Details of the Drug-Related molecule(s) Expression Atlas

General Information of Drug (ID: DMAFBCY)

Drug Name

Mequitazine Drug Info

Synonyms

Butix; Instotal; Kitazemin; Mequitazina; Mequitazinum; Metaplexan; Mircol; Primalan; Quitadrill; Vigigan; Virginan; Zesulan; Italfarmaco brand of mequitazine; Mequitazina [Spanish]; Mequitazine hydrochloride; Pierre Fabre brand of mequitazine; LM 209; Kitazemin (TN); LM-209; Mequitazina [INN-Spanish]; Mequitazinum [INN-Latin]; Mequitazine (JP15/INN); Mequitazine [INN:BAN:DCF:JAN]; Mequitazine tartrate, (R-(R*,R*))-isomer; 10-(1-Azabicyclo[2.2.2]oct-3-ylmethyl)-10H-phenothiazine; 10-(1-azabicyclo(2.2.2)oct-8-ylmethyl)phenothiazine; 10-(1-azabicyclo[2.2.2]octan-3-ylmethyl)phenothiazine; 10-(3-Quinuclidinylmethyl)phenothiazine; 10H-Phenothiazine, 10-(1-azabicyclo(2.2.2)oct-3-ylmethyl)-(9CI); 3-Methylquinuclidinyl-10-phenothiazine

Indication

Disease Entry	ICD 11	Status	REF
Allergic rhinitis	CA08.0	Approved	[1]
Respiratory disease	CB40	Phase 2	[2]

Therapeutic Class

Antihistamines

Cross-matching ID

PubChem CID: 4066
ChEBI ID: CHEBI:31821
CAS Number: CAS 29216-28-2
TTD Drug ID: DMAFBCY
VARIDT Drug ID: DR01379
INTEDE Drug ID: DR1030

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Histamine H1 receptor (H1R)	TTTIBOJ	HRH1_HUMAN	Antagonist	[3]

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Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	Highest Status	REF
P-glycoprotein 1 (ABCB1)	DTUGYRD	MDR1_HUMAN	Approved	[4]

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Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	Highest Status	REF
Cytochrome P450 2D6 (CYP2D6)	DECB0K3	CP2D6_HUMAN	Investigative	[5]

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The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule	Molecule Type	Gene Name	Liver	Colon	Kidney	Small Intestine
Histamine H1 receptor (H1R)	DTT	HRH1	5.972	5.7	5.816	6.002
P-glycoprotein 1 (ABCB1)	DTP	P-GP	7.009	6.988	7.442	8.135
Cytochrome P450 2D6 (CYP2D6)	DME	CYP2D6	3.307	5.005	3.921	5.327

Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

The Studied Disease

Allergic rhinitis

ICD Disease Classification

CA08.0

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Histamine H1 receptor (H1R)	DTT	HRH1	6.74E-01	0.13	0.43
P-glycoprotein 1 (ABCB1)	DTP	P-GP	6.54E-01	1.95E-01	4.04E-01
Cytochrome P450 2D6 (CYP2D6)	DME	CYP2D6	8.70E-01	2.98E-02	1.22E-01

Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1	Drug information of Mequitazine, 2008. eduDrugs.
2	ClinicalTrials.gov (NCT01951222) Bronchodilator Properties and Safety in Asthma. U.S. National Institutes of Health.
3	Efficiency of mequitazine in the treatment of allergic rhinitis and chronic urticaria in children. A bibliographic systematic review. Rev Alerg Mex. 2008 Jan-Feb;55(1):3-9.
4	Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs. J Pharmacol Exp Ther. 2002 Dec;303(3):1029-37.
5	Oxidation of histamine H1 antagonist mequitazine is catalyzed by cytochrome P450 2D6 in human liver microsomes. J Pharmacol Exp Ther. 1998 Feb;284(2):437-42.