Target Information
| Target General Information | Top | |||||
|---|---|---|---|---|---|---|
| Target ID |
T34429
(Former ID: TTDS00520)
|
|||||
| Target Name |
Neuronal acetylcholine receptor alpha-7 (CHRNA7)
|
|||||
| Synonyms |
Nicotinic acetylcholine receptor subunit alpha 7; Nicotinic acetylcholine receptor alpha7; CHRNA7; Alpha7 nicotinic receptor; Alpha7 nAChR; Alpha-7 nAChR; Alpha(7) nicotinic receptor
Click to Show/Hide
|
|||||
| Gene Name |
CHRNA7
|
|||||
| Target Type |
Successful target
|
[1] | ||||
| Disease | [+] 2 Target-related Diseases | + | ||||
| 1 | Corneal disease [ICD-11: 9A76-9A78] | |||||
| 2 | Schizophrenia [ICD-11: 6A20] | |||||
| Function |
After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane. The channel is blocked by alpha-bungarotoxin.
Click to Show/Hide
|
|||||
| BioChemical Class |
Neurotransmitter receptor
|
|||||
| UniProt ID | ||||||
| Sequence |
MRCSPGGVWLALAASLLHVSLQGEFQRKLYKELVKNYNPLERPVANDSQPLTVYFSLSLL
QIMDVDEKNQVLTTNIWLQMSWTDHYLQWNVSEYPGVKTVRFPDGQIWKPDILLYNSADE RFDATFHTNVLVNSSGHCQYLPPGIFKSSCYIDVRWFPFDVQHCKLKFGSWSYGGWSLDL QMQEADISGYIPNGEWDLVGIPGKRSERFYECCKEPYPDVTFTVTMRRRTLYYGLNLLIP CVLISALALLVFLLPADSGEKISLGITVLLSLTVFMLLVAEIMPATSDSVPLIAQYFAST MIIVGLSVVVTVIVLQYHHHDPDGGKMPKWTRVILLNWCAWFLRMKRPGEDKVRPACQHK QRRCSLASVEMSAVAPPPASNGNLLYIGFRGLDGVHCVPTPDSGVVCGRMACSPTHDEHL LHGGQPPEGDPDLAKILEEVRYIANRFRCQDESEAVCSEWKFAACVVDRLCLMAFSVFTI ICTIGILMSAPNFVEAVSKDFA Click to Show/Hide
|
|||||
| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| HIT2.0 ID | T34I45 | |||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 2 Approved Drugs | + | ||||
| 1 | ALCURONIUM | Drug Info | Approved | Anaesthesia | [2], [3] | |
| 2 | Ziprasidone | Drug Info | Approved | Schizophrenia | [1], [4], [5] | |
| Clinical Trial Drug(s) | [+] 14 Clinical Trial Drugs | + | ||||
| 1 | AMG 386 | Drug Info | Phase 3 | Neuropathic pain | [6] | |
| 2 | CYTISINE | Drug Info | Phase 3 | Tobacco dependence | [7] | |
| 3 | EVP-6124 | Drug Info | Phase 3 | Schizophrenia | [8] | |
| 4 | ABT-126 | Drug Info | Phase 2 | Schizophrenia | [9] | |
| 5 | AQW-051 | Drug Info | Phase 2 | Alzheimer disease | [10], [11] | |
| 6 | Bradanicline | Drug Info | Phase 2 | Chronic cough | [12] | |
| 7 | GTS-21 | Drug Info | Phase 2 | Parkinson disease | [13] | |
| 8 | JNJ-39393406 | Drug Info | Phase 2 | Depression | [7] | |
| 9 | MEM-3454 | Drug Info | Phase 2 | Schizophrenia | [1] | |
| 10 | TC-6987 | Drug Info | Phase 2 | Asthma | [14] | |
| 11 | AVL-3288 | Drug Info | Phase 1 | Cognitive impairment | [15] | |
| 12 | BMS-933043 | Drug Info | Phase 1 | Psychiatric disorder | [16] | |
| 13 | BNC375 | Drug Info | Phase 1 | Cognitive impairment | [17], [18] | |
| 14 | R4996 | Drug Info | Phase 1 | Neurological disorder | [19] | |
| Discontinued Drug(s) | [+] 4 Discontinued Drugs | + | ||||
| 1 | AZD-9684 | Drug Info | Discontinued in Phase 2 | Thrombosis | [20] | |
| 2 | AZD0328 | Drug Info | Discontinued in Phase 2 | Alzheimer disease | [21], [22] | |
| 3 | ABT-107 | Drug Info | Discontinued in Phase 1 | Attention deficit hyperactivity disorder | [23] | |
| 4 | PNU-282987 | Drug Info | Terminated | Schizophrenia | [25], [1] | |
| Preclinical Drug(s) | [+] 2 Preclinical Drugs | + | ||||
| 1 | PHA-568487 | Drug Info | Preclinical | Cognitive impairment | [24] | |
| 2 | RMG-40083 | Drug Info | Preclinical | Schizophrenia | [1] | |
| Mode of Action | [+] 6 Modes of Action | + | ||||
| Inhibitor | [+] 9 Inhibitor drugs | + | ||||
| 1 | ALCURONIUM | Drug Info | [26] | |||
| 2 | CYTISINE | Drug Info | [28] | |||
| 3 | 3,8-dibromoboldine | Drug Info | [43] | |||
| 4 | 3-bromoboldine | Drug Info | [43] | |||
| 5 | CP-810123 | Drug Info | [49] | |||
| 6 | GCCSHPACAGNNQHIC* | Drug Info | [50] | |||
| 7 | GCCSNPVCHLEHSNLC* | Drug Info | [50] | |||
| 8 | PH-709829 | Drug Info | [53] | |||
| 9 | TOXIFERINE | Drug Info | [26] | |||
| Binder | [+] 1 Binder drugs | + | ||||
| 1 | Ziprasidone | Drug Info | [1] | |||
| Agonist | [+] 15 Agonist drugs | + | ||||
| 1 | AMG 386 | Drug Info | [27] | |||
| 2 | AQW-051 | Drug Info | [31] | |||
| 3 | Bradanicline | Drug Info | [32] | |||
| 4 | GTS-21 | Drug Info | [33], [34] | |||
| 5 | R4996 | Drug Info | [27] | |||
| 6 | PHA-568487 | Drug Info | [42] | |||
| 7 | 4BP-TQS | Drug Info | [44] | |||
| 8 | A-582941 | Drug Info | [45] | |||
| 9 | AZD-6319 | Drug Info | [47] | |||
| 10 | EVP-4473 | Drug Info | [47] | |||
| 11 | JN-711 | Drug Info | [47] | |||
| 12 | PSAB-OFP | Drug Info | [55] | |||
| 13 | [125I]epibatidine | Drug Info | [47] | |||
| 14 | [3H]A-585539 | Drug Info | [56] | |||
| 15 | [3H]AZ11637326 | Drug Info | [57] | |||
| Modulator | [+] 11 Modulator drugs | + | ||||
| 1 | EVP-6124 | Drug Info | [29] | |||
| 2 | ABT-126 | Drug Info | [30] | |||
| 3 | JNJ-39393406 | Drug Info | [35] | |||
| 4 | TC-6987 | Drug Info | [36] | |||
| 5 | AVL-3288 | Drug Info | [37] | |||
| 6 | BMS-933043 | Drug Info | [38] | |||
| 7 | BNC375 | Drug Info | [17] | |||
| 8 | AZD0328 | Drug Info | [40] | |||
| 9 | ABT-107 | Drug Info | [41] | |||
| 10 | JNJ-1930942 | Drug Info | [47] | |||
| 11 | PheTQS | Drug Info | [47] | |||
| Antagonist | [+] 6 Antagonist drugs | + | ||||
| 1 | MEM-3454 | Drug Info | [1] | |||
| 2 | AZD-9684 | Drug Info | [39] | |||
| 3 | RMG-40083 | Drug Info | [1] | |||
| 4 | PNU-282987 | Drug Info | [1] | |||
| 5 | Barbituric acid derivative | Drug Info | [48] | |||
| 6 | [3H]methyllycaconitine | Drug Info | [47], [58], [59] | |||
| Modulator (allosteric modulator) | [+] 4 Modulator (allosteric modulator) drugs | + | ||||
| 1 | A-867744 | Drug Info | [46] | |||
| 2 | LY2087101 | Drug Info | [51] | |||
| 3 | NS1738 | Drug Info | [52] | |||
| 4 | PNU-120596 | Drug Info | [54] | |||
| Cell-based Target Expression Variations | Top | |||||
|---|---|---|---|---|---|---|
| Cell-based Target Expression Variations | ||||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| Ligand Name: EVP-6124 | Ligand Info | |||||
| Structure Description | human alpha 7 nicotinic acetylcholine receptor bound to EVP-6124 | PDB:7EKP | ||||
| Method | Electron microscopy | Resolution | 2.85 Å | Mutation | No | [60] |
| PDB Sequence |
GEFQRKLYKE
32 LVKNYNPLER42 PVANDSQPLT52 VYFSLSLLQI62 MDVDEKNQVL72 TTNIWLQMSW 82 TDHYLQWNVS92 EYPGVKTVRF102 PDGQIWKPDI112 LLYNSADERF122 DATFHTNVLV 132 NSSGHCQYLP142 PGIFKSSCYI152 DVRWFPFDVQ162 HCKLKFGSWS172 YGGWSLDLQM 182 QEADISGYIP192 NGEWDLVGIP202 GKRSERFYEC212 CKEPYPDVTF222 TVTMRRRTLY 232 YGLNLLIPCV242 LISALALLVF252 LLPADSGEKI262 SLGITVLLSL272 TVFMLLVAEI 282 MPATSDSVPL292 IAQYFASTMI302 IVGLSVVVTV312 IVLQYHHHDP322 DGGKMPKWTR 332 VILLNWCAWF342 LRMKRDLAKI436 LEEVRYIANR446 FRCQDESEAV456 CSEWKFAACV 466 VDRLCLMAFS476 VFTIICTIGI486 LMSAPNFVEA496 VSKDFA
|
|||||
|
|
||||||
| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| Ligand Name: Cholesterol | Ligand Info | |||||
| Structure Description | human alpha 7 nicotinic acetylcholine receptor bound to EVP-6124 | PDB:7EKP | ||||
| Method | Electron microscopy | Resolution | 2.85 Å | Mutation | No | [60] |
| PDB Sequence |
GEFQRKLYKE
32 LVKNYNPLER42 PVANDSQPLT52 VYFSLSLLQI62 MDVDEKNQVL72 TTNIWLQMSW 82 TDHYLQWNVS92 EYPGVKTVRF102 PDGQIWKPDI112 LLYNSADERF122 DATFHTNVLV 132 NSSGHCQYLP142 PGIFKSSCYI152 DVRWFPFDVQ162 HCKLKFGSWS172 YGGWSLDLQM 182 QEADISGYIP192 NGEWDLVGIP202 GKRSERFYEC212 CKEPYPDVTF222 TVTMRRRTLY 232 YGLNLLIPCV242 LISALALLVF252 LLPADSGEKI262 SLGITVLLSL272 TVFMLLVAEI 282 MPATSDSVPL292 IAQYFASTMI302 IVGLSVVVTV312 IVLQYHHHDP322 DGGKMPKWTR 332 VILLNWCAWF342 LRMKRDLAKI436 LEEVRYIANR446 FRCQDESEAV456 CSEWKFAACV 466 VDRLCLMAFS476 VFTIICTIGI486 LMSAPNFVEA496 VSKDFA
|
|||||
|
|
||||||
| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| Click to View More Binding Site Information of This Target with Different Ligands | ||||||
| Different Human System Profiles of Target | Top |
|---|---|
|
Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Pathway Affiliation
of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function.
Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes
(Pharmacol Rev, 58: 259-279, 2006).
Human Similarity Proteins
Human Pathway Affiliation
|
|
|
There is no similarity protein (E value < 0.005) for this target
|
| KEGG Pathway | Pathway ID | Affiliated Target | Pathway Map |
|---|---|---|---|
| Calcium signaling pathway | hsa04020 | Affiliated Target |
|
| Class: Environmental Information Processing => Signal transduction | Pathway Hierarchy | ||
| Neuroactive ligand-receptor interaction | hsa04080 | Affiliated Target |
|
| Class: Environmental Information Processing => Signaling molecules and interaction | Pathway Hierarchy | ||
| Cholinergic synapse | hsa04725 | Affiliated Target |
|
| Class: Organismal Systems => Nervous system | Pathway Hierarchy | ||
| Chemical Structure based Activity Landscape of Target | Top |
|---|---|
| Drug Property Profile of Target | Top | |
|---|---|---|
| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
|
|
||
| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
|
|
||
| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
|
|
||
| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Co-Targets | Top | |||||
|---|---|---|---|---|---|---|
| Co-Targets | ||||||
| Target Poor or Non Binders | Top | |||||
|---|---|---|---|---|---|---|
| Target Poor or Non Binders | ||||||
| Target Affiliated Biological Pathways | Top | |||||
|---|---|---|---|---|---|---|
| KEGG Pathway | [+] 5 KEGG Pathways | + | ||||
| 1 | Calcium signaling pathway | |||||
| 2 | Neuroactive ligand-receptor interaction | |||||
| 3 | Cholinergic synapse | |||||
| 4 | Nicotine addiction | |||||
| 5 | Chemical carcinogenesis | |||||
| Panther Pathway | [+] 2 Panther Pathways | + | ||||
| 1 | Alzheimer disease-amyloid secretase pathway | |||||
| 2 | Nicotinic acetylcholine receptor signaling pathway | |||||
| Reactome | [+] 1 Reactome Pathways | + | ||||
| 1 | Highly calcium permeable postsynaptic nicotinic acetylcholine receptors | |||||
| WikiPathways | [+] 2 WikiPathways | + | ||||
| 1 | SIDS Susceptibility Pathways | |||||
| 2 | Neurotransmitter Receptor Binding And Downstream Transmission In The Postsynaptic Cell | |||||
| Target-Related Models and Studies | Top | |||||
|---|---|---|---|---|---|---|
| Target Validation | ||||||
| References | Top | |||||
|---|---|---|---|---|---|---|
| REF 1 | The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22. | |||||
| REF 2 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 341). | |||||
| REF 3 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| REF 4 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 59). | |||||
| REF 5 | Emerging anxiolytics. Expert Opin Emerg Drugs. 2007 Nov;12(4):541-54. | |||||
| REF 6 | Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26. | |||||
| REF 7 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 8 | ClinicalTrials.gov (NCT02004392) Study of the Safety and Clinical Effects of 2 Doses of EVP-6124 in Subjects With Alzheimer's Disease Who Complete Study EVP-6124-024 or EVP-6124-025. U.S. National Institutes of Health. | |||||
| REF 9 | ClinicalTrials.gov (NCT01655680) A Study to Evaluate ABT-126 for the Treatment of Cognitive Deficits in Schizophrenia. U.S. National Institutes of Health. | |||||
| REF 10 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7371). | |||||
| REF 11 | ClinicalTrials.gov (NCT01474421) Safety and Efficacy of AQW051 in L-dopa Induced Dyskinesias in Patients With Parkinson's Disease. U.S. National Institutes of Health. | |||||
| REF 12 | ClinicalTrials.gov (NCT03622216) A Dose Escalation Study to Assess the Efficacy and Safety of Bradanicline in Subjects With Refractory Chronic Cough. U.S.National Institutes of Health. | |||||
| REF 13 | ClinicalTrials.gov (NCT02432066) Effects of GTS-21 on Smoking Behavior and Neurocognitive Functions. U.S. National Institutes of Health. | |||||
| REF 14 | ClinicalTrials.gov (NCT01296087) TC-6987 for the Treatment of Mild to Moderate Asthma. U.S. National Institutes of Health. | |||||
| REF 15 | ClinicalTrials.gov (NCT01851603) Phase I Study to Evaluate the Safety and Pharmacokinetics of Oral Doses of Anvylic-3288 in Healthy Subjects. U.S. National Institutes of Health. | |||||
| REF 16 | ClinicalTrials.gov (NCT01605994) Multiple Ascending-Dose Study to Evaluate the Safety, Tolerability and Pharmacokinetics of BMS-933043 in Healthy Subjects. U.S. National Institutes of Health. | |||||
| REF 17 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 18 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 19 | Clinical pipeline report, company report or official report of Roche. | |||||
| REF 20 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018349) | |||||
| REF 21 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7697). | |||||
| REF 22 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018503) | |||||
| REF 23 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026401) | |||||
| REF 24 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018656) | |||||
| REF 25 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 3988). | |||||
| REF 26 | Pharmacological characteristics and binding modes of caracurine V analogues and related compounds at the neuronal alpha7 nicotinic acetylcholine re... J Med Chem. 2007 Sep 20;50(19):4616-29. | |||||
| REF 27 | Clinical pipeline report, company report or official report of Roche (2009). | |||||
| REF 28 | 3,5-Bicyclic aryl piperidines: a novel class of alpha4beta2 neuronal nicotinic receptor partial agonists for smoking cessation. Bioorg Med Chem Lett. 2005 Nov 15;15(22):4889-97. | |||||
| REF 29 | Normalizing effects of EVP-6124, an alpha-7 nicotinic partial agonist, on event-related potentials and cognition: a proof of concept, randomized trial in patients with schizophrenia. J Psychiatr Pract. 2014 Jan;20(1):12-24. | |||||
| REF 30 | A phase 2 randomized, controlled trial of the alpha7 agonist ABT-126 in mild-to-moderate Alzheimer's dementia. Alzheimer's & Dementia: Translational Research & Clinical Interventions Volume 1, Issue 1, June 2015, Pages 81-90. | |||||
| REF 31 | AQW051, a novel and selective nicotinic acetylcholine receptor alpha7 partial agonist, reduces l-Dopa-induced dyskinesias and extends the duration of l-Dopa effects in parkinsonian monkeys. Parkinsonism Relat Disord. 2014 Nov;20(11):1119-23. | |||||
| REF 32 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2023. Adis Insight | |||||
| REF 33 | The brain alpha7 nicotinic receptor may be an important therapeutic target for the treatment of Alzheimer's disease: studies with DMXBA (GTS-21). Behav Brain Res. 2000 Aug;113(1-2):169-81. | |||||
| REF 34 | Selective alpha7-nicotinic agonists normalize inhibition of auditory response in DBA mice. Psychopharmacology (Berl). 1998 Apr;136(4):320-7. | |||||
| REF 35 | Allosteric alpha-7 nicotinic receptor modulation and P50 sensory gating in schizophrenia: a proof-of-mechanism study. Neuropharmacology. 2013 Jan;64:197-204. | |||||
| REF 36 | ClinicalTrials.gov (NCT01293669) Glycemic Control, Safety and Tolerability of TC-6987 Monotherapy in Type 2 Diabetes Mellitus. U.S. National Institutes of Health. | |||||
| REF 37 | Differential immediate and sustained memory enhancing effects of alpha7 nicotinic receptor agonists and allosteric modulators in rats. PLoS One. 2011;6(11):e27014. | |||||
| REF 38 | Clinical pipeline report, company report or official report of Phrma.org Alzheimers 2012. | |||||
| REF 39 | Blockade and activation of the human neuronal nicotinic acetylcholine receptors by atracurium and laudanosine. Anesthesiology. 2001 Apr;94(4):643-51. | |||||
| REF 40 | Ultra-low exposure to -7 nicotinic acetylcholine receptor partial agonists elicits an improvement in cognition that corresponds with an increase in -7 receptor expression in rodents: implications for low dose clinical efficacy.Neuroscience.2011 Jul 14;186:76-87. | |||||
| REF 41 | In vitro pharmacological characterization of a novel selective alpha7 neuronal nicotinic acetylcholine receptor agonist ABT-107. J Pharmacol Exp Ther. 2010 Sep 1;334(3):863-74. | |||||
| REF 42 | Multiple species metabolism of PHA-568487, a selective alpha 7 nicotinic acetylcholine receptor agonist. Drug Metab Lett. 2010 Aug;4(3):162-72. | |||||
| REF 43 | Aporphine metho salts as neuronal nicotinic acetylcholine receptor blockers. Bioorg Med Chem. 2007 May 15;15(10):3368-72. | |||||
| REF 44 | Agonist activation of alpha7 nicotinic acetylcholine receptors via an allosteric transmembrane site. Proc Natl Acad Sci U S A. 2011 Apr 5;108(14):5867-72. | |||||
| REF 45 | Broad-spectrum efficacy across cognitive domains by alpha7 nicotinic acetylcholine receptor agonism correlates with activation of ERK1/2 and CREB phosphorylation pathways. J Neurosci. 2007 Sep 26;27(39):10578-87. | |||||
| REF 46 | In vitro pharmacological characterization of a novel allosteric modulator of alpha 7 neuronal acetylcholine receptor, 4-(5-(4-chlorophenyl)-2-methy... J Pharmacol Exp Ther. 2009 Jul;330(1):257-67. | |||||
| REF 47 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 468). | |||||
| REF 48 | Whiting PJ: The GABAA receptor gene family: new opportunities for drug development. Curr Opin Drug Discov Devel. 2003 Sep;6(5):648-57. | |||||
| REF 49 | Discovery of 4-(5-methyloxazolo[4,5-b]pyridin-2-yl)-1,4-diazabicyclo[3.2.2]nonane (CP-810,123), a novel alpha 7 nicotinic acetylcholine receptor ag... J Med Chem. 2010 Feb 11;53(3):1222-37. | |||||
| REF 50 | Neuronal nicotinic acetylcholine receptors: structural revelations, target identifications, and therapeutic inspirations. J Med Chem. 2005 Jul 28;48(15):4705-45. | |||||
| REF 51 | Identification and pharmacological profile of a new class of selective nicotinic acetylcholine receptor potentiators. J Pharmacol Exp Ther. 2006 Sep;318(3):1108-17. | |||||
| REF 52 | An allosteric modulator of the alpha7 nicotinic acetylcholine receptor possessing cognition-enhancing properties in vivo. J Pharmacol Exp Ther. 2007 Oct;323(1):294-307. | |||||
| REF 53 | Discovery of N-[(3R,5R)-1-azabicyclo[3.2.1]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide as an agonist of the alpha7 nicotinic acetylcholine receptor:... Bioorg Med Chem Lett. 2008 Jun 15;18(12):3611-5. | |||||
| REF 54 | A novel positive allosteric modulator of the alpha7 neuronal nicotinic acetylcholine receptor: in vitro and in vivo characterization. J Neurosci. 2005 Apr 27;25(17):4396-405. | |||||
| REF 55 | PSAB-OFP, a selective alpha 7 nicotinic receptor agonist, is also a potent agonist of the 5-HT3 receptor. Eur J Pharmacol. 2002 Oct 4;452(2):137-44. | |||||
| REF 56 | [3H]A-585539 [(1S,4S)-2,2-dimethyl-5-(6-phenylpyridazin-3-yl)-5-aza-2-azoniabicyclo[2.2.1]heptane], a novel high-affinity alpha7 neuronal nicotinic... J Pharmacol Exp Ther. 2008 Jan;324(1):179-87. | |||||
| REF 57 | In vitro binding characteristics of [3H]AZ11637326, a novel alpha7-selective neuronal nicotinic receptor agonist radioligand. Eur J Pharmacol. 2010 Oct 25;645(1-3):63-9. | |||||
| REF 58 | Nicotine increases the expression of high affinity nerve growth factor receptors in both in vitro and in vivo. Life Sci. 2002 Feb 15;70(13):1543-54. | |||||
| REF 59 | Experience of Black participants in the Lung Health Study smoking cessation intervention program. Nicotine Tob Res. 2001 Nov;3(4):375-82. | |||||
| REF 60 | Structural basis of human Alpha7 nicotinic acetylcholine receptor activation. Cell Res. 2021 Jun;31(6):713-716. | |||||
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.