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Table 1 Histamine receptors antagonists: therapeutic applications and outcomes

From: Histaminergic system in brain disorders: lessons from the translational approach and future perspectives

Receptor Drug Disorder Study Outcome Reference
H1R Chlorpheniramine Model of stress by immobilization/sleep disturb Preclinical Reduction in REM sleep. [53]
Dimebon AD Clinical No significant improvement in a phase III trial. [54]
Doxepin Insomnia Clinical Improvements in sleep maintenance and duration in a 4-week outpatient trial of elderly adults. [55],[56]
H2R Dimebon AD Clinical No significant improvement in a phase III trial. [54]
Famotidine Autism Clinical Attenuated symptoms like irritability, hyperactivity and atypical pattern of eye contact in children with autism. [57]
SCH Clinical Reduced scores in BPRS, CGI, and SANS. [58],[59]
H3R GSK239512 AD Clinical Failed on improving executive function/working memory in a randomized, double-blind, placebo-controlled. [60]
ABT-288 AD Clinical No significant improvements in a randomized study. [61]
SCH Clinical Failed on providing cognitive improvements to patients. [62]
JNJ-10181457 Model of AD Preclinical Reversed cognitive deficits induced by scopolamine and normalized ACh neurotransmission. [63]
Pitolisant Narcolepsy Clinical Reduced excessive daytime sleepiness [64]
ABT-239 Model of SCH Preclinical Attenuated cognitive deficits caused by ketamine and MK-801. [50]
A-431404 Model of SCH Preclinical Attenuated cognitive deficits caused by ketamine and MK-801. [50]
JNJ-31001074 ADHD Clinical No significant improvements in adult patients. [65]
Betahistine SCH Clinical Reduced weight gain by patients with SCH treated with olanzapine. [66]
JNJ-39220675 Model of alcoholism Preclinical Reduced intake of alcohol after a period of abstinence. [67]
Thioperamide Model of SCH Preclinical Enhancement of prepulse inhibition. [68]
Model of PD Preclinical Decreased hyperactivity. [69]
GSK189254 Model of neuropathic pain Preclinical Antinociceptive effect. [70],[71]
GSK334429 Model of neuropathic pain Preclinical Antinociceptive effect. [71]
SAR110894 Model of SCH Preclinical Normalized impaired social behavior. [72]
Ciproxifan Model of SCH Preclinical Enhancement of prepulse inhibition. [68]
Model of AD Preclinical Improvements in hyperactivity and memory deficits. [73]
H4R JNJ7777120 Model of neuropathic pain Preclinical Antinociceptive effect. [74],[75]
ZPL3893787 Tested in healthy volunteers. Potential treatment for asthma, allergic rhinitis, pain, and other inflammatory diseases. Clinical Completed phase I trial. Safe and well tolerated. [76]
UR63325 Allergic rhinitis Clinical Currently on phase II clinical trial. No data available. [76]
KD1157 Tested in healthy volunteers. Potential treatment for allergic rhinitis. Clinical Safe and well tolerated. [76]
JNJ38518168 Asthma Clinical Currently on phase II clinical trial. No data available. [76]
JNJ39758979 Asthma Clinical Completed phase II clinical trial. No data available. [76]