DT-Web

DB00767 - Benzquinamide


Identification
Name Benzquinamide
Accession Number DB00767 (APRD00820)
Type small molecule
Description Benzquinamide is an antiemetic compound with antihistaminic, mild anticholinergic, and sedative properties. The mechanism of action is not known, but presumably benzquinamide works via antagonism of muscarinic acetycholine receptors and histamine H1 receptors.
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 404.4999
Groups approved
Monoisotopic Weight 404.231122144
Pharmacology
Indication Used to prevent and treat nausea and vomiting associated with anesthesia and surgery, administered intramuscularly or intravenously.
Mechanism of action The mechanism of action is not known, but presumably benzquinamide works via antagonism of muscarinic acetycholine receptors and histamine H1 receptors.
Absorption Incomplete, with 33–39% bioavailability via the capsule and suppository routes, relative to the intramuscular route.
Protein binding Not Available
Biotransformation Not Available
Route of elimination Not Available
Toxicity Not Available
Affected organisms
  • Humans and other mammals
Interactions
Drug Interactions Not Available
Food Interactions Not Available

Targets


Histamine H1 receptor
Name Histamine H1 receptor
Gene Name HRH1
Pharmacological action yes
Actions antagonist
References
  • Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. - Pubmed
  • Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. - Pubmed
  • Maurer H, Pfleger K: Identification and differentiation of alkylamine antihistamines and their metabolites in urine by computerized gas chromatography-mass spectrometry. J Chromatogr. 1988 Aug 19;430(1):31-41. - Pubmed
  • Niemegeers CJ: Antiemetic specificity of dopamine antagonists. Psychopharmacology (Berl). 1982;78(3):210-3. - Pubmed
DTHybrid score 0.62
Muscarinic acetylcholine receptor M4
Name Muscarinic acetylcholine receptor M4
Gene Name CHRM4
Pharmacological action yes
Actions antagonist
References
  • Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. - Pubmed
  • Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. - Pubmed
DTHybrid score 0.5555
Muscarinic acetylcholine receptor M1
Name Muscarinic acetylcholine receptor M1
Gene Name CHRM1
Pharmacological action yes
Actions antagonist
References
  • Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. - Pubmed
  • Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. - Pubmed
DTHybrid score 0.8966
Muscarinic acetylcholine receptor M5
Name Muscarinic acetylcholine receptor M5
Gene Name CHRM5
Pharmacological action yes
Actions antagonist
References
  • Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. - Pubmed
  • Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. - Pubmed
DTHybrid score 0.4556
Muscarinic acetylcholine receptor M2
Name Muscarinic acetylcholine receptor M2
Gene Name CHRM2
Pharmacological action yes
Actions antagonist
References
  • Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. - Pubmed
  • Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. - Pubmed
DTHybrid score 0.779
Muscarinic acetylcholine receptor M3
Name Muscarinic acetylcholine receptor M3
Gene Name CHRM3
Pharmacological action yes
Actions antagonist
References
  • Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. - Pubmed
  • Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. - Pubmed
DTHybrid score 0.7766

Predictions


Id Partner name Gene Name Score
4119 Cytochrome P450 2D6 CYP2D6 0.1931
4512 Cytochrome P450 3A4 CYP3A4 0.1505
502 5-hydroxytryptamine 2A receptor HTR2A 0.1209
556 Alpha-1A adrenergic receptor ADRA1A 0.1084
1588 Multidrug resistance protein 1 ABCB1 0.0976
831 D(2) dopamine receptor DRD2 0.0871
590 5-hydroxytryptamine 2C receptor HTR2C 0.0854
3923 Cholinesterase BCHE 0.0803
4200 Cytochrome P450 1A2 CYP1A2 0.0767
813 Neuronal acetylcholine receptor subunit alpha-2 CHRNA2 0.0764
4757 Cytochrome P450 2C9 CYP2C9 0.0734
23 D(1A) dopamine receptor DRD1 0.0714
6016 Cytochrome P450 2C19 CYP2C19 0.0711
540 Sodium-dependent noradrenaline transporter SLC6A2 0.0642
789 Alpha-1D adrenergic receptor ADRA1D 0.0603
632 Alpha-1B adrenergic receptor ADRA1B 0.0599
432 D(4) dopamine receptor DRD4 0.055
824 Sodium-dependent serotonin transporter SLC6A4 0.0545
6030 Cytochrome P450 2B6 CYP2B6 0.0529
6013 Cytochrome P450 2E1 CYP2E1 0.052
1181 Alpha-1-acid glycoprotein 1 ORM1 0.0502
318 Alpha-2A adrenergic receptor ADRA2A 0.0499
320 5-hydroxytryptamine 1A receptor HTR1A 0.0473
638 D(3) dopamine receptor DRD3 0.0456
4924 Cytochrome P450 2C8 CYP2C8 0.0402
4118 Cytochrome P450 3A5 CYP3A5 0.0394
378 Alpha-2C adrenergic receptor ADRA2C 0.039
629 Alpha-2B adrenergic receptor ADRA2B 0.0386
833 Organic cation/carnitine transporter 1 SLC22A4 0.0322
1256 5-hydroxytryptamine 6 receptor HTR6 0.0319
528 5-hydroxytryptamine 1E receptor HTR1E 0.0318
2129 Sucrase-isomaltase, intestinal SI 0.0317
341 5-hydroxytryptamine 3 receptor HTR3A 0.0316
716 5-hydroxytryptamine 7 receptor HTR7 0.031
163 D(1B) dopamine receptor DRD5 0.0288
6145 Solute carrier family 22 member 1 SLC22A1 0.0282
713 Sodium-dependent dopamine transporter SLC6A3 0.0278
436 5-hydroxytryptamine 2B receptor HTR2B 0.0274
6144 Solute carrier family 22 member 2 SLC22A2 0.0269
118 Organic cation/carnitine transporter 2 SLC22A5 0.0262
725 5-hydroxytryptamine 1D receptor HTR1D 0.0257
6107 Cytochrome P450 3A7 CYP3A7 0.0249
6098 Potassium voltage-gated channel subfamily D member 2 KCND2 0.0247
6099 Potassium voltage-gated channel subfamily D member 3 KCND3 0.0247
885 5-hydroxytryptamine 1B receptor HTR1B 0.0241
124 Histamine H2 receptor HRH2 0.0217
5718 Cytochrome P450 2A6 CYP2A6 0.0193
465 Calmodulin CALM1 0.0189
5878 Alpha-7 nicotinic cholinergic receptor subunit CHRFAM7A 0.018
1341 Histamine H3 receptor HRH3 0.0175
1656 CYP2B protein CYP2B 0.0171
516 Neurotensin receptor type 2 NTSR2 0.0168
6024 Cytochrome P450 1A1 CYP1A1 0.0165
6432 Transporter snf 0.0151
706 Glutamate [NMDA] receptor subunit 3A GRIN3A 0.0146
458 Neuronal acetylcholine receptor subunit alpha-10 CHRNA10 0.0136
723 Cytosolic phospholipase A2 PLA2G4A 0.0124
587 Serum albumin ALB 0.0124
6106 Cytochrome P450 2C18 CYP2C18 0.0123
6104 Dimethylaniline monooxygenase [N-oxide-forming] 1 FMO1 0.012
6176 UDP-glucuronosyltransferase 1-3 UGT1A3 0.0119
6147 Solute carrier family 22 member 3 SLC22A3 0.0118
1360 Sphingomyelin phosphodiesterase SMPD1 0.0105
6101 Dimethylaniline monooxygenase [N-oxide-forming] 3 FMO3 0.0103
6100 BDNF/NT-3 growth factors receptor NTRK2 0.0093
164 Histamine H4 receptor HRH4 0.0088
220 Sodium channel protein type 5 subunit alpha SCN5A 0.0088
6047 Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A PDE1A 0.0086
1275 Estrogen sulfotransferase SULT1E1 0.0086
5692 Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1B PDE1B 0.0081
696 Kappa-type opioid receptor OPRK1 0.0079
474 Acetylcholinesterase ACHE 0.0079
6182 Cytochrome P450 2J2 CYP2J2 0.0078
4115 Voltage-dependent L-type calcium channel subunit alpha-1D CACNA1D 0.0077
6154 Multidrug and toxin extrusion protein 1 SLC47A1 0.0076
478 Voltage-dependent L-type calcium channel subunit alpha-1C CACNA1C 0.0075
1618 High affinity nerve growth factor receptor NTRK1 0.0072
1086 Potassium voltage-gated channel subfamily KQT member 2 KCNQ2 0.0069
20 Prostaglandin G/H synthase 1 PTGS1 0.0066
762 Voltage-dependent calcium channel subunit alpha-2/delta-1 CACNA2D1 0.0065
4110 Voltage-dependent L-type calcium channel subunit beta-2 CACNB2 0.0064
467 Delta-type opioid receptor OPRD1 0.0064
101 Potassium voltage-gated channel subfamily H member 2 KCNH2 0.0061
734 D1 dopamine receptor-interacting protein calcyon CALY 0.0061
6139 Solute carrier organic anion transporter family member 1A2 SLCO1A2 0.0057
6025 UDP-glucuronosyltransferase 1-4 UGT1A4 0.0056
858 Potassium voltage-gated channel subfamily A member 1 KCNA1 0.0056
193 Beta-1 adrenergic receptor ADRB1 0.0055
766 Beta-2 adrenergic receptor ADRB2 0.0054
6097 Protein S100-A2 S100A2 0.005
1810 Protein S100-A1 S100A1 0.005
198 Sodium channel protein type 10 subunit alpha SCN10A 0.0049
215 Sodium channel protein type 11 subunit alpha SCN11A 0.0045
1729 Solute carrier family 22 member 6 SLC22A6 0.0043
1048 Protein S100-A13 S100A13 0.0043
2226 Protein S100-A12 S100A12 0.0043
2132 Protein S100-B S100B 0.004
15 Voltage-dependent T-type calcium channel subunit alpha-1I CACNA1I 0.0037
1898 Cytochrome P450 1B1 CYP1B1 0.0037
94 5-hydroxytryptamine 4 receptor HTR4 0.0036
535 Voltage-dependent T-type calcium channel subunit alpha-1G CACNA1G 0.0035
6217 High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8B PDE8B 0.0035
964 Voltage-dependent T-type calcium channel subunit alpha-1H CACNA1H 0.0034
6023 Cytochrome P450 11B2, mitochondrial CYP11B2 0.0033
3876 Aromatic-L-amino-acid decarboxylase DDC 0.0033
380 Cytochrome P450 17A1 CYP17A1 0.0032
6216 High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8A PDE8A 0.003
805 Cytochrome P450 11B1, mitochondrial CYP11B1 0.0029
691 cAMP-specific 3',5'-cyclic phosphodiesterase 7B PDE7B 0.0029
779 High-affinity cAMP-specific 3',5'-cyclic phosphodiesterase 7A PDE7A 0.0026
439 Glutamate [NMDA] receptor subunit epsilon-4 GRIN2D 0.0026
6157 Solute carrier organic anion transporter family member 1B3 SLCO1B3 0.0024
1632 Solute carrier organic anion transporter family member 2B1 SLCO2B1 0.0024
4109 cAMP-specific 3',5'-cyclic phosphodiesterase 4C PDE4C 0.0024
591 Glutamate [NMDA] receptor subunit 3B GRIN3B 0.0023
401 Glutamate [NMDA] receptor subunit zeta-1 GRIN1 0.0023
1490 Solute carrier organic anion transporter family member 1B1 SLCO1B1 0.0021
6040 6-phosphogluconate dehydrogenase, decarboxylating PGD 0.0021
1971 cAMP-specific 3',5'-cyclic phosphodiesterase 4A PDE4A 0.002
2358 cAMP-specific 3',5'-cyclic phosphodiesterase 4D PDE4D 0.0019
4203 Histamine N-methyltransferase HNMT 0.0019
541 cAMP-specific 3',5'-cyclic phosphodiesterase 4B PDE4B 0.0018
847 Mu-type opioid receptor OPRM1 0.0018
3941 Amine oxidase [flavin-containing] A MAOA 0.0018
4113 Voltage-dependent L-type calcium channel subunit alpha-1F CACNA1F 0.0016
872 Gamma-aminobutyric-acid receptor subunit alpha-1 GABRA1 0.0015
4111 Voltage-dependent L-type calcium channel subunit alpha-1S CACNA1S 0.0013
776 Bile salt export pump ABCB11 0.001
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