General Information of Drug (ID: DMGFWSM)

Drug Name
Zaleplon Drug Info
Synonyms
Sonata; Zalaplon; Zerene; CL 284846; L 846; L846; LJC 10846; ZAL 846; AZ-007; CL 284,846; CL-284846; CL284,846; L-846; LJC-10846; SKP-1041; Sonata (TN); Staccato-zaleplon; Starnoc (TN); ZAL-846; Zaleplon [USAN:INN]; Zaleplon (JAN/USAN/INN); N-[3-(3-cyanopyrazolo[1,5-a]pyrimidin-7-yl)phenyl]-N-ethylacetamide; N-(3-(3-Cyanopyrazolo(1,5-a)pyrimidin-7-yl)phenyl)-N-ethylacetamide; 3'-(3-Cyanopyrazolo(1,5-a)pyrimidin-7-yl)-N-ethylacetanilide; 3'-(3-Cyanopyrazolo(1,5-alpha)pyrimidin-7-yl)-N-ethylacetanilide
Indication
Disease Entry ICD 11 Status REF
Insomnia 7A00-7A0Z Approved [1]
Sleep disorder, initiating and maintaining sleep Investigative [2]
Therapeutic Class
Hypnotics and Sedatives
Cross-matching ID
PubChem CID
5719
ChEBI ID
CHEBI:10102
CAS Number
CAS 151319-34-5
TTD Drug ID
DMGFWSM
INTEDE Drug ID
DR1725
ACDINA Drug ID
D00738

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DME
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Preclinical Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Ethanol DMDRQZU Chronic pain MG30 Approved [7]
Zolpidem DMWOSKJ Insomnia 7A00-7A0Z Approved [8]
Methoxyflurane DML0RAE Anaesthesia 9A78.6 Approved [7]
Nitrazepam DMEGIQ6 Epilepsy 8A60-8A68 Approved [7]
Allopregnanolone DMNLHAC Depression 6A70-6A7Z approved [9]
Clobazam - Lundbeck DMW1OQ0 Anxiety disorder 6B00-6B0Z Approved [7]
Hexobarbital DMQ314B Anaesthesia 9A78.6 Approved [7]
THIOCOLCHICOSIDE DMEPWYA Muscle spasm MB47.3 Approved [10]
Meprobamate DMHM93Y Anxiety Approved [7]
Ethchlorvynol DM53IP1 Insomnia 7A00-7A0Z Approved [7]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By Cytochrome P450 3A4 (CYP3A4)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [11]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [12]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [13]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [14]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [15]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [16]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [17]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [18]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [12]
Verapamil DMA7PEW Angina pectoris BA40 Approved [19]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By Cytochrome P450 3A5 (CYP3A5)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [20]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [21]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [22]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [5]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [23]
Sulfasalazine DMICA9H Irritable bowel syndrome DD91.0 Approved [24]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [25]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [26]
Verapamil DMA7PEW Angina pectoris BA40 Approved [27]
Sorafenib DMS8IFC Adenocarcinoma 2D40 Approved [5]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By Cytochrome P450 3A7 (CYP3A7)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Progesterone DMUY35B Amenorrhea GA20.0 Approved [28]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [5]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [5]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [5]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [29]
Verapamil DMA7PEW Angina pectoris BA40 Approved [30]
Sorafenib DMS8IFC Adenocarcinoma 2D40 Approved [5]
Quinine DMSWYF5 Malaria 1F40-1F45 Approved [5]
Irinotecan DMP6SC2 Adenocarcinoma 2D40 Approved [5]
Metronidazole DMTIVEN Abscess Approved [31]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By Aldehyde oxidase (AOX1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
XL147 DMML7BE Solid tumour/cancer 2A00-2F9Z Phase 2 [6]
SGX523 DM3RSMF Solid tumour/cancer 2A00-2F9Z Phase 1 [32]
VUFB-11502 DM7WFR0 N. A. N. A. Preclinical [33]

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
GABA(A) receptor alpha-1 (GABRA1) TT1MPAY GBRA1_HUMAN Modulator [3]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Substrate [4]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Substrate [5]
Cytochrome P450 3A7 (CYP3A7) DERD86B CP3A7_HUMAN Substrate [5]
Aldehyde oxidase (AOX1) DEAWHS8 AOXA_HUMAN Substrate [6]

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: 4345).
2 Zaleplon FDA Label
3 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
4 Metabolism of zaleplon by human liver: evidence for involvement of aldehyde oxidase. Xenobiotica. 2002 Oct;32(10):835-47.
5 Drug Interactions Flockhart Table
6 Characterization of aldehyde oxidase enzyme activity in cryopreserved human hepatocytes. Drug Metab Dispos. 2012 Feb;40(2):267-75.
7 DrugBank: a knowledgebase for drugs, drug actions and drug targets. Nucleic Acids Res. 2008 Jan;36(Database issue):D901-6.
8 Zolpidem, a selective GABA(A) receptor alpha1 subunit agonist, induces comparable Fos expression in oxytocinergic neurons of the hypothalamic paraventricular and accessory but not supraoptic nuclei in the rat.Brain Res Bull.2006 Dec 11;71(1-3):200-7.
9 Neurosteroid analogues. 10. The effect of methyl group substitution at the C-6 and C-7 positions on the GABA modulatory and anesthetic actions of (... J Med Chem. 2005 Apr 21;48(8):3051-9.
10 3-demethoxy-3-glycosylaminothiocolchicines: Synthesis of a new class of putative muscle relaxant compounds. J Med Chem. 2006 Sep 7;49(18):5571-7.
11 Expression levels and activation of a PXR variant are directly related to drug resistance in osteosarcoma cell lines. Cancer. 2007 Mar 1;109(5):957-65.
12 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
13 Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6. J Pharmacol Exp Ther. 2004 Sep;310(3):1062-75.
14 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
15 Metabolic interactions between acetaminophen (paracetamol) and two flavonoids, luteolin and quercetin, through in-vitro inhibition studies. J Pharm Pharmacol. 2017 Dec;69(12):1762-1772.
16 Potent mechanism-based inhibition of CYP3A4 by imatinib explains its liability to interact with CYP3A4 substrates. Br J Pharmacol. 2012 Apr;165(8):2787-98.
17 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
18 The metabolism of zidovudine by human liver microsomes in vitro: formation of 3'-amino-3'-deoxythymidine. Biochem Pharmacol. 1994 Jul 19;48(2):267-76.
19 Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
20 Drug related genetic polymorphisms affecting adverse reactions to methotrexate, vinblastine, doxorubicin and cisplatin in patients with urothelial cancer. J Urol. 2008 Dec;180(6):2389-95.
21 Human prostate CYP3A5: identification of a unique 5'-untranslated sequence and characterization of purified recombinant protein. Biochem Biophys Res Commun. 1999 Jul 14;260(3):676-81.
22 Polymorphisms in cytochrome P4503A5 (CYP3A5) may be associated with race and tumor characteristics, but not metabolism and side effects of tamoxifen in breast cancer patients. Cancer Lett. 2005 Jan 10;217(1):61-72.
23 Induction of hepatic CYP2E1 by a subtoxic dose of acetaminophen in rats: increase in dichloromethane metabolism and carboxyhemoglobin elevation. Drug Metab Dispos. 2007 Oct;35(10):1754-8.
24 Urinary 6 beta-hydroxycortisol excretion in rheumatoid arthritis. Br J Rheumatol. 1997 Jan;36(1):54-8.
25 Clinical pharmacokinetics of imatinib. Clin Pharmacokinet. 2005;44(9):879-94.
26 Kinetics and regulation of cytochrome P450-mediated etoposide metabolism. Drug Metab Dispos. 2004 Sep;32(9):993-1000.
27 Differential mechanism-based inhibition of CYP3A4 and CYP3A5 by verapamil. Drug Metab Dispos. 2005 May;33(5):664-71.
28 The role of cytochrome P450 3A (CYP3A) isoform(s) in oxidative metabolism of testosterone and benzphetamine in human adult and fetal liver. J Steroid Biochem Mol Biol. 1993 Jan;44(1):61-7.
29 Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448.
30 Prediction of cytochrome P450 3A inhibition by verapamil enantiomers and their metabolites. Drug Metab Dispos. 2004 Feb;32(2):259-66.
31 The role of human cytochrome P450 enzymes in the formation of 2-hydroxymetronidazole: CYP2A6 is the high affinity (low Km) catalyst. Drug Metab Dispos. 2013 Sep;41(9):1686-94.
32 Species-specific metabolism of SGX523 by aldehyde oxidase and the toxicological implications. Drug Metab Dispos. 2010 Aug;38(8):1277-85.
33 The critical role of oxidative stress in the toxicity and metabolism of quinoxaline 1,4-di-N-oxides in vitro and in vivo. Drug Metab Rev. 2016 May;48(2):159-82.