Table 1 Histamine receptors antagonists: therapeutic applications and outcomes

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]