The activity of 12 human and guinea pig histamine H1-receptor agonists are investigated computationally. The mapped electrostatic potentials on the molecular surfaces of each of the structures are analyzed at HF/3-21G level of theory to identify any common features that possibly relate to their subsequent agonistic activities. Statistically derived quantities including potential’s minima VS,min...

Cyclizine (1-benzhydryl-4-methyl-piperazine, CAS 82-92-8, CYC, I), a piperazine derivative, belongs to H1 antihistamine group of drugs that shows such pharmacological properties as anti-inflammatory, anti-allergic and anti-platelet effects, similar to other H1-receptor antagonists. In this study, two new tolyl and cumene derivatives of I (1-ethyl-4-[(p-isopropylphenyl) (p-tolyl) methyl]-piperaz...

OBJECTIVE(S) The present study investigated the effects of microinjection of histamine and histamine H1, H2, and H3 receptor antagonists, chlorpheniramine, ranitidine and thioperamide, respectively into the primary somatosensory cortex (PSC) on inflammatory pain. MATERIAL AND METHODS Two stainless steel guide canulas were bilaterally implanted into the PSC of anaesthetized rats. Inflammatory ...

Numerous "antihistamines" as well as various psychotropic medications with antihistamine properties are widely utilized to treat insomnia. Over-the-counter sleep aids usually contain an antihistamine and various antidepressants and antipsychotics with antihistamine properties have sedative-hypnotic actions. Although widely used for the treatment of insomnia, many agents that block the histamine...

Histamine mediates its physiological function through binding to four known histamine receptors. Here, we describe the first selective antagonist of the histamine H4 receptor, the newest member of the histamine receptor family, and provide evidence that such antagonists have anti-inflammatory activity in vivo. 1-[(5-chloro-1H-indol-2-yl)carbonyl]-4-methylpiperazine (JNJ 7777120) has a K(i) of 4...

the aim of this study was to assess the effects of exogenous histamine and h1 and h2 central receptorson electrocardiographic (ecg) parameters, heart rate and mean electrical axis in broiler chickens. for thispurpose, ross broiler chickens (750-800 g weight) received intracerebroventricularly (icv) histamine.moreover, to determine the receptors involved in histamine-induced alterations in ecg c...

Bunium persicum (Boiss.) is an economically important medicinal plant growing wildly in arid regions in Iran. The fruit of B. persicum is widely used in traditional Iranian medicine to control colic pain and dysmenorrhoea. The aim of the current study was to determine antinociceptive mechanisms of B. persicum essential oil using an acetic acid-induced writhing test as a model of visceral pain a...