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Drug-Target Interaction

Drug

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PubChem ID:24466
Structure:
Synonyms:
197U50
2,4-Diamino-5-(3',4'-dichlorophenyl)-6-methyl pyrimidine
2,4-Diamino-5-(3,4-dichlorophenyl)-6-methylpyrimidine
2,4-Pyrimidinediamine, 5-(3,4-dichlorophenyl)-6-methyl-
2aov
5-(3,4-Dichlorophenyl)-6-methyl-2,4-pyrimidinediamine
5-(3,4-DICHLOROPHENYL)-6-METHYLPYRIMIDINE-2,4-DIAMINE
5-(3,4-Dichlorphenyl)-6-methyl-2,4-pyrimidindiamin
5-25-12-00253 (Beilstein Handbook Reference)
7761-45-7
AC1L2NGD
AC1Q2OZ6
AI3-26402
AIDS-006915
AIDS006915
BRN 0223622
BW 197 U
BW 1970
BW 197U
BW 50,197
BW 50-197
BW 50197
BW-197U
BW50197
C11H10Cl2N4
C2M
CCG-35473
CHEBI:166251
CHEMBL264373
CPD-10891
D00309
DB04655
DDMP
LS-135022
Methodichlorophen
Metoprine
Metoprine (USAN)
Metoprine [USAN]
METOPRINE, METHODICHLOROPHEN
MLS002701892
NCI60_041610
NCIMech_000234
Neuro_000005
NSC 19494
NSC 7364
NSC-19494
NSC19494
NSC7364
Pyrimidine, 2,4-diamino-5-(3,4-dichlorophenyl)-6-methyl-
SK 5265
SMR001565478
TCMDC-123931
U 197
U-197
WLN: T6N CNJ BZ DZ ER CG DG& F1

Target

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Uniprot ID:HNMT_RAT
Synonyms:
Histamine N-methyltransferase
HMT
EC-Numbers:2.1.1.8
Organism:Rat
Rattus norvegicus
PDB IDs:-

Binding Affinities:

Ki: Kd:Ic 50:Ec50/Ic50:
----

References:

15082866
Involvement of the renin-angiotensin system in endogenous central histamine-induced reversal of critical haemorrhagic hypotension in rats.. J Jochem (2004) Journal of physiology and pharmacology : an official journal of the Polish Physiological Society display abstract
The study was undertaken to examine the involvement of the renin-angiotensin system in the reversal by endogenous central histamine of critical haemorrhagic hypotension in anaesthetised Wistar rats. Histamine N-methyltransferase inhibitor metoprine (20 microg) administered intracerebroventricularly at 5 min of critical hypotension 20-25 mmHg produced increases in histamine concentrations as measured 20 min after treatment in the hypothalamus (581.33 +/- 63.23 vs. 488.26 +/- 56.34 ng/g of wet tissue; P < 0.01) and medulla oblongata (53.42 +/- 14.65 vs. 34.68 +/- 13.52 ng/g of wet tissue; P < 0.05). That was accompanied by 34.7% higher plasma angiotensin II concentration in comparison to the control group. Metoprine produced dose-dependent (5-20 microg) rises in mean arterial pressure (MAP) and heart rate, which were significantly higher than those in normotensive animals. The resuscitating action of metoprine (20 microg) was associated with rises in renal, mesenteric and hindquarters blood flows, and a 100% survival at 2 h after treatment, while in the saline-treated group, all the animals died within 30 min. Angiotensin type 1 (AT(1)) receptor antagonist ZD 7155 (0.5 mg/kg; iv) decreased regional vascular resistance and inhibited metoprine-induced increase in MAP, whereas AT(2) receptor blocker PD 123319 (10 mg/kg; i.v.) had no effect. Angiotensin-converting enzyme inhibitor captopril (30 mg/kg; i.v.) reduced the increase in plasma angiotensin II level and the haemodynamic effects of metoprine. Neither capropril, nor angiotensin receptor antagonists influence the survival at 2 h after treatment. In conclusion, the renin-angiotensin system is involved in central histamine-induced resuscitating action in rats.