*  Psychopharmakotherapie | Metabolische Nebenwirkungen von Psychopharmaka | springermedizin.de
H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs. ... Eating disorder and epilepsy in mice lacking 5-HT2c serotonin receptors. Nature 1995 Apr 6;374(6522):542-546. CrossRefPubMed ... Ratliff J, Barber J, Palmese L, Reutenauer E, Tek C. Association of prescription H1 antihistamine use with obesity: Results ... Association study of GABAA alpha2 receptor subunit gene variants in antipsychotic-associated weight gain. J Clin ...
  https://www.springermedizin.de/psychopharmakotherapie/metabolische-nebenwirkungen-von-psychopharmaka/12126810
*  Influence of glycosylation inhibitors on dihydropyridine binding to cardiac cells | Springer for Research & Development
Mitsuhashi M, Payan DG: Receptor glycosylation regulates the affinity of histamine H1 receptors during smooth muscle cell ... calcium channel glycosylation inhibitor cultured cardiac cells dihydropyridine receptors glycoproteins This is a preview of ... Jorgensen AO, Shen ACY, Arnold W, Mcpherson PS, Campbell KP: The Ca2+-release channel/ryanodine receptor is localized in ... Jorgensen AO, Shen AC, Arnold W, Leung AT, Campbell KP: Subcellular distribution of the 1,4-dihydropyridine receptor in rabbit ...
  https://rd.springer.com/chapter/10.1007/978-1-4613-1279-6_6
*  Ziprasidone - Wikipedia
... of the dopamine and serotonin receptors and the α1-adrenergic receptor are high and its affinity for the histamine H1 receptor ... "H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs". ... Ziprasidone is a full antagonist of D2 receptors and of 5-HT2A receptors and is a partial agonist of 5-HT1A receptors and a ... Kongsamut S, Kang J, Chen XL, Roehr J, Rampe D (2002). "A comparison of the receptor binding and HERG channel affinities for a ...
  https://en.wikipedia.org/wiki/Ziprasidone
*  Olanzapine - Wikipedia
... due to its high affinity for the D1 receptor over the D2 receptor. Antagonizing H1 histamine receptors causes sedation and may ... "H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs". ... Olanzapine has a higher affinity for 5-HT2A serotonin receptors than D2 dopamine receptors, which is a common property of most ... histamine H1 and alpha 1-adrenergic receptors in vitro". Schizophr. Res. 37 (1): 107-22. doi:10.1016/s0920-9964(98)00146-7. ...
  https://en.wikipedia.org/wiki/Olanzapine
*  Muscarinic antagonist - Wikipedia
"H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs". ... Krystal AD, Richelson E, Roth T (2013). "Review of the histamine system and the clinical effects of H1 antagonists: basis for a ... Bymaster FP, Falcone JF (2000). "Decreased binding affinity of olanzapine and clozapine for human muscarinic receptors in ... "Affinity profiles of various muscarinic antagonists for cloned human muscarinic acetylcholine receptor (mAChR) subtypes and ...
  https://en.wikipedia.org/wiki/Muscarinic_antagonist
*  Tiotixene - Wikipedia
... subnanomolar affinity). It is also an antagonist of the histamine H1, α1-adrenergic, and serotonin 5-HT7 receptors (low ... "H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs". ... Kanba S, Richelson E (1984). "Histamine H1 receptors in human brain labelled with [3H]doxepin". Brain Res. 304 (1): 1-7. PMID ... I. Muscarinic M3 receptor binding affinity could predict the risk of antipsychotics to induce type 2 diabetes". Methods Find ...
  https://en.wikipedia.org/wiki/Tiotixene
*  Aripiprazole - Wikipedia
"H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs". ... The drug differs from other atypical antipsychotics in having higher affinity for the D2 receptor than for the 5-HT2A receptor ... such as the histamine H1, α-adrenergic, and dopamine D4 receptors as well as the serotonin transporter, while it has negligible ... Aripiprazole is also a partial agonist of the D3 receptor. In healthy human volunteers, D2 and D3 receptor occupancy levels are ...
  https://en.wikipedia.org/wiki/Aripiprazole
*  Purchase Cetirizine Online - Retail Price For Cetirizine - Pharmacies Cetirizine
Cetirizine has high affinity for histamine H1-receptors. It has less affinity, however, than terfenadine or hydroxyzine for ... Histamine and 5-hydroxytryptamine serotonin and their antagonists. In: Gilman AG, Goodman LS, Rall TW et al eds. Take ... Sedating H1-blockers: Dry mouth, drowsiness and other antihistamine-related side effects may occur in patients receiving ... In both atopic and normal human volunteers, cetirizine reduction of histamine wheal and flare is similar to that of clemastine ...
  http://cetirizine.imen.info
*  Lifestyle Intervention and Metformin for Treatment of Antipsychotic-Induced Weight Gain: A Randomized Controlled Trial |...
H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs. ... H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs. ... Matsui-Sakata AOhtani HSawada Y Receptor occupancy-based analysis of the contribution of various receptors to antipsychotic- ... Matsui-Sakata AOhtani HSawada Y Receptor occupancy-based analysis of the contribution of various receptors to antipsychotic- ...
  https://jamanetwork.com/journals/jama/fullarticle/1380162
*  Comparative pharmacology of antipsychotics possessing combined dopamine D2and serotonin 5-HT1Areceptor properties | SpringerLink
There is increasing interest in antipsychotics intended to manage positive symptoms via D2 receptor blockade and improve ... H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs. ... role of 5-HT2C and histamine H1 receptors. Psychopharmacol Berl 207:119-125Google Scholar ... I. In vitro receptor affinity and efficacy profile. Br J Pharmacol 151:237-252PubMedGoogle Scholar ...
  https://link.springer.com/article/10.1007%2Fs00213-011-2247-y
*  Allergic eye disease mechanisms | British Journal of Ophthalmology
99 has a high speed binding affinity for histamine H1 receptors, but does not interact with cholinergic receptors100-102 and ... Oral histamine H1 receptor antagonists (antihistamines) such as astemizole, terfanidine, and loratidine have been shown to be ... Evaluation in the histamine and compound 48/80 models of ocular allergy in humans. Ophthalmology 95:1494-1497. ... 1987) Non IgE dependent bacteria induced histamine release from human lung and tonsillar mast cells. Clin Allergy 17:341-353. ...
  http://bjo.bmj.com/content/82/10/1203
*  Mirtazapine: dubious and misleading evidence - Psychotropical
Kroeze, WK, et al., H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs ... The most potent property of both drugs is histamine receptor H1 antagonism, which has been shown to be strongly associated with ... The weight of current evidence concerning the receptor affinity for A2 receptors is that it is the same for both drugs, or that ... The key observation is that, paradoxically, MIRT is less potent at A2 receptors. This result contradicts what is required by ...
  https://psychotropical.info/mirtazapine-dubious-evidence/
*  Quetiapine: The miracle of Seroquel - Psychotropical
4. Kroeze, WK, Hufeisen, SJ, Popadak, BA, Renock, SM, et al., H1-histamine receptor affinity predicts short-term weight gain ... 2. Salvi, V, Mencacci, C, and Barone-Adesi, F, H1-histamine receptor affinity predicts weight gain with antidepressants. Eur. ... Antipsychotic drug-induced weight gain mediated by histamine H1 receptor-linked activation of hypothalamic AMP-kinase. Proc ... especially dopamine D2 receptors and 5-HT2A receptors. If only partial blockade of dopamine receptors is part of the secret ...
  https://psychotropical.info/quetiapine-the-miracle-of-seroquel/
*  P&G, Somaxon deploy reps and e-detailing for Silenor launch - Medical Marketing and Media
"Silenor has high affinity for the histamine H1 receptor and though the exact mechanism by which it works to promote sleep is ... it is believed to work by antagonism of the H1 receptor - a different mechanism than other currently available insomnia ...
  http://www.mmm-online.com/channel/pg-somaxon-deploy-reps-and-e-detailing-for-silenor-launch/article/179820/
*  Amesergide - Wikipedia
It has negligible affinity for the histamine H1 and muscarinic acetylcholine receptors (Ki > 10,000 nM). The drug does not ... Amesergide also has affinity for the serotonin 5-HT1D receptor (Ki = 57.9 nM) and lower affinity for the serotonin 5-HT1A, α1- ... Cushing DJ, Zgombick JM, Nelson DL, Cohen ML (1996). "LY215840, a high-affinity 5-HT7 receptor ligand, blocks serotonin-induced ... It is also an antagonist of the serotonin 5-HT7 receptor with relatively lower affinity (Ki = 78.0 nM). The drug is a potent ...
  https://en.wikipedia.org/wiki/Amesergide
*  Protocols and Video Articles Authored by Eva Wagner
... a H1R antagonist shows high affinity to the histamine H1 receptor but only a moderate affinity to the histamine H4 receptor. ... modify the astemizole to keep high affinity to the histamine H1 receptor and to increase affinity to the histamine H4 receptor ... The new compounds show affinity to the histamine H1 receptor in the pK i range from 5.3 to 8.8, whereas the affinity of these ... Pharmacological Profile of Astemizole-derived Compounds at the Histamine H1 and H4 Receptor--H1/H4 Receptor Selectivity Naunyn- ...
  https://www.jove.com/author/Eva_Wagner
*  Lurasidone - Wikipedia
The drug also has negligible affinity for the histamine H1 receptor and the muscarinic acetylcholine receptors, and hence has ... It has only low and likely clinically unimportant affinity for the serotonin 5-HT2C receptor, which may underlie its low ... Lurasidone acts as an antagonist of the dopamine D2 and D3 receptors, the serotonin 5-HT2A and 5-HT7 receptors, and the α2C- ... adrenergic receptor, and as a partial agonist of the serotonin 5-HT1A receptor. ...
  https://en.wikipedia.org/wiki/Lurasidone
*  Nefazodone - Wikipedia
It has low but potentially significant affinity for the histamine H1 receptor, where it is an antagonist, and hence may have ... It also has high affinity for the α1-adrenergic receptor and serotonin 5-HT1A receptor, and relatively lower affinity for the ... α2-adrenergic receptor and dopamine D2 receptor. Nefazodone has low but significant affinity for the serotonin, norepinephrine ... due to its combined actions as a potent serotonin 5-HT2A receptor and 5-HT2C receptor antagonist and weak serotonin- ...
  https://en.wikipedia.org/wiki/Nefazodone
*  Cariprazine - DrugBank
... with high selectivity towards the D3 receptor. This mechanism is relatively unique, since many other antipsychotics are D2 and ... Cariprazine acts as a D2 and D3 receptor partial agonist, ... affinity as well as it binds to the histamine H1 receptors. ... Histamine receptor activity. Specific Function. In peripheral tissues, the H1 subclass of histamine receptors mediates the ... Cariprazine shows lower binding affinity to the serotonin 5- HT2C and α1A- adrenergic receptors and has no appreciable affinity ...
  https://www.drugbank.ca/drugs/DB06016
*  Iloperidone - Wikipedia
... and low affinity for the serotonin 5HT1A (168 nM), dopamine D1 and histamine H1 receptors. In addition, pharmacogenomic studies ... Iloperidone has been shown to act as an antagonist at all tested receptors. It exhibits high (nM) affinity to serotonin 5HT2A ( ... Ki value of 5.6 nM), dopamine D2 (6.3 nM) and D3 (7.1 nM) and noradrenaline α1 receptors (0.36 nM), moderate affinity for ... It is considered an 'atypical' antipsychotic because it displays serotonin receptor antagonism, similar to other atypical ...
  https://en.wikipedia.org/wiki/Iloperidone
*  Lirias: Genomic cloning, heterologous expression and pharmacological characterization of a human histamine H1 receptor
Binding affinities of histamine and known histamine antagonists were similar to those for histamine H1 receptors in guinea-pig ... A human histamine H1 receptor gene lacking introns was isolated by screening a human genomic library with a bovine histamine H1 ... Genomic cloning, heterologous expression and pharmacological characterization of a human histamine H1 receptor. ... The deduced protein of 487 amino acids showed characteristic properties of G-protein-coupled receptors. The coding region was ...
  https://lirias.kuleuven.be/handle/123456789/343909
*  Genomics Meets Histamine Receptors: New Subtypes, New Receptors | Molecular Pharmacology
1989) High affinity, saturable [3H]mepyramine binding sites on rat liver plasma membrane do not represent histamine H1- ... 1994) Does the [3H]mepyramine binding site represent the histamine H1 receptor? Re-examination of the histamine H1 receptor ... researchers in this field knew of the existence of only three histamine receptors (H1, H2, and H3). But histamine receptors are ... unknown histamine receptors. Although the new H4work accounts for the existence of some novel histamine receptors previously ...
  http://molpharm.aspetjournals.org/content/59/3/415
*  Tricyclic antidepressant - Wikipedia
The TCAs also have varying but typically high affinity for antagonising the H1 and H2 histamine receptors, as well as the ... The binding profiles of various TCAs and some metabolites in terms of their affinities (Ki, nM) for various receptors and ... Tsai BS, Yellin TO (November 1984). "Differences in the interaction of histamine H2 receptor antagonists and tricyclic ... and NMDA receptors, and as agonists at the sigma receptors (σ1 and σ2), some of which may contribute to their therapeutic ...
  https://en.wikipedia.org/wiki/Tricyclic_antidepressant
*  Bilastine - Wikipedia
... demonstrate the affinity and specificity of bilastine for histamine H1-receptors compared with other histamine receptors ... Bilastine binds to guinea-pig cerebellar histamine H1-receptors (Ki=44 nM) and to human recombinant histamine H1-receptors (Ki= ... a new selective histamine H1 receptor antagonist: Receptor selectivity and in vitro antihistaminic activity". Drugs in R&D. 6 ( ... a new selective histamine H1 receptor antagonist. Receptor selectivity and in vitro antihistaminic activity". Drugs RD. 6 (6): ...
  https://en.wikipedia.org/wiki/Bilastine
*  Pharmacological Profile of Lurasidone, a Novel Antipsychotic Agent with Potent 5-Hydroxytryptamine 7 (5-HT7) and 5-HT1A...
2003) H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs. ... Affinity for noradrenaline α1, α2A, and 5-HT2C receptors was weak, whereas affinity for histamine H1 and muscarinic ... that lurasidone has relatively low affinity for noradrenergic α1 receptor or negligible affinity for histamine H1 receptor. ... and olanzapine and clozapine have significant binding affinity for the muscarinic receptor. Histamine H1 receptor blockade has ...
  http://jpet.aspetjournals.org/content/334/1/171.long