"目录号: HY-14289
GPCR/G ProteinImmunology/Inflammation|
Cimetidine是H2受体拮抗剂。
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生物活性
Description
Cimetidine is a histamine-2 (H2) receptor antagonist.IC50 Value: Target: Histamine-2 Receptorin vitro: Cimetidine, a partial agonist for H2R, has a pharmacological profile different from ranitidine and famotidine, possibly contributing to its antitumor activity on gastrointestinal cancers [1]. Cimetidine had no effect on the uptake and cytotoxicity of cisplatin in ovarian cancer cells with high OCT2 mRNA levels (IGROV-1 cells) [2]. Cimetidine showed no effect on proliferation, survival, migration and invasion of 3LL cells. Cimetidine reversed MDSC-mediated T-cell suppression, and improved IFN-γ production. [3]. Cimetidine-mediated down-regulation of NCAM involved suppression of the nuclear translocation of NF-kappaB, a transcriptional activator of NCAM gene expression [4].in vivo: the antitumor efficacy of cisplatin in mice bearing luciferase-tagged IGROV-1 xenografts was unaffected by cimetidine (P = 0.39). Data obtained in 18 patients receiving cisplatin (100 mg/m(2)) in a randomized crossover fashion with or without cimetidine (800 mg × 2) revealed that cimetidine did not alter exposure to unbound cisplatin [2]. cimetidine reduced CD11b(+)Gr-1(+) myeloid derived-suppressive cell (MDSC) accumulation in spleen, blood and tumor tissue of tumor-bearing mice [3]. Cimetidine exerts a beneficial effect on periodontal disease in rats, decreasing the RANKL/OPG ratio in gingival connective tissue and reducing alveolar bone resorption [5].
Clinical Trial
Centre Hospitalier Universitaire de Saint Etienne
Kidney Transplantation
March 2007
Knopp Biosciences
Amyotrophic Lateral Sclerosis
March 2012
Phase 1
University of Maryland|Food and Drug Administration (FDA)
Healthy
March 2011
Phase 1
Chiesi Farmaceutici S.p.A.
COPD
May 2014
Phase 1
Pfizer
Generalized Anxiety Disorder
January 2009
Phase 1
Community Research Initiative of New England|NIH AIDS Clinical Trials Information Service
HIV Infections
AstraZeneca
Stress Ulcer Prophylaxis
July 2014
Phase 3
Boehringer Ingelheim
Healthy
July 2000
Phase 1
University of Maryland|Food and Drug Administration (FDA)
Healthy
June 2009
Phase 1
Valeant Pharmaceuticals International, Inc.
Upper Gastrointestinal Bleeding
May 2002
Phase 3
AstraZeneca
Bleeding Peptic Ulcer
February 2013
Phase 3
Boehringer Ingelheim
Healthy
September 2014
Phase 1
Canadian Network for Observational Drug Effect Studies, CNODES|Drug Safety and Effectiveness Network, Canada|Canadian Institutes of Health Research (CIHR)
Gastroesophageal Reflux Disease (GERD)|Community-acquired Pneumonia
September 2011
Hoag Memorial Hospital Presbyterian
Kidney Cancer|Melanoma (Skin)|Unspecified Adult Solid Tumor, Protocol Specific
January 1996
Phase 2
M.D. Anderson Cancer Center
Endometrial Cancer
April 2001
Phase 2
Centre Hospitalier Universitaire de Saint Etienne
Kidney Transplantation
March 2007
Knopp Biosciences
Amyotrophic Lateral Sclerosis
March 2012
Phase 1
University of Maryland|Food and Drug Administration (FDA)
Healthy
March 2011
Phase 1
Chiesi Farmaceutici S.p.A.
COPD
May 2014
Phase 1
Pfizer
Generalized Anxiety Disorder
January 2009
Phase 1
Community Research Initiative of New England|NIH AIDS Clinical Trials Information Service
HIV Infections
AstraZeneca
Stress Ulcer Prophylaxis
July 2014
Phase 3
Boehringer Ingelheim
Healthy
July 2000
Phase 1
University of Maryland|Food and Drug Administration (FDA)
Healthy
June 2009
Phase 1
Valeant Pharmaceuticals International, Inc.
Upper Gastrointestinal Bleeding
May 2002
Phase 3
AstraZeneca
Bleeding Peptic Ulcer
February 2013
Phase 3
Boehringer Ingelheim
Healthy
September 2014
Phase 1
Canadian Network for Observational Drug Effect Studies, CNODES|Drug Safety and Effectiveness Network, Canada|Canadian Institutes of Health Research (CIHR)
Gastroesophageal Reflux Disease (GERD)|Community-acquired Pneumonia
September 2011
Hoag Memorial Hospital Presbyterian
Kidney Cancer|Melanoma (Skin)|Unspecified Adult Solid Tumor, Protocol Specific
January 1996
Phase 2
M.D. Anderson Cancer Center
Endometrial Cancer
April 2001
Phase 2
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References
