THERAPY DOSSIER · th-68cd8170b22a

Endogenous histamine, studied using HDC knockout mice, exogenous histamine supplementation and the receptor antagonists pyrilamine (H1) and cimetidine (H2)

Drug · Histamine: H1 receptor agonist (AGONIST); study also uses H1 antagonist pyrilamine and H2 antagonist cimetidine

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Evidence & regulatory context

Mechanism: Histamine: H1 receptor agonist (AGONIST); study also uses H1 antagonist pyrilamine and H2 antagonist cimetidine
Target: CHEMBL231
Injury models: Other
Reported indication: Not recorded
First approval: 1939
Development stage: Not recorded
ChEMBL record: CHEMBL90 ↗
ChEMBL max phase: 4 / 4 (development scale, not regulatory approval)
Synonyms: Histamine; pyrilamine (co-listed); cimetidine (co-listed)
Note: Not recorded

Clinical trials 0

0 linked trials carry an injury-indication flag. These flags support record-level exploration and sit alongside the stringent aggregate counts described in Methods.

No linked human trial in this dataset.

Preclinical evidence 1

1 studies reported at therapy level; 1 evidence entries itemised.

PMID 26278136 ↗2015Reported benefit

Histamine deficiency exacerbates myocardial injury in acute myocardial infarction through impaired macrophage infiltration and increased cardiomyocyte apoptosis.

MouseOtherHDC-EGFP BAC transgenic and HDC knockout mice on Balb/C and C57BL/6 backgrounds; H9c2 rat cardiomyoblasts used in vitron = 7 mice in the combined pyrilamine plus cimetidine group; 14…Intraperitoneal in vivo; culture medium in vitroHistamine 4 mg/kg/day intraperitoneally; pyrilamine 10 mg/k…Dosing started 3 days before coronary ligation and continued until euthanasia

Model: Acute myocardial infarction induced by permanent ligation of the left anterior descending coronary artery under isoflurane anaesthesia, with sham thoracotomy controls

Histamine deficiency raised CK-MB, enlarged infarct size, lowered ejection fraction and increased cardiomyocyte apoptosis while reducing early macrophage infiltration, and exogenous histamine reversed these changes; combined pyrilamine plus cimetidine markedly reduced 7 day survival (1 of 7 mice su…

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