subnanomolar affinity for α |
| AID302774 | Agonist activity at recombinant human alpha-3-beta-4 nAChR expressed in HEK293 cells assessed as induction of calcium influx by FLIPR assay | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22 | Synthesis and structure-activity relationship studies of 3,6-diazabicyclo[3.2.0]heptanes as novel alpha4beta2 nicotinic acetylcholine receptor selective agonists. |
| AID375115 | Binding affinity to Aplysia californica AchBP I106M, M116L, Y195F mutant expressed in HEK293S cells assessed as specific photoincorporation at 46 pmol by scintillation counting relative to wild type | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID145850 | Selectivity ratio of Ki of Nicotinic acetylcholine receptor of Drosophila to Nicotinic acetylcholine receptor alpha4-beta2 | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Structural features of azidopyridinyl neonicotinoid probes conferring high affinity and selectivity for mammalian alpha4beta2 and Drosophila nicotinic receptors. |
| AID177745 | Agonist activity against alpha beta Nicotinic acetylcholine receptor (nAChR) in male rat cerebral cortex in antinociceptive assay in hot plate test | 2002 | Journal of medicinal chemistry, Oct-10, Volume: 45, Issue:21 | Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2-exo-2-(2',3'-disubstituted 5'-pyridinyl)-7-azabicyclo[2.2.1]heptanes: epibatidine analogues. |
| AID146771 | Binding affinity towards Nicotinic acetylcholine receptor alpha4-beta4 using [3H]epibatidine | 2004 | Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8 | Synthesis and pharmacological characterization of bivalent ligands of epibatidine at neuronal nicotinic acetylcholine receptors. |
| AID296790 | Displacement of [3H]epibatidine from nAChR of rat cortical membrane | 2007 | Journal of medicinal chemistry, Aug-09, Volume: 50, Issue:16 | Derivatives of (-)-7-methyl-2-(5-(pyridinyl)pyridin-3-yl)-7-azabicyclo[2.2.1]heptane are potential ligands for positron emission tomography imaging of extrathalamic nicotinic acetylcholine receptors. |
| AID375122 | Binding affinity to Aplysia californica AchBP S114M, M116L mutant expressed in HEK293S cells assessed as specific photoincorporation at 46 pmol by scintillation counting relative to wild type | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID1682109 | Toxicity in iv dosed rat | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Pyridine alkaloids with activity in the central nervous system. |
| AID146171 | Potency to displace [3H]nicotine binding to Nicotinic acetylcholine receptor alpha4-beta2 immuno-isolated from M10 cells | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Structural features of azidopyridinyl neonicotinoid probes conferring high affinity and selectivity for mammalian alpha4beta2 and Drosophila nicotinic receptors. |
| AID375116 | Binding affinity to Aplysia californica AchBP A107M mutant expressed in HEK293S cells assessed as specific photoincorporation at 46 pmol by scintillation counting relative to wild type | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID246901 | Effective dose to induce antinociception in mouse determined in tail-flick test | 2005 | Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4 | Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 3'-substituted deschloroepibatidine analogues. Novel nicotinic antagonists. |
| AID91525 | Ability to stimulate Rb+ efflux from human IMR-32 cell preparations containing human alpha3-betaX receptors | 1996 | Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4 | Novel 3-Pyridyl ethers with subnanomolar affinity for central neuronal nicotinic acetylcholine receptors. |
| AID91534 | Maximum efficacy relative to 100(uM) (S)-nicotine for cell preparations containing alpha3-betaX IMR32 cells | 1996 | Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4 | Novel 3-Pyridyl ethers with subnanomolar affinity for central neuronal nicotinic acetylcholine receptors. |
| AID1682129 | Potency index, ratio of morphine ED50 to test compound ED50 for antinociceptive activity in naloxone treated mouse assessed as induction of Straub-tail response | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Pyridine alkaloids with activity in the central nervous system. |
| AID417950 | Displacement of [3H]cytisine from alpha4beta2 nAChR in rat brain membrane | 2009 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6 | Preparation and characterization of N-(3-pyridinyl) spirocyclic diamines as ligands for nicotinic acetylcholine receptors. |
| AID147083 | Binding affinity at homopentameric Nicotinic acetylcholine receptor alpha-7 subtype using [3H]S-(-)-nicotine as radioligand | 1999 | Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16 | Molecular recognition in nicotinic acetylcholine receptors: the importance of pi-cation interactions. |
| AID341261 | Displacement of [3H]epibatidine from rat alpha3beta2 nAChR expressed in HEK293 cells | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Discovery of (-)-7-methyl-2-exo-[3'-(6-[18F]fluoropyridin-2-yl)-5'-pyridinyl]-7-azabicyclo[2.2.1]heptane, a radiolabeled antagonist for cerebral nicotinic acetylcholine receptor (alpha4beta2-nAChR) with optimal positron emission tomography imaging propert |
| AID417952 | Agonist activity at human recombinant alpha4beta2 nAChR expressed in human IMR32 cells assessed as calcium dynamics by FLIPR assay relative to nicotine | 2009 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6 | Preparation and characterization of N-(3-pyridinyl) spirocyclic diamines as ligands for nicotinic acetylcholine receptors. |
| AID238148 | Dissociation constant against Nicotinic acetylcholine receptor alpha3-beta2 | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Novel pyridyl ring C5 substituted analogues of epibatidine and 3-(1-methyl-2(S)-pyrrolidinylmethoxy)pyridine (A-84543) as highly selective agents for neuronal nicotinic acetylcholine receptors containing beta2 subunits. |
| AID302772 | Displacement of [3H]cytisine from neuronal nicotinic acetylcholine receptor in rat brain membrane | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22 | Synthesis and structure-activity relationship studies of 3,6-diazabicyclo[3.2.0]heptanes as novel alpha4beta2 nicotinic acetylcholine receptor selective agonists. |
| AID146943 | Inhibition of [125I]- iodo-MLA binding at the Nicotinic acetylcholine receptor alpha-7 (nAChR) in male rat cerebral cortex | 2002 | Journal of medicinal chemistry, Oct-10, Volume: 45, Issue:21 | Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2-exo-2-(2',3'-disubstituted 5'-pyridinyl)-7-azabicyclo[2.2.1]heptanes: epibatidine analogues. |
| AID282346 | Agonist activity at alpha-3-beta-4 nAChR in KXalpha-3-beta-4R2 cells by rubidium efflux assay relative to nicotine | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Coaxing a pyridine nucleus to give up its aromaticity: synthesis and pharmacological characterization of novel conformationally restricted analogues of nicotine and anabasine. |
| AID374883 | Binding affinity to Aplysia californica AchBP I118M, M116L, Y195F mutant expressed in HEK293S cells assessed as specific photoincorporation at 46 pmol by scintillation counting | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID146155 | Agonistic activity against rat Alpha3 beta-4 Nicotinic Receptor expressed in Xenopus oocytes | 2001 | Journal of medicinal chemistry, Jan-04, Volume: 44, Issue:1 | exo-2-(Pyridazin-4-yl)-7-azabicyclo[2.2.1]heptanes: syntheses and nicotinic acetylcholine receptor agonist activity of potent pyridazine analogues of (+/-)-epibatidine. |
| AID640180 | Displacement of [3H]bungarotoxin from nAChR alpha7 receptor on rat cortical membrane homogenate by gamma-counting | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2 | Synthesis and binding affinity at α4β2 and α7 nicotinic acetylcholine receptors of new analogs of epibatidine and epiboxidine containing the 7-azabicyclo[2.2.1]hept-2-ene ring system. |
| AID374887 | Binding affinity to Aplysia californica AchBP Y195F mutant expressed in HEK293S cells assessed as specific photoincorporation at 46 pmol by scintillation counting relative to wild type | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID146158 | Functional potency measured as stimulation at rat Nicotinic acetylcholine receptor alpha3-beta4 expressed in Xenopus oocytes | 2004 | Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8 | Epibatidine structure-activity relationships. |
| AID239589 | Displacement of [3H]-cytisine from Alpha4-beta2 Nicotinic acetylcholine receptor of rat brain homogenates | 2005 | Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16 | Ligand selectivity for the acetylcholine binding site of the rat alpha4beta2 and alpha3beta4 nicotinic subtypes investigated by molecular docking. |
| AID1101296 | Toxicity against Musca domestica (house fly) dosed with compound through intra-thoracic injection pre-treated with 100 ug/g metabolic detoxification inhibitor O-propyl O-(2-propynyl)phenylphosphonate | 2000 | Journal of agricultural and food chemistry, Dec, Volume: 48, Issue:12 | Neonicotinoid insecticides: molecular features conferring selectivity for insect versus mammalian nicotinic receptors. |
| AID1410540 | Displacement of [3H]epibatidine from rat forebrain nAChR after 4 hrs by liquid scintillation counting method | 2018 | Journal of natural products, 04-27, Volume: 81, Issue:4 | Absolute Configuration and Pharmacology of the Poison Frog Alkaloid Phantasmidine. |
| AID322339 | Antinociceptive activity in sc dosed in acute pain mouse model by hot plate method | 2008 | Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2 | Synthesis, nicotinic acetylcholine receptor binding, and pharmacological properties of 3'-(substituted phenyl)deschloroepibatidine analogs. |
| AID146939 | Binding potency for Nicotinic acetylcholine receptor alpha-7 (rat brain) | 1997 | Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26 | Neuronal nicotinic acetylcholine receptors as targets for drug discovery. |
| AID291934 | Agonist activity at alpha-4-beta-2 in IMR-32cells assessed as calcium influx by FLIPR assay | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15 | Structure-activity studies and analgesic efficacy of N-(3-pyridinyl)-bridged bicyclic diamines, exceptionally potent agonists at nicotinic acetylcholine receptors. |
| AID244249 | Selectivity against Nicotinic acetylcholine receptor subtypes alpha3-beta4 and alpha4-beta2 | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Novel pyridyl ring C5 substituted analogues of epibatidine and 3-(1-methyl-2(S)-pyrrolidinylmethoxy)pyridine (A-84543) as highly selective agents for neuronal nicotinic acetylcholine receptors containing beta2 subunits. |
| AID302776 | Agonist activity at recombinant human alpha3beta4 nAChR expressed in HEK293 cells assessed as induction of calcium influx by FLIPR assay relative to nicotine | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22 | Synthesis and structure-activity relationship studies of 3,6-diazabicyclo[3.2.0]heptanes as novel alpha4beta2 nicotinic acetylcholine receptor selective agonists. |
| AID145853 | Inhibition of [3H]- epibatidine binding at the Nicotinic acetylcholine receptor alpha beta (nAChR) in male rat cerebral cortex | 2002 | Journal of medicinal chemistry, Oct-10, Volume: 45, Issue:21 | Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2-exo-2-(2',3'-disubstituted 5'-pyridinyl)-7-azabicyclo[2.2.1]heptanes: epibatidine analogues. |
| AID1092037 | Binding affinity to Drosophila brain nicotinic acetylcholine receptor assessed as [3H]IMI binding by radioligand binding assay | 2011 | Journal of agricultural and food chemistry, Apr-13, Volume: 59, Issue:7 | Unique neonicotinoid binding conformations conferring selective receptor interactions. |
| AID374846 | Binding affinity to Aplysia californica AchBP V108M mutant expressed in HEK293S cells by scintillation proximity assay | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID146161 | Binding affinity towards Nicotinic acetylcholine receptor alpha3-beta4 using [3H]epibatidine | 2004 | Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8 | Synthesis and pharmacological characterization of bivalent ligands of epibatidine at neuronal nicotinic acetylcholine receptors. |
| AID1101297 | Toxicity in ip dosed Mus musculus (mouse) | 2000 | Journal of agricultural and food chemistry, Dec, Volume: 48, Issue:12 | Neonicotinoid insecticides: molecular features conferring selectivity for insect versus mammalian nicotinic receptors. |
| AID341259 | Displacement of [3H]epibatidine from rat alpha2beta2 nAChR expressed in HEK293 cells | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Discovery of (-)-7-methyl-2-exo-[3'-(6-[18F]fluoropyridin-2-yl)-5'-pyridinyl]-7-azabicyclo[2.2.1]heptane, a radiolabeled antagonist for cerebral nicotinic acetylcholine receptor (alpha4beta2-nAChR) with optimal positron emission tomography imaging propert |
| AID1074614 | Displacement of [3H]-epibatidine from alpha4beta2* nAChR in Sprague-Dawley rat cerebral cortex after 4 hrs by liquid scintillation counting analysis | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3 | Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2'-fluoro-3'-(substituted pyridinyl)-7-deschloroepibatidine analogues. |
| AID146483 | Binding affinity to Nicotinic acetylcholine receptor alpha4-beta2 using +/-[3H]epibatidine as radioligand in rat brain | 2002 | Journal of medicinal chemistry, Feb-28, Volume: 45, Issue:5 | Synthesis and nicotinic binding studies on enantiopure diazine analogues of the novel (2-chloro-5-pyridyl)-9-azabicyclo[4.2.1]non-2-ene UB-165. |
| AID465076 | Agonist activity at rat alpha3beta4 nAChR expressed in HEK cells assessed as membrane depolarization after 1 hr by HPLC based fluorescence assay | 2010 | Journal of natural products, Mar-26, Volume: 73, Issue:3 | Phantasmidine: an epibatidine congener from the ecuadorian poison frog Epipedobates anthonyi. |
| AID145677 | Kapp value towards nicotinic acetylcholine receptor was obtained from three to four independent competition binding experiments using [3H]-NCEPB | 1997 | Journal of medicinal chemistry, Jul-18, Volume: 40, Issue:15 | Synthesis and nicotinic acetylcholine receptor binding properties of exo-2-(2'-fluoro-5'-pyridinyl)-7-azabicyclo-[2.2.1]heptane: a new positron emission tomography ligand for nicotinic receptors. |
| AID132750 | In vivo analgesic agonist activity after subcutaneous administration, using hotplate assay | 2002 | Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14 | Synthesis and biological evaluation at nicotinic acetylcholine receptors of N-arylalkyl- and N-aryl-7-azabicyclo[2.2.1]heptanes. |
| AID146007 | Binding affinity towards rat Nicotinic acetylcholine receptor alpha3-beta2 expressed in Xenopus oocytes using [3H]epibatidine as radioligand | 2004 | Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8 | Epibatidine structure-activity relationships. |
| AID397989 | Displacement of [3H]cytisine from alpha4beta2 nicotinic acetylcholine receptor in rat brain minus cerebellum membrane | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Octahydropyrrolo[3,4-c]pyrrole: a diamine scaffold for construction of either alpha4beta2 or alpha7-selective nicotinic acetylcholine receptor (nAChR) ligands. Substitutions that switch subtype selectivity. |
| AID251184 | Percentage efficacy in TE671 cells expressing acetylcholine neuromuscular receptor as change in membrane potential | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4 | Halogenated and isosteric cytisine derivatives with increased affinity and functional activity at nicotinic acetylcholine receptors. |
| AID452526 | Inhibition of alpha3beta4 nAChR | 2010 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1 | Structure-activity relationships of N-substituted ligands for the alpha7 nicotinic acetylcholine receptor. |
| AID246397 | Change in membrane potential in TE-671 cells expressing acetylcholine neuromuscular receptors | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4 | Halogenated and isosteric cytisine derivatives with increased affinity and functional activity at nicotinic acetylcholine receptors. |
| AID146006 | Binding affinity towards rat Nicotinic acetylcholine receptor alpha3-beta2 expressed in HEK293 cells using [3H]EB as radioligand | 2004 | Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8 | Pharmacology of the agonist binding sites of rat neuronal nicotinic receptor subtypes expressed in HEK 293 cells. |
| AID146151 | Tested for binding affinity against Nicotinic acetylcholine receptor alpha3-beta4 | 2003 | Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6 | Synthesis, nicotinic acetylcholine receptor binding affinities, and molecular modeling of constrained epibatidine analogues. |
| AID291935 | Agonist activity at rat striatal tissue assessed as dopamine release | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15 | Structure-activity studies and analgesic efficacy of N-(3-pyridinyl)-bridged bicyclic diamines, exceptionally potent agonists at nicotinic acetylcholine receptors. |
| AID238080 | Dissociation constant for nicotinic acetylcholine receptor alpha4-beta2 of mouse M10 cells; n=3 | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4 | 6'-Methylpyrido[3,4-b]norhomotropane: synthesis and outstanding potency in relation to the alpha4beta2 nicotinic receptor pharmacophore model. |
| AID146470 | Binding affinity towards alpha4-beta2 nicotinic receptor was determined in rat brain membrane using [3H]cytisine as radioligand | 2003 | Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6 | Syntheses and biological properties of cysteine-reactive epibatidine derivatives. |
| AID374866 | Binding affinity to Aplysia californica AchBP M116Y, Y195F mutant expressed in HEK293S cells by scintillation proximity assay | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID1092036 | Binding affinity to recombinant Gallus gallus (chicken) alpha4beta2 nicotinic acetylcholine receptor assessed as [3H]NIC binding by radioligand binding assay | 2011 | Journal of agricultural and food chemistry, Apr-13, Volume: 59, Issue:7 | Unique neonicotinoid binding conformations conferring selective receptor interactions. |
| AID145678 | Ability of compound to compete with 50 pM of 5-[125I]iodo-A-85,380 for receptor binding sites in rat brain membranes at room temperature | 2004 | Journal of medicinal chemistry, May-06, Volume: 47, Issue:10 | 5-substituted derivatives of 6-halogeno-3-((2-(S)-azetidinyl)methoxy)pyridine and 6-halogeno-3-((2-(S)-pyrrolidinyl)methoxy)pyridine with low picomolar affinity for alpha4beta2 nicotinic acetylcholine receptor and wide range of lipophilicity: potential pr |
| AID375114 | Binding affinity to Aplysia californica AchBP I106M, M116L mutant expressed in HEK293S cells assessed as specific photoincorporation at 46 pmol by scintillation counting relative to wild type | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID341263 | Displacement of [3H]epibatidine from rat alpha4beta4 nAChR expressed in HEK293 cells | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Discovery of (-)-7-methyl-2-exo-[3'-(6-[18F]fluoropyridin-2-yl)-5'-pyridinyl]-7-azabicyclo[2.2.1]heptane, a radiolabeled antagonist for cerebral nicotinic acetylcholine receptor (alpha4beta2-nAChR) with optimal positron emission tomography imaging propert |
| AID465079 | Agonist activity at rat alpha3beta4 nAChR expressed in HEK cells assessed as elevation of intracellular calcium after 1 hr by HPLC based fluorescence assay | 2010 | Journal of natural products, Mar-26, Volume: 73, Issue:3 | Phantasmidine: an epibatidine congener from the ecuadorian poison frog Epipedobates anthonyi. |
| AID3056 | In vitro binding affinity towards (alpha-4)2(beta-2)3 neuronal nicotinic acetylcholine receptor in P2 membrane fractions of rat forebrain | 2003 | Journal of medicinal chemistry, May-22, Volume: 46, Issue:11 | 3D QSAR analyses-guided rational design of novel ligands for the (alpha4)2(beta2)3 nicotinic acetylcholine receptor. |
| AID145686 | Compound was evaluated for its ability to displace [3H]-cytisine binding from high-affinity Nicotinic acetylcholine receptor in rat brain (principally the alpha4-beta2 nAChR subtype) | 1998 | Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4 | Identification and initial structure-activity relationships of (R)-5-(2-azetidinylmethoxy)-2-chloropyridine (ABT-594), a potent, orally active, non-opiate analgesic agent acting via neuronal nicotinic acetylcholine receptors. |
| AID1410541 | Potency index, ratio of epibatidine Ki to racemic phantasmidine Ki for displacement of [3H]epibatidine from rat forebrain nAChR | 2018 | Journal of natural products, 04-27, Volume: 81, Issue:4 | Absolute Configuration and Pharmacology of the Poison Frog Alkaloid Phantasmidine. |
| AID1682126 | Antinociceptive activity in mouse | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Pyridine alkaloids with activity in the central nervous system. |
| AID233593 | Ratio of IC50 values for displacing [3H]-MCC to [3H]OXO-M | 1999 | Journal of medicinal chemistry, Dec-02, Volume: 42, Issue:24 | Improving the nicotinic pharmacophore with a series of (Isoxazole)methylene-1-azacyclic compounds: synthesis, structure-activity relationship, and molecular modeling. |
| AID177746 | Agonist activity against alpha beta Nicotinic acetylcholine receptor (nAChR) in male rat cerebral cortex in antinociceptive assay in hypothermia test | 2002 | Journal of medicinal chemistry, Oct-10, Volume: 45, Issue:21 | Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2-exo-2-(2',3'-disubstituted 5'-pyridinyl)-7-azabicyclo[2.2.1]heptanes: epibatidine analogues. |
| AID146931 | Binding affinity at rat brain Nicotinic acetylcholine receptor alpha7 | 2002 | Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15 | Synthesis and pharmacological characterization of novel analogues of the nicotinic acetylcholine receptor agonist (+/-)-UB-165. |
| AID374842 | Binding affinity to Aplysia californica AchBP A107M, M116L mutant expressed in HEK293S cells by scintillation proximity assay | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID452525 | Inhibition of alpha4beta2 nAChR | 2010 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1 | Structure-activity relationships of N-substituted ligands for the alpha7 nicotinic acetylcholine receptor. |
| AID146477 | Functional potency measured as stimulation at rat Nicotinic acetylcholine receptor alpha4-beta2 expressed in Xenopus oocytes | 2004 | Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8 | Epibatidine structure-activity relationships. |
| AID146612 | In vitro binding affinity by inhibiting [3H]cytisine binding in rat brain tissue at Nicotinic acetylcholine receptor alpha4-beta2 | 2002 | Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14 | Synthesis and biological evaluation at nicotinic acetylcholine receptors of N-arylalkyl- and N-aryl-7-azabicyclo[2.2.1]heptanes. |
| AID146005 | Binding affinity towards Nicotinic acetylcholine receptor alpha3-beta2 using [3H]epibatidine | 2004 | Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8 | Synthesis and pharmacological characterization of bivalent ligands of epibatidine at neuronal nicotinic acetylcholine receptors. |
| AID374877 | Binding affinity to Aplysia californica AchBP V108M mutant expressed in HEK293S cells assessed as specific photoincorporation at 46 pmol by scintillation counting | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID239419 | Binding affinity for nicotinic acetylcholine receptor alpha4-beta2 from mouse M10 cells; n=3 | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4 | 6'-Methylpyrido[3,4-b]norhomotropane: synthesis and outstanding potency in relation to the alpha4beta2 nicotinic receptor pharmacophore model. |
| AID115288 | Minimal dose able to induce a statistically significant increase of the pain threshold, done on mouse; sc | 1998 | Journal of medicinal chemistry, Feb-26, Volume: 41, Issue:5 | Mono- and disubstituted-3,8-diazabicyclo[3.2.1]octane derivatives as analgesics structurally related to epibatidine: synthesis, activity, and modeling. |
| AID689290 | Displacement of [3H]epibatidine from chimeric human alpha7-5-HT3A receptor expressed in HEK293 cells after 2 hrs by scintillation counter analysis | 2012 | Bioorganic & medicinal chemistry, Oct-01, Volume: 20, Issue:19 | Identification of novel α7 nicotinic receptor ligands by in silico screening against the crystal structure of a chimeric α7 receptor ligand binding domain. |
| AID1074598 | Effect on hypothermia in sc dosed mouse after 30 mins | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3 | Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2'-fluoro-3'-(substituted pyridinyl)-7-deschloroepibatidine analogues. |
| AID145846 | Binding affinity against nicotinic acetylcholine receptor using [3H]epibatidine as radioligand in rat brain tissue | 2004 | Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1 | Synthesis and nicotinic receptor activity of a hydroxylated tropane. |
| AID1359523 | Displacement of [125I]alpha-bungarotoxin from alpha7 nAChR in rat hippocampal membranes | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Pyridinyl- and pyridazinyl-3,6-diazabicyclo[3.1.1]heptane-anilines: Novel selective ligands with subnanomolar affinity for α |
| AID427649 | Displacement of [3H]epibatidine from rat alpha2beta4 nicotinic receptor expressed in human HEK293 cells by liquid scintillation counting | 2009 | Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13 | Synthesis and biological evaluation of novel carbon-11 labeled pyridyl ethers: candidate ligands for in vivo imaging of alpha4beta2 nicotinic acetylcholine receptors (alpha4beta2-nAChRs) in the brain with positron emission tomography. |
| AID1074608 | Antagonist activity at rat alpha7 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of acetylcholine-induced current at 100 uM by two-electrode voltage clamp electrophysiological analysis relative to acetylcholine | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3 | Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2'-fluoro-3'-(substituted pyridinyl)-7-deschloroepibatidine analogues. |
| AID697853 | Inhibition of horse BChE at 2 mg/ml by Ellman's method | 2012 | Bioorganic & medicinal chemistry, Nov-15, Volume: 20, Issue:22 | Exploration of natural compounds as sources of new bifunctional scaffolds targeting cholinesterases and beta amyloid aggregation: the case of chelerythrine. |
| AID146478 | In vitro binding affinity by inhibiting [3H]dopamine release in rat brain tissue at Nicotinic acetylcholine receptor alpha4-beta2 | 2002 | Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14 | Synthesis and biological evaluation at nicotinic acetylcholine receptors of N-arylalkyl- and N-aryl-7-azabicyclo[2.2.1]heptanes. |
| AID129321 | Antinociceptive activity was tested in the mouse tail-flick test at 15 mg/kg | 2004 | Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8 | Epibatidine structure-activity relationships. |
| AID322332 | Displacement of [125I]iodoMLA from alpha-7 nAChR in rat cerebral cortex | 2008 | Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2 | Synthesis, nicotinic acetylcholine receptor binding, and pharmacological properties of 3'-(substituted phenyl)deschloroepibatidine analogs. |
| AID146773 | Binding affinity towards rat Nicotinic acetylcholine receptor alpha4-beta4 expressed in Xenopus oocytes using [3H]epibatidine as radioligand | 2004 | Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8 | Epibatidine structure-activity relationships. |
| AID145987 | Tested for binding affinity against Nicotinic acetylcholine receptor alpha2-beta4 | 2003 | Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6 | Synthesis, nicotinic acetylcholine receptor binding affinities, and molecular modeling of constrained epibatidine analogues. |
| AID536867 | Agonist activity at rat alpha3beta4 nAChR expressed in HEK292 cells assessed as increase of calcium influx by FLIPR assay | 2010 | Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22 | Novel α3β4 nicotinic acetylcholine receptor-selective ligands. Discovery, structure-activity studies, and pharmacological evaluation. |
| AID146458 | Binding potency for Nicotinic acetylcholine receptor alpha4-beta2 (rat brain) | 1997 | Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26 | Neuronal nicotinic acetylcholine receptors as targets for drug discovery. |
| AID146774 | Functional potency measured as maximum stimulation at rat Nicotinic acetylcholine receptor alpha4-beta4 expressed in Xenopus oocytes | 2004 | Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8 | Epibatidine structure-activity relationships. |
| AID21871 | Calculated partition coefficient (clogP) | 2004 | Journal of medicinal chemistry, May-06, Volume: 47, Issue:10 | 5-substituted derivatives of 6-halogeno-3-((2-(S)-azetidinyl)methoxy)pyridine and 6-halogeno-3-((2-(S)-pyrrolidinyl)methoxy)pyridine with low picomolar affinity for alpha4beta2 nicotinic acetylcholine receptor and wide range of lipophilicity: potential pr |
| AID239452 | Inhibition of [3H]epibatidine binding to Nicotinic acetylcholine receptor alpha4-beta2 in rat cerebral cortex | 2005 | Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4 | Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 3'-substituted deschloroepibatidine analogues. Novel nicotinic antagonists. |
| AID371856 | Binding affinity to Aplysia californica AchBP M116L mutant expressed in HEK293S cells by scintillation proximity assay | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID246869 | Effective dose to induce spontaneous activity in mouse was determined | 2005 | Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4 | Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 3'-substituted deschloroepibatidine analogues. Novel nicotinic antagonists. |
| AID417953 | Agonist activity at human recombinant alpha3beta4 nAChR expressed in human IMR32 cells assessed as calcium dynamics by FLIPR assay | 2009 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6 | Preparation and characterization of N-(3-pyridinyl) spirocyclic diamines as ligands for nicotinic acetylcholine receptors. |
| AID195570 | Agonistic activity against Rat muscle Nicotinic Receptor | 2001 | Journal of medicinal chemistry, Jan-04, Volume: 44, Issue:1 | exo-2-(Pyridazin-4-yl)-7-azabicyclo[2.2.1]heptanes: syntheses and nicotinic acetylcholine receptor agonist activity of potent pyridazine analogues of (+/-)-epibatidine. |
| AID1074600 | Antinociceptive activity in sc dosed mouse after 5 mins by tail flick test | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3 | Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2'-fluoro-3'-(substituted pyridinyl)-7-deschloroepibatidine analogues. |
| AID21870 | Calculated partition coefficient (clogD7.4) | 2004 | Journal of medicinal chemistry, May-06, Volume: 47, Issue:10 | 5-substituted derivatives of 6-halogeno-3-((2-(S)-azetidinyl)methoxy)pyridine and 6-halogeno-3-((2-(S)-pyrrolidinyl)methoxy)pyridine with low picomolar affinity for alpha4beta2 nicotinic acetylcholine receptor and wide range of lipophilicity: potential pr |
| AID374864 | Binding affinity to Aplysia californica AchBP M116Y mutant expressed in HEK293S cells by scintillation proximity assay | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID146768 | Tested for binding affinity against Nicotinic acetylcholine receptor alpha4-beta4 | 2003 | Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6 | Synthesis, nicotinic acetylcholine receptor binding affinities, and molecular modeling of constrained epibatidine analogues. |
| AID1410545 | Agonist activity at human alpha4beta2 nAChR by cell-based rubidium flux assay relative to 100 uM nicotine | 2018 | Journal of natural products, 04-27, Volume: 81, Issue:4 | Absolute Configuration and Pharmacology of the Poison Frog Alkaloid Phantasmidine. |
| AID254463 | In vitro binding affinity towards rat Nicotinic acetylcholine receptor alpha3-beta2 using 0.5 nM [3H]epibatidine | 2005 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 15, Issue:19 | Epibatidine analogues as selective ligands for the alpha(x)beta2-containing subtypes of nicotinic acetylcholine receptors. |
| AID129319 | Antinociceptive activity was tested in the mouse hot plate test at 15 mg/kg | 2004 | Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8 | Epibatidine structure-activity relationships. |
| AID310061 | Inhibition of alpha-4-beta-2 nAChR | 2007 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 17, Issue:22 | Unique spirocyclopiperazinium salt III: further investigation of monospirocyclopiperazinium (MSPZ) salts as potential analgesics. |
| AID145821 | In vitro inhibition of 5-(125I)A-85380 binding to nicotinic acetylcholine receptor (nAChR) of rat brain | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Synthesis and evaluation of a novel series of 2-chloro-5-((1-methyl-2-(S)-pyrrolidinyl)methoxy)-3-(2-(4-pyridinyl)vinyl)pyridine analogues as potential positron emission tomography imaging agents for nicotinic acetylcholine receptors. |
| AID256414 | Agonistic activity as [86Rb+] efflux from KXalpha-3-beta-4R2 cells expressing rat Nicotinic acetylcholine receptor at 100 uM | 2005 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 15, Issue:19 | Epibatidine analogues as selective ligands for the alpha(x)beta2-containing subtypes of nicotinic acetylcholine receptors. |
| AID1101293 | Inhibition of [3H]alpha-BGT binding to alpha7 nicotinic acetylcholine receptor in Homo sapiens (human) SH-SY5Y cells | 2000 | Journal of agricultural and food chemistry, Dec, Volume: 48, Issue:12 | Neonicotinoid insecticides: molecular features conferring selectivity for insect versus mammalian nicotinic receptors. |
| AID1410539 | Potency index, ratio of epibatidine Ki to racemic phantasmidine Ki for displacement of [3H]epibatidine from alpha4beta2 nAChR (unknown origin) expressed in HEK cell membranes | 2018 | Journal of natural products, 04-27, Volume: 81, Issue:4 | Absolute Configuration and Pharmacology of the Poison Frog Alkaloid Phantasmidine. |
| AID374836 | Binding affinity to Aplysia californica AchBP I106M, M116L mutant expressed in HEK293S cells by scintillation proximity assay | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID146769 | Tested for binding affinity against Nicotinic acetylcholine receptor alpha4-beta4 | 2003 | Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6 | Synthesis, nicotinic acetylcholine receptor binding affinities, and molecular modeling of constrained epibatidine analogues. |
| AID251066 | Percentage efficacy in KXalpha-3-beta-4R2 cells expressing rat nicotinic acetylcholine receptor alpha3 beta-4 subunits relative to (1)-epibatidine | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4 | Halogenated and isosteric cytisine derivatives with increased affinity and functional activity at nicotinic acetylcholine receptors. |
| AID146637 | Binding affinity against nicotinic acetylcholine receptor alpha4-beta2 using [3H]epibatidine as radioligand expressed in HEK293 cells or tsA cells | 2004 | Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1 | Synthesis and nicotinic receptor activity of a hydroxylated tropane. |
| AID91526 | Cholinergic interactions was measured with FLIPR device on IMR-32 cells of human neuroblastoma clonal line, given as effective dose | 1998 | Journal of medicinal chemistry, Feb-26, Volume: 41, Issue:5 | Mono- and disubstituted-3,8-diazabicyclo[3.2.1]octane derivatives as analgesics structurally related to epibatidine: synthesis, activity, and modeling. |
| AID375123 | Binding affinity to Aplysia californica AchBP S114M, M116L, Y195F mutant expressed in HEK293S cells assessed as specific photoincorporation at 46 pmol by scintillation counting relative to wild type | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID238149 | Dissociation constant against Nicotinic acetylcholine receptor alpha3-beta4 | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Novel pyridyl ring C5 substituted analogues of epibatidine and 3-(1-methyl-2(S)-pyrrolidinylmethoxy)pyridine (A-84543) as highly selective agents for neuronal nicotinic acetylcholine receptors containing beta2 subunits. |
| AID1074599 | Antinociceptive activity in sc dosed mouse by hot plate test | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3 | Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2'-fluoro-3'-(substituted pyridinyl)-7-deschloroepibatidine analogues. |
| AID536863 | Displacement of [3H]epibatidine from rat alpha4beta2 nAChR expressed in HEK292 cells after 3 hrs | 2010 | Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22 | Novel α3β4 nicotinic acetylcholine receptor-selective ligands. Discovery, structure-activity studies, and pharmacological evaluation. |
| AID488648 | Displacement of [125I]alpha-Bungarotoxin from alpha7 nAChR in rat cortical membrane | 2010 | Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12 | Novel tricyclic Delta(2)-isoxazoline and 3-oxo-2-methyl-isoxazolidine derivatives: synthesis and binding affinity at neuronal nicotinic acetylcholine receptor subtypes. |
| AID238150 | Dissociation constant against Nicotinic acetylcholine receptor alpha4-beta2 | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Novel pyridyl ring C5 substituted analogues of epibatidine and 3-(1-methyl-2(S)-pyrrolidinylmethoxy)pyridine (A-84543) as highly selective agents for neuronal nicotinic acetylcholine receptors containing beta2 subunits. |
| AID322331 | Displacement of [3H]epibatidine from alpha-4-beta-2 nAChR in rat cerebral cortex | 2008 | Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2 | Synthesis, nicotinic acetylcholine receptor binding, and pharmacological properties of 3'-(substituted phenyl)deschloroepibatidine analogs. |
| AID145859 | Tested for binding affinity against Nicotinic acetylcholine receptor alpha2-beta2 | 2003 | Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6 | Synthesis, nicotinic acetylcholine receptor binding affinities, and molecular modeling of constrained epibatidine analogues. |
| AID1682119 | Binding affinity to human alpha3beta4 nAChR | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Pyridine alkaloids with activity in the central nervous system. |
| AID219638 | Functional potency for nAChR subtype Alpha-1-beta-1-delta gamma (torpedo) | 1997 | Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26 | Neuronal nicotinic acetylcholine receptors as targets for drug discovery. |
| AID322358 | Effect on locomotor activity in sc dosed mouse assessed as spontaneous activity | 2008 | Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2 | Synthesis, nicotinic acetylcholine receptor binding, and pharmacological properties of 3'-(substituted phenyl)deschloroepibatidine analogs. |
| AID146464 | Agonistic activity against rat Nicotinic acetylcholine receptor alpha4-beta2 expressed in Xenopus oocytes | 2001 | Journal of medicinal chemistry, Jan-04, Volume: 44, Issue:1 | exo-2-(Pyridazin-4-yl)-7-azabicyclo[2.2.1]heptanes: syntheses and nicotinic acetylcholine receptor agonist activity of potent pyridazine analogues of (+/-)-epibatidine. |
| AID146455 | Binding affinity at rat brain Nicotinic acetylcholine receptor alpha4-beta2 | 2002 | Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15 | Synthesis and pharmacological characterization of novel analogues of the nicotinic acetylcholine receptor agonist (+/-)-UB-165. |
| AID242894 | Maximal response against Nicotinic acetylcholine receptor alpha4-beta2 expressed in HEK293 cells | 2005 | Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15 | Neuronal nicotinic acetylcholine receptors: structural revelations, target identifications, and therapeutic inspirations. |
| AID375127 | Binding affinity to Aplysia californica AchBP M116Y, Y195F mutant expressed in HEK293S cells assessed as specific photoincorporation at 46 pmol by scintillation counting relative to wild type | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID132953 | Compound was evaluated for the analgesic activity by mouse hotplate assay at the dose 0.1; No significant effect observed at the doses tested | 1998 | Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4 | Identification and initial structure-activity relationships of (R)-5-(2-azetidinylmethoxy)-2-chloropyridine (ABT-594), a potent, orally active, non-opiate analgesic agent acting via neuronal nicotinic acetylcholine receptors. |
| AID254464 | In vitro binding affinity towards rat Nicotinic acetylcholine receptor alpha3-beta4 using 0.5 nM [3H]epibatidine | 2005 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 15, Issue:19 | Epibatidine analogues as selective ligands for the alpha(x)beta2-containing subtypes of nicotinic acetylcholine receptors. |
| AID409996 | Displacement of [3H]epibatine from nAChR in rat cortical membrane | 2008 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 18, Issue:23 | New synthesis and evaluation of enantiomers of 7-methyl-2-exo-(3'-iodo-5'-pyridinyl)-7-azabicyclo[2.2.1]heptane as stereoselective ligands for PET imaging of nicotinic acetylcholine receptors. |
| AID146000 | Tested for binding affinity against Nicotinic acetylcholine receptor alpha3-beta2 | 2003 | Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6 | Synthesis, nicotinic acetylcholine receptor binding affinities, and molecular modeling of constrained epibatidine analogues. |
| AID291933 | Displacement of [3H]cytisine from alpha-4-beta-2 in rat cerebral cortical membrane | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15 | Structure-activity studies and analgesic efficacy of N-(3-pyridinyl)-bridged bicyclic diamines, exceptionally potent agonists at nicotinic acetylcholine receptors. |
| AID1682123 | Potency index, ratio of nicotine IC50 to test compound IC50 for displacement of [3H]cytisine from rat brain nAChR using radiolabelled compound | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Pyridine alkaloids with activity in the central nervous system. |
| AID375113 | Binding affinity to Aplysia californica AchBP M116L,Y195F mutant expressed in HEK293S cells assessed as specific photoincorporation at 46 pmol by scintillation counting relative to wild type | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID374852 | Binding affinity to Aplysia californica AchBP S114M mutant expressed in HEK293S cells by scintillation proximity assay | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID129320 | Antinociceptive activity was tested in the mouse tail-flick test | 2004 | Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8 | Epibatidine structure-activity relationships. |
| AID145981 | Binding affinity towards nicotinic acetylcholine receptor alpha2-beta2 using [3H]epibatidine | 2004 | Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8 | Synthesis and pharmacological characterization of bivalent ligands of epibatidine at neuronal nicotinic acetylcholine receptors. |
| AID397991 | Selectivity ratio of Ki for alpha7 nicotinic acetylcholine receptor to Ki for alpha4beta2 nicotinic acetylcholine receptor in rat brain minus cerebellum membrane | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Octahydropyrrolo[3,4-c]pyrrole: a diamine scaffold for construction of either alpha4beta2 or alpha7-selective nicotinic acetylcholine receptor (nAChR) ligands. Substitutions that switch subtype selectivity. |
| AID322334 | Antinociceptive activity in sc dosed acute pain mouse model by tail flick method | 2008 | Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2 | Synthesis, nicotinic acetylcholine receptor binding, and pharmacological properties of 3'-(substituted phenyl)deschloroepibatidine analogs. |
| AID132751 | In vivo analgesic agonist activity after subcutaneous administration, using tail-flick assay | 2002 | Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14 | Synthesis and biological evaluation at nicotinic acetylcholine receptors of N-arylalkyl- and N-aryl-7-azabicyclo[2.2.1]heptanes. |
| AID243385 | Binding affinity (Ki) for rat nicotinic acetylcholine receptor alpha3-beta4 subunits versus 0.5 nM [3H](1)-epibatidine | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4 | Halogenated and isosteric cytisine derivatives with increased affinity and functional activity at nicotinic acetylcholine receptors. |
| AID146159 | Binding affinity at rat brain Nicotinic acetylcholine receptor alpha3-beta4 | 2002 | Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15 | Synthesis and pharmacological characterization of novel analogues of the nicotinic acetylcholine receptor agonist (+/-)-UB-165. |
| AID146462 | Tested for binding affinity against Nicotinic acetylcholine receptor alpha4-beta2 | 2003 | Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6 | Synthesis, nicotinic acetylcholine receptor binding affinities, and molecular modeling of constrained epibatidine analogues. |
| AID374832 | Binding affinity to Aplysia californica AchBP Y195F mutant expressed in HEK293S cells by scintillation proximity assay | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID145845 | Agonist activity against Nicotinic acetylcholine receptor (nAchR) | 1999 | Journal of medicinal chemistry, May-06, Volume: 42, Issue:9 | Emerging molecular approaches to pain therapy. |
| AID341258 | Displacement of [3H]epibatidine from rat alpha4beta2 nAChR expressed in HEK293 cells | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Discovery of (-)-7-methyl-2-exo-[3'-(6-[18F]fluoropyridin-2-yl)-5'-pyridinyl]-7-azabicyclo[2.2.1]heptane, a radiolabeled antagonist for cerebral nicotinic acetylcholine receptor (alpha4beta2-nAChR) with optimal positron emission tomography imaging propert |
| AID254461 | In vitro binding affinity towards rat Nicotinic acetylcholine receptor alpha2-beta2 using 0.5 nM [3H]epibatidine | 2005 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 15, Issue:19 | Epibatidine analogues as selective ligands for the alpha(x)beta2-containing subtypes of nicotinic acetylcholine receptors. |
| AID264239 | Displacement of [3H]epibatidine from rat alpha-4-beta-4 nACHR expressed in human HEK293 cells | 2006 | Journal of medicinal chemistry, May-04, Volume: 49, Issue:9 | Synthesis and pharmacological evaluation of novel 9- and 10-substituted cytisine derivatives. Nicotinic ligands of enhanced subtype selectivity. |
| AID242892 | Maximal response against Nicotinic acetylcholine receptor alpha3-beta2 expressed in HEK293 cells | 2005 | Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15 | Neuronal nicotinic acetylcholine receptors: structural revelations, target identifications, and therapeutic inspirations. |
| AID452524 | Displacement of [3H]585539 from alpha7 nAChR in rat brain | 2010 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1 | Structure-activity relationships of N-substituted ligands for the alpha7 nicotinic acetylcholine receptor. |
| AID1682334 | Displacement of [125I]alpha-bungarotoxin from human alpha7 nAChR expressed in K28 cell membrane | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Pyridine alkaloids with activity in the central nervous system. |
| AID116105 | Maximal nontoxic dose of the compound, done on mouse; sc | 1998 | Journal of medicinal chemistry, Feb-26, Volume: 41, Issue:5 | Mono- and disubstituted-3,8-diazabicyclo[3.2.1]octane derivatives as analgesics structurally related to epibatidine: synthesis, activity, and modeling. |
| AID243384 | Binding affinity (Ki) for rat brain nicotinic receptors ganglionic-type alpha-4 and beta2 subunits versus 0.5 nM [3H](1)-epibatidine | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4 | Halogenated and isosteric cytisine derivatives with increased affinity and functional activity at nicotinic acetylcholine receptors. |
| AID175480 | Compound was evaluated for functional potencies and efficacies at rat nAChR subtype DA release | 1997 | Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26 | Neuronal nicotinic acetylcholine receptors as targets for drug discovery. |
| AID146798 | Functional potency for Nicotinic acetylcholine receptor alpha-7 (rat brain) | 1997 | Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26 | Neuronal nicotinic acetylcholine receptors as targets for drug discovery. |
| AID374871 | Binding affinity to Aplysia californica AchBP M116L,Y195F mutant expressed in HEK293S cells assessed as specific photoincorporation at 46 pmol by scintillation counting | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID427654 | Displacement of [3H]epibatidine from rat alpha4beta4 nicotinic receptor expressed in human HEK293 cells by liquid scintillation counting | 2009 | Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13 | Synthesis and biological evaluation of novel carbon-11 labeled pyridyl ethers: candidate ligands for in vivo imaging of alpha4beta2 nicotinic acetylcholine receptors (alpha4beta2-nAChRs) in the brain with positron emission tomography. |
| AID1410559 | Toxicity in iv dosed Swiss-Webster mouse | 2018 | Journal of natural products, 04-27, Volume: 81, Issue:4 | Absolute Configuration and Pharmacology of the Poison Frog Alkaloid Phantasmidine. |
| AID1074597 | Effect on spontaneous activity in sc dosed mouse after 5 mins | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3 | Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2'-fluoro-3'-(substituted pyridinyl)-7-deschloroepibatidine analogues. |
| AID1410543 | Agonist activity at rat alpha3beta4 nAChR by cell-based rubidium flux assay relative to 100 uM nicotine | 2018 | Journal of natural products, 04-27, Volume: 81, Issue:4 | Absolute Configuration and Pharmacology of the Poison Frog Alkaloid Phantasmidine. |
| AID1410546 | Selectivity ratio of EC50 for agonist activity at rat alpha3beta4 nAChR (unknown origin) to EC50 for agonist activity at alpha4beta2 nAChR (unknown origin) | 2018 | Journal of natural products, 04-27, Volume: 81, Issue:4 | Absolute Configuration and Pharmacology of the Poison Frog Alkaloid Phantasmidine. |
| AID146164 | Functional potency measured as maximum stimulation at rat Nicotinic acetylcholine receptor alpha3-beta4 expressed in Xenopus oocytes | 2004 | Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8 | Epibatidine structure-activity relationships. |
| AID1074610 | Antagonist activity at rat alpha4beta2 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of acetylcholine-induced current at 100 uM by two-electrode voltage clamp electrophysiological analysis relative to acetylcholine | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3 | Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2'-fluoro-3'-(substituted pyridinyl)-7-deschloroepibatidine analogues. |
| AID374886 | Binding affinity to Aplysia californica AchBP M116L mutant expressed in HEK293S cells assessed as specific photoincorporation at 46 pmol by scintillation counting relative to wild type | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID146620 | Inhibition of [3H]nicotine binding to Nicotinic acetylcholine receptor alpha4-beta2 from rat membranes | 2004 | Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8 | Epibatidine structure-activity relationships. |
| AID145356 | Compound was evaluated for functional potencies and efficacies at human Nicotinic acetylcholine receptor subtype IMR-32 (ganglionic) | 1997 | Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26 | Neuronal nicotinic acetylcholine receptors as targets for drug discovery. |
| AID146452 | Tested for binding affinity against Nicotinic acetylcholine receptor alpha4-beta2 | 2003 | Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6 | Synthesis, nicotinic acetylcholine receptor binding affinities, and molecular modeling of constrained epibatidine analogues. |
| AID374840 | Binding affinity to Aplysia californica AchBP A107M mutant expressed in HEK293S cells by scintillation proximity assay | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Nicotinic agonist binding site mapped by methionine- and tyrosine-scanning coupled with azidochloropyridinyl photoaffinity labeling. |
| AID588519 | A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities | 2011 | Antiviral research, Sep, Volume: 91, Issue:3 | High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors. |
| AID540299 | A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis | 2010 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21 | Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis. |
| AID1799850 | Interaction Assay from Article 10.1021/bi1006354: \\Interaction kinetic and structural dynamic analysis of ligand binding to acetylcholine-binding protein.\\ | 2010 | Biochemistry, Sep-21, Volume: 49, Issue:37 | Interaction kinetic and structural dynamic analysis of ligand binding to acetylcholine-binding protein. |
| AID1799761 | Radioligand Competition Assay from Article 10.1074/jbc.M111.292243: \\Intersubunit bridge formation governs agonist efficacy at nicotinic acetylcholine u00CEu00B14u00CEu00B22 receptors: unique role of halogen bonding revealed.\\ | 2012 | The Journal of biological chemistry, Feb-03, Volume: 287, Issue:6 | Intersubunit bridge formation governs agonist efficacy at nicotinic acetylcholine α4β2 receptors: unique role of halogen bonding revealed. |
| AID239319 | Inhibition of alpha beta[3H]epibatidine binding to Nicotinic acetylcholine receptor alpha4-beta2 of rat cerebral cortex | 2004 | Journal of medicinal chemistry, Aug-26, Volume: 47, Issue:18 | Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2'-fluoro-3'-(substituted phenyl)deschloroepibatidine analogues. Novel nicotinic antagonist. |
| AID265650 | Hypothermia in mouse | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11 | Synthesis and pharmacological characterization of nicotinic acetylcholine receptor properties of (+)- and (-)-pyrido-[3,4-b]homotropanes. |
| AID129323 | Antinociceptive activity was tested in the mouse tail-flick test from ref 17 | 2004 | Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8 | Epibatidine structure-activity relationships. |
| AID1275134 | Binding affinity to alpha4beta2 nACh receptor (unknown origin) expressed in Xenopus oocytes | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Modification of the anabaseine pyridine nucleus allows achieving binding and functional selectivity for the α3β4 nicotinic acetylcholine receptor subtype. |
| AID246832 | Antinociceptive response was determined in mice using hypothermia method | 2004 | Journal of medicinal chemistry, Aug-26, Volume: 47, Issue:18 | Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2'-fluoro-3'-(substituted phenyl)deschloroepibatidine analogues. Novel nicotinic antagonist. |
| AID1275131 | Selectivity ratio of Ki for rat alpha4beta2 nACh receptor to Ki for human alpha3beta4 nACh receptor | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Modification of the anabaseine pyridine nucleus allows achieving binding and functional selectivity for the α3β4 nicotinic acetylcholine receptor subtype. |
| AID1563867 | Displacement of [3H]epibatidine from human alpha3beta4 nAChR transfected in HEK243 cell membrane | |||
| AID265653 | Spontaneous activity in mouse | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11 | Synthesis and pharmacological characterization of nicotinic acetylcholine receptor properties of (+)- and (-)-pyrido-[3,4-b]homotropanes. |
| AID1739243 | Displacement of [125I] alpha bungarotoxin from human neuronal alpha7 nAChR expressed in human SH-SY5Y cell membrane measured after 120 mins by Topcount scintillation counting method | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Optical control of muscular nicotinic channels with azocuroniums, photoswitchable azobenzenes bearing two N-methyl-N-carbocyclic quaternary ammonium groups. |
| AID1275129 | Displacement of [125I] alpha bungarotoxin from rat alpha7 nACh receptor expressed in rat hippocampal membrane preincubated for 30 mins followed by radioligand addition by gamma counting analysis | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Modification of the anabaseine pyridine nucleus allows achieving binding and functional selectivity for the α3β4 nicotinic acetylcholine receptor subtype. |
| AID129322 | Antinociceptive activity was tested in the mouse tail-flick test from ref 15 | 2004 | Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8 | Epibatidine structure-activity relationships. |
| AID1275132 | Selectivity ratio of Ki for rat alpha7 nACh receptor to Ki for human alpha3beta4 nACh receptor | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Modification of the anabaseine pyridine nucleus allows achieving binding and functional selectivity for the α3β4 nicotinic acetylcholine receptor subtype. |
| AID265642 | Antinociceptive activity in mouse by tail flick assay | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11 | Synthesis and pharmacological characterization of nicotinic acetylcholine receptor properties of (+)- and (-)-pyrido-[3,4-b]homotropanes. |
| AID129320 | Antinociceptive activity was tested in the mouse tail-flick test | 2004 | Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8 | Epibatidine structure-activity relationships. |
| AID1563865 | Displacement of [125I]alpha-bungarotoxin from alpha7nAChR in rat hippocampus membrane | |||
| AID1102410 | Displacement of [3HIMI from nicotinic acetylcholine receptor in Musca domestica (house fly) head membranes incubated for 60 min by liquid scintillation counting method | 2003 | Bioscience, biotechnology, and biochemistry, May, Volume: 67, Issue:5 | Asymmetric chloronicotinyl insecticide, 1-[1-(6-chloro-3-pyridyl)ethyl]-2-nitroiminoimidazolidine: preparation, resolution and biological activities toward insects and their nerve preparations. |
| AID225733 | Inhibition of [3H]nicotine binding to Nicotinic acetylcholine receptor alpha4-beta2 from rat membranes from ref 15 | 2004 | Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8 | Epibatidine structure-activity relationships. |
| AID35535 | Inhibition of [3H]epibatidine binding at the alpha beta nicotinic AChR in male rat cerebral cortex | 2001 | Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24 | Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2-exo-2-(2'-substituted-3'-phenyl-5'-pyridinyl)-7-azabicyclo[2.2.1]heptanes. Novel nicotinic antagonist. |
| AID276254 | Displacement of [3H]Nicotine from alpha4beta2 nAChR in rat cortical membranes | 2006 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21 | Epibatidine isomers and analogues: structure-activity relationships. |
| AID1739245 | Displacement of [125I] alpha bungarotoxin from human neuronal alpha4beta2 nAChR expressed in human SH-SY5Y cell membrane measured after 120 mins by Topcount scintillation counting method | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Optical control of muscular nicotinic channels with azocuroniums, photoswitchable azobenzenes bearing two N-methyl-N-carbocyclic quaternary ammonium groups. |
| AID276256 | Selectivity for rat alpha4beta2 nAChR over rat alpha-7 nAChR | 2006 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21 | Epibatidine isomers and analogues: structure-activity relationships. |
| AID265641 | Displacement of [3H]epibatidine from alpha-4-beta-2 nACHR in rat cerebral cortex | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11 | Synthesis and pharmacological characterization of nicotinic acetylcholine receptor properties of (+)- and (-)-pyrido-[3,4-b]homotropanes. |
| AID146621 | Inhibition of [3H]nicotine binding to Nicotinic acetylcholine receptor alpha4-beta2 from rat membranes from ref 14 | 2004 | Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8 | Epibatidine structure-activity relationships. |
| AID146620 | Inhibition of [3H]nicotine binding to Nicotinic acetylcholine receptor alpha4-beta2 from rat membranes | 2004 | Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8 | Epibatidine structure-activity relationships. |
| AID265646 | Antinociceptive activity in sc dosed mouse by hot plate assay after 5 mins | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11 | Synthesis and pharmacological characterization of nicotinic acetylcholine receptor properties of (+)- and (-)-pyrido-[3,4-b]homotropanes. |
| AID129297 | Antinociception by tail-flick test in male ICR mice after intrathecal (i.t.) injection | 2001 | Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13 | Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2-exo-2-(2'-substituted 5'-pyridinyl)-7-azabicyclo[2.2.1]heptanes. Epibatidine analogues. |
| AID276255 | Displacement of [125I-alpha]-Bungarotoxin from alpha-7 nAChR in rat hippocampal membranes | 2006 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21 | Epibatidine isomers and analogues: structure-activity relationships. |
| AID1739244 | Displacement of [125I] alpha bungarotoxin from human muscle type nAChR expressed in human TE-671 cell membrane measured after 120 mins by Topcount scintillation counting method | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Optical control of muscular nicotinic channels with azocuroniums, photoswitchable azobenzenes bearing two N-methyl-N-carbocyclic quaternary ammonium groups. |
| AID146476 | Non-specific binding in presence of 300 uM nicotine at nicotinic acetylcholine receptor alpha4-beta2 in rat cerebral cortex membranes | 2001 | Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13 | Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2-exo-2-(2'-substituted 5'-pyridinyl)-7-azabicyclo[2.2.1]heptanes. Epibatidine analogues. |
| AID239201 | Inhibition of [125I]-iodo-MLA binding to Nicotinic acetylcholine receptor alpha-7 of rat cerebral cortex | 2004 | Journal of medicinal chemistry, Aug-26, Volume: 47, Issue:18 | Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2'-fluoro-3'-(substituted phenyl)deschloroepibatidine analogues. Novel nicotinic antagonist. |
| AID131354 | Drug discrimination in mice from ref 15 | 2004 | Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8 | Epibatidine structure-activity relationships. |
| AID1275130 | Displacement of [125I] alpha bungarotoxin from human alpha7 nACh receptor incubated for 20 secs | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Modification of the anabaseine pyridine nucleus allows achieving binding and functional selectivity for the α3β4 nicotinic acetylcholine receptor subtype. |
| AID131576 | Spontaneous activity in mice from ref 15 | 2004 | Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8 | Epibatidine structure-activity relationships. |
| AID129318 | Antinociceptive activity was tested in the mouse hot plate test | 2004 | Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8 | Epibatidine structure-activity relationships. |
| AID1275133 | Binding affinity to alpha3beta4 nACh receptor (unknown origin) expressed in Xenopus oocytes | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Modification of the anabaseine pyridine nucleus allows achieving binding and functional selectivity for the α3β4 nicotinic acetylcholine receptor subtype. |
| AID1563864 | Displacement of [3H]epibatidine from alpha4beta2 nAChR in rat cerebral cortex membrane | |||
| AID146473 | Inhibition of [3H]epibatidine binding at the nicotinic acetylcholine receptor alpha4-beta2 in male rat cerebral cortex | 2001 | Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13 | Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2-exo-2-(2'-substituted 5'-pyridinyl)-7-azabicyclo[2.2.1]heptanes. Epibatidine analogues. |
| AID246831 | Antinociceptive response was determined in mice using tail flick method | 2004 | Journal of medicinal chemistry, Aug-26, Volume: 47, Issue:18 | Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2'-fluoro-3'-(substituted phenyl)deschloroepibatidine analogues. Novel nicotinic antagonist. |
| AID146618 | Inhibition of [3H]epibatidine binding to Nicotinic acetylcholine receptor alpha4-beta2 from rat membranes from ref 16 | 2004 | Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8 | Epibatidine structure-activity relationships. |
| AID146941 | Inhibition of [125I]MLA binding to Nicotinic acetylcholine receptor alpha7 from rat brain membranes | 2004 | Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8 | Epibatidine structure-activity relationships. |
| AID226647 | Hill slope value of the compound | 2001 | Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13 | Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2-exo-2-(2'-substituted 5'-pyridinyl)-7-azabicyclo[2.2.1]heptanes. Epibatidine analogues. |
| AID246838 | Antinociceptive response was determined in mice using hot plate flick method | 2004 | Journal of medicinal chemistry, Aug-26, Volume: 47, Issue:18 | Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2'-fluoro-3'-(substituted phenyl)deschloroepibatidine analogues. Novel nicotinic 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 | 0 (0.00) | 18.7374 |
| 1990's | 124 (19.47) | 18.2507 |
| 2000's | 363 (56.99) | 29.6817 |
| 2010's | 141 (22.14) | 24.3611 |
| 2020's | 9 (1.41) | 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 strong demand-to-supply ratio for research on this compound.
| This Compound (45.04) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Trials | 0 (0.00%) | 5.53% |
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 22 (3.71%) | 6.00% |
| Reviews | 5 (7.14%) | 6.00% |
| Reviews | 1 (8.33%) | 6.00% |
| Case Studies | 2 (0.34%) | 4.05% |
| Case Studies | 0 (0.00%) | 4.05% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Observational | 0 (0.00%) | 0.25% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 569 (95.95%) | 84.16% |
| Other | 65 (92.86%) | 84.16% |
| Other | 11 (91.67%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||