• Blockade
  • Blockade of the 5-HT2A receptor may also play a role in its effectiveness against positive symptoms, though the significance of this property in antipsychotic drugs is still debated among researchers. (wikipedia.org)
  • In mildly asthmatic subjects, cetirizine hydrochloride at 5 to 20 mg blocked bronchoconstriction due to nebulized histamine, with virtually total blockade after a 20 mg dose. (imen.info)
  • There is increasing interest in antipsychotics intended to manage positive symptoms via D 2 receptor blockade and improve negative symptoms and cognitive deficits via 5-HT 1A activation. (springer.com)
  • e.g., parkinsonism, dystonia, akathisia, and tardive dyskinesia) that are thought to reflect blockade of D 2 receptors in the basal ganglia ( Casey, 1996 ). (aspetjournals.org)
  • pharmacological
  • This study aims to review pharmacological literature on compounds interacting at both 5-HT 1A and D 2 receptors (as well as at other receptors), including aripiprazole, perospirone, ziprasidone, bifeprunox, lurasidone and cariprazine, PF-217830, adoprazine, SSR181507, and F15063. (springer.com)
  • vivo
  • Amargos-Bosch M, Bortolozzi A, Puig MV, Serrats J, Adell A, Celada P, Toth M, Mengod G, Artigas F (2004) Co-expression and in vivo interaction of serotonin1A and serotonin2A receptors in pyramidal neurons of prefrontal cortex. (springer.com)
  • In vivo experimentation confirmed the antihistaminic and antiallergic activity, which was at least comparable to that of other second-generation H1-antihistamines such as cetirizine. (wikipedia.org)
  • neurotransmitter
  • Acetylcholine (often abbreviated ACh) is a neurotransmitter whose receptor is a protein found in synapses and other cell membranes. (wikipedia.org)
  • Besides responding to their primary neurochemical, neurotransmitter receptors can be sensitive to a variety of other molecules. (wikipedia.org)
  • vitro
  • Cariprazine forms two major metabolites, desmethyl cariprazine (DCAR) and didesmethyl cariprazine (DDCAR), that have in vitro receptor binding profiles similar to the parent drug. (drugbank.ca)
  • Topical ocular administration of emedastine inhibits histamine-stimulated vascular permeability in the conjunctiva as a concentration-dependent manner in in vitro study. (wikipedia.org)
  • cetirizine
  • The effects of intradermal injection of various other mediators or histamine releasers were also inhibited by cetirizine, as was response to a cold challenge in patients with cold-induced urticaria. (imen.info)
  • In different murine models, bilastine by oral route, antagonizes the effects of histamine in a dose-dependent manner, with potency similar to that of cetirizine and between 5.5 and 10 times greater than that of fexofenadine. (wikipedia.org)
  • Clinical studies using different dosages were done on histamine-induced wheal and flare reaction over a 24-h period, compared with a single 10-mg oral dose of cetirizine. (wikipedia.org)
  • The results of this research indicated that bilastine was at least as efficient as cetirizine in reducing histamine-mediated effects in healthy volunteers. (wikipedia.org)
  • activity
  • Nevertheless, further investigations are necessary to evaluate recent compounds, notably in view of their differing levels of 5-HT 1A affinity and efficacy, which can markedly influence activity and side-effect profiles. (springer.com)
  • Thiothixene blocks postsynaptic dopamine receptors in the mesolimbic system and medullary chemoreceptor trigger zone, thereby decreasing dopamine activity leading to decreased stimulation of the vomiting center and psychotic effects, such as hallucinations and delusions. (healthmatics.info)
  • potency
  • I have been surprised while doing this update of quetiapine that none of the papers I have reviewed even mention, never mind discuss, its H1 potency: we certainly are living in the 'post-truth' era! (psychotropical.info)
  • Here is the seminal paper linking weight gain and H1 potency from Solomon Snyder's lab (1), and others (2-4). (psychotropical.info)