General Information of Drug (ID: DMZWQH3)

Drug Name
[125I]epibatidine Drug Info
Synonyms
CHEMBL6623; NLPRAJRHRHZCQQ-UHFFFAOYSA-N; 140111-52-0; [3H]EPIBATIDINE; SR-01000597620; [125I]EPIBATIDINE; AC1Q3PYA; AC1L1AYB; 208/210 Epibatidine; KBioSS_000603; KBioGR_000603; BSPBio_001263; (R)-2-(6-Chloro-pyridin-3-yl)-7-aza-bicyclo[221]heptane; [3H]epibatidine
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
1204
ChEBI ID
CHEBI:91678
TTD Drug ID
DMZWQH3

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Investigative Drug(s)
Discontinued Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Ziprasidone DMM58JY Bipolar disorder 6A60 Approved [6]
ALCURONIUM DM2U4XQ Anaesthesia 9A78.6 Approved [7]
AMG 386 DMQJXL4 Breast cancer 2C60-2C65 Phase 3 [8]
CYTISINE DMUF0BJ Tobacco dependence 6C4A.2 Phase 3 [9]
EVP-6124 DMLQO7F Alzheimer disease 8A20 Phase 3 [10]
GTS-21 DMEN5KA Parkinson disease 8A00.0 Phase 2 [11]
JNJ-39393406 DMUOEKM Depression 6A70-6A7Z Phase 2 [12]
ABT-126 DM2OS51 Alzheimer disease 8A20 Phase 2 [13]
TC-6987 DMNFP21 Asthma CA23 Phase 2 [14]
AQW-051 DMD2RFO Alzheimer disease 8A20 Phase 2 [15]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Rocuronium DMY9BMK Muscle spasm MB47.3 Approved [16]
Tubocurarine DMBZIVP Anaesthesia 9A78.6 Approved [16]
Cisatracurium DMUZPJ5 Muscle spasm MB47.3 Approved [16]
Vecuronium DMP0UK2 Spasm MB47.3 Approved [16]
Levallorphan DMCOLUP Narcotic depression 6A7Z Approved [17]
Mivacurium DM473VD Anaesthesia 9A78.6 Approved [16]
Carbachol DMX9K8F Glaucoma/ocular hypertension 9C61 Approved [17]
Pipecuronium DM5F84A Spasm MB47.3 Approved [17]
CYTISINE DMUF0BJ Tobacco dependence 6C4A.2 Phase 3 [18]
CHOLINE DM5D9YK Insomnia 7A00-7A0Z Investigative [19]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Promazine DMZAL7W Acute intermittent hepatic porphyria 5C58.11 Approved [20]
ACECLIDINE DMOLNCZ Glaucoma/ocular hypertension 9C61 Approved [21]
Pilocarpine DMV9ADG Glaucoma/ocular hypertension 9C61 Approved [22]
Anisodine DMNOSWU Central and peripheral nervous disease 8A04-8E7Z Approved [23]
Atropine DMEN6X7 Organophosphate poisoning NE6Z Approved [24]
Propiverine DMUWBIJ Urinary incontinence MF50.2 Approved [25]
Umeclidinium DM4E8O9 Chronic obstructive pulmonary disease CA22 Approved [26]
Cimetropium bromide DMZHPNE Gastric motility disorder DA21 Approved [27]
Butylscopolamine DMZKXB7 Dysmenorrhea GA34.3 Approved [28]
Trospium DMX6RTG Overactive bladder GC50.0 Approved [29]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
CYTISINE DMUF0BJ Tobacco dependence 6C4A.2 Phase 3 [30]
TC-5214 DM8AM60 Palmar hyperhidrosis EE00.00 Phase 2 [31]
SUVN-911 DMLPBVF Major depressive disorder 6A70.3 Phase 1 [32]
AZD-9684 DMHA5ME Thrombosis DB61-GB90 Discontinued in Phase 2 [33]
ABT-594 DMGMBCW N. A. N. A. Discontinued in Phase 2 [34]
ABT-418 DMNP72I Alzheimer disease 8A20 Discontinued in Phase 2 [35]
HOMOEPIBATIDINE DMHP9WV N. A. N. A. Terminated [30]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one DMM9X0G Discovery agent N.A. Investigative [36]
(2S,3S)-2-Phenyl-3,5,5-trimethylmorpholin-2-ol DMDUGZS Discovery agent N.A. Investigative [37]
(2S,3S)-2-(m-Tolyl)-3,5,5-trimethylmorpholin-2-ol DMDUI8R Discovery agent N.A. Investigative [37]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Muscarinic acetylcholine receptor M5 (CHRM5) TTH18TF ACM5_HUMAN Agonist [2]
Neuronal acetylcholine receptor alpha-2 (CHRNA2) TTF4E0J ACHA2_HUMAN Agonist [3]
Neuronal acetylcholine receptor alpha-7 (CHRNA7) TTLA931 ACHA7_HUMAN Agonist [4]
Neuronal acetylcholine receptor beta-2 (CHRNB2) TT5KPZR ACHB2_HUMAN Agonist [5]

References

1 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: 3976).
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. (Target id: 467).
3 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: 463).
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. (Target id: 468).
5 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: 465).
6 The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22.
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8 Clinical pipeline report, company report or official report of Roche (2009).
9 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.
10 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.
11 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.
12 Allosteric alpha-7 nicotinic receptor modulation and P50 sensory gating in schizophrenia: a proof-of-mechanism study. Neuropharmacology. 2013 Jan;64:197-204.
13 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.
14 ClinicalTrials.gov (NCT01293669) Glycemic Control, Safety and Tolerability of TC-6987 Monotherapy in Type 2 Diabetes Mellitus. U.S. National Institutes of Health.
15 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.
16 Pharmacological characteristics of the inhibition of nondepolarizing neuromuscular blocking agents at human adult muscle nicotinic acetylcholine receptor. Anesthesiology. 2009 Jun;110(6):1244-52.
17 Synergy between pairs of competitive antagonists at adult human muscle acetylcholine receptors. Anesth Analg. 2008 Aug;107(2):525-33.
18 Synthesis and pharmacological evaluation of novel 9- and 10-substituted cytisine derivatives. Nicotinic ligands of enhanced subtype selectivity. J Med Chem. 2006 May 4;49(9):2673-6.
19 Pharmacology of the agonist binding sites of rat neuronal nicotinic receptor subtypes expressed in HEK 293 cells. Bioorg Med Chem Lett. 2004 Apr 19;14(8):1845-8.
20 Muscarinic cholinergic and histamine H1 receptor binding of phenothiazine drug metabolites. Life Sci. 1988;43(5):405-12.
21 Design, synthesis, and neurochemical evaluation of 5-(3-alkyl-1,2,4- oxadiazol-5-yl)-1,4,5,6-tetrahydropyrimidines as M1 muscarinic receptor agonists. J Med Chem. 1993 Apr 2;36(7):842-7.
22 Retinoic acid prevents virus-induced airway hyperreactivity and M2 receptor dysfunction via anti-inflammatory and antiviral effects. Am J Physiol Lung Cell Mol Physiol. 2009 Aug;297(2):L340-6.
23 Medicinal plants in therapy. Bull World Health Organ. 1985;63(6):965-81.
24 Additive protective effects of donepezil and nicotine against salsolinol-induced cytotoxicity in SH-SY5Y cells. Neurotox Res. 2009 Oct;16(3):194-204.
25 Affinity profiles of various muscarinic antagonists for cloned human muscarinic acetylcholine receptor (mAChR) subtypes and mAChRs in rat heart and submandibular gland. Life Sci. 1999;64(25):2351-8.
26 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: 7354).
27 Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77.
28 Comparison of pharmacological effects of L- and DL-n-butyl-scopolamine in rat uterus. Yao Xue Xue Bao. 1994;29(1):24-7.
29 Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.
30 Epibatidine isomers and analogues: structure-activity relationships. Bioorg Med Chem Lett. 2006 Nov 1;16(21):5493-7.
31 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
32 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
33 Blockade and activation of the human neuronal nicotinic acetylcholine receptors by atracurium and laudanosine. Anesthesiology. 2001 Apr;94(4):643-51.
34 The nicotinic acetylcholine receptor agonist ABT-594 increases FGF-2 expression in various rat brain regions. Neuroreport. 1999 Dec 16;10(18):3909-13.
35 Nicotine, brain nicotinic receptors, and neuropsychiatric disorders. Arch Med Res. 2000 Mar-Apr;31(2):131-44.
36 Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 rec... J Med Chem. 2010 Sep 9;53(17):6386-97.
37 Synthesis and characterization of in vitro and in vivo profiles of hydroxybupropion analogues: aids to smoking cessation. J Med Chem. 2010 Jun 24;53(12):4731-48.