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Histamine Receptor Inhibitors

We now offer a broad range of Histamine Receptor Inhibitors. Histamine is an inflammatory mediator that is ubiquitously expressed and has a broad range of pharmacologic effects. The effects of histamine are mediated by a family of G protein-coupled receptors, the Histamine H1, H2, H3 and H4 Receptors. Histamine Receptor Inhibitors offered by Santa Cruz inhibit Histamine Receptor and, in some cases, other inflammation and immune response related proteins. View detailed Histamine Receptor Inhibitor specifications, including Histamine Receptor Inhibitor CAS number, molecular weight, molecular formula and chemical structure, by linking to the specific product blocks.

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For functional analysis of Histamine Receptor Inhibitors, see our complete listing of Histamine Receptor Antibodies.


PRODUCT NAMECATALOG #DESCRIPTIONCITATIONSRANKING
Azelastine HClsc-201096Azelastine HCl is an H1-receptor antagonist with associated antiallergic activity. Azelastine HCl is also shown to block the secretion of IL-6, IL-8, and TNF alpha from mast cells. CAS # 79307-93-0

Antazoline hydrochloridesc-203515Imidazoline binding site ligand; a potent inducer of insulin secretion in rat pancreas and also an antihistamine. CAS # 2508-72-7

A 943931 dihydrochloridesc-291775A 943931 dihydrochloride is a potent and selective histamine H4 receptor antagonist (pKi values are 7.15 and 8.12 at human and rat receptors respectively).

A 987306sc-291776A 987306 is a potent histamine H4 receptor antagonist. CAS # 1082954-71-9

Aminopotentidinesc-203817A very potent and specific histamine H2-receptor antagonist. CAS # 140873-26-3

Astemizolesc-201088Astemizole is a potent antihistamine (H1-receptor antagonist) that displays selectivity for H1 receptors over 5-HT, dopamine and muscarinic acetylcholine receptors. CAS # 68844-77-9

Brompheniramine Maleatesc-210967Brompheniramine Maleate is a histamine H1 receptors antagonist. Brompheniramine Maleate also functions as a moderately effective anticholinergic agent. CAS # 980-71-2

Burimamide oxalatesc-203535Burimamide oxalate is a mixed Histamine H3 Receptor and Histamine H2 Receptor( H2/H3) antagonist. In SK-N-MC cells, this compound displays partial agonist activity. CAS # 34970-69-9

GT 2016sc-362740GT 2016 is a high affinity H3 receptor antagonist (Ki = 43.8 nM). This compound displays selectivity against H1 and H2 receptors. CAS # 152241-24-2

Cetirizine Dihydrochloridesc-202992Cetirizine is a caarboxylated metabolite of hydroxyzine that acts as a racemic selective Histamine H1 receptor inverse agonist. CAS # 83881-52-1

Cimetidinesc-202996Cimetidine is an immunomodulator and a histamine congener. Cimetidine competitively inhibits histamine binding to histamine H2 receptors, and suppresses the growth of several tumors. CAS # 51481-61-9

Clemastine fumaratesc-203897Clemastine fumarate is a selective histamine H1 antagonist that inhibits histamine induced rise in [Ca2+]i in HL-60 cells. CAS # 14976-57-9

Clobenpropit Dihydrobromide, VUF 9153sc-202999Clobenpropit dihydrobromide, VUF 9153 has been shown to be an extremely potent (pA2 = 9.93) and selective histamine H3 receptor antagonist. CAS # 145231-45-4

Carcinine ditrifluoroacetatesc-361133Carcinine ditrifluoroacetate is an extremely selective H3 receptor antagonist. CAS # 56897-53-1

Clobenpropit hydrobromidesc-205258Clobenpropit hydrobromide is a selective histamine H3 receptor antagonist that crosses the blood-brain barrier, inhibiting histamine binding in rat brain. CAS # 145231-35-2

Conessinesc-203554Conessine is a selective and potent histamine H3 receptor antagonist (pKi values are 7.61 and 8.27 at rat and human H3 receptors respectively). A steroidal alkaloid which displays in vitro antiplasmodial activity (IC50 = 1.04 μM). High affinity for α2C adrenoceptors (pKi = 7.98). CAS # 546-06-5

Dimebolin dihydrochloridesc-294348Dimebolin dihydrochloride is a histamine receptor inhibitor, AR inhibitor, and calcium channel protein inhibitor. CAS # 97657-92-6

Asenapine maleatesc-361110Asenapine maleate is an antagonist of noradrenalin, dopamine, 5-HT and histamine receptor subtypes. CAS # 65576-45-6

Doxepin hydrochloridesc-203930Doxepin hydrochloride is a highly potent histamine H1 antagonist. Doxepin hydrochloride also binds to histamine H4 receptor. CAS # 1229-29-4

ICI 162,846sc-361207ICI 162,846 has been shown to be a potent histamine H2 receptor antagonist. CAS # 84545-30-2

Lidocainesc-204056Lidocaine is a selective inverse peripheral histamine H1-receptor agonist. Lidocaine is also an anasthetic and class Ib antiarrhythmic agent. CAS # 137-58-6

Impentamine dihydrobromidesc-203604Impentamine dihydrobromide is a selective H3 receptor antagonist. This compound displays >30000-fold selectivity over H1 and H2 receptors. In SK-N-MC cells expressing human H3 receptors, this can act as a partial agonist. CAS # 34973-91-6

Iodophenpropit dihydrobromidesc-361213Iodophenpropit dihydrobromide has been reported to be an antagonist of histamine H3 (KD = 0.3 nM). CAS # 143407-29-8

JNJ 10191584 maleatesc-203613JNJ 10191584 maleate is a highly selective histamine H4 receptor silent antagonist that binds with high affinity to the human H4 receptor (Ki = 26 nM). This compound is > 540-fold selective over the H3 receptor (Ki = 14.1 μM). CAS # 869497-75-6

Ketotifen fumaratesc-201094Ketotifen fumarate is a histamine H1 antagonist and inhibitor of mast cell growth. Ketotifen fumarate is also an inhibitor of vascular permeability and conjuctival edema. CAS # 34580-14-8

Mepyramine maleatesc-203629Mepyramine is a histamine H1 receptor antagonist and binds with high affinity to G(q/11) protein. CAS # 59-33-6

Diphenhydramine hydrochloridesc-204729Diphenhydramine hydrochloride blocks the effect of histamine at H1 receptor sites, has been shown to have inhibitive tumor promotion properties, and decreases peripheral nociceptors sensitization. CAS # 147-24-0

Cyproheptadine hydrochloridesc-203557Migraine prophylactic and Non-selective 5HT2 antagonist. CAS # 969-33-5

Ranitidinesc-203679Ranitidine is a potent, selective and competitive histamine H2 receptor antagonist which mediates gastric secretion. CAS # 66357-35-5

ROS 234 dioxalatesc-204893ROS 234 dioxalate is a potent H3 antagonist. CAS # 184576-87-2

Fananserinsc-203951Fananserin is a potent serotonin SR-2A and dopamine D4 antagonist, with efficacy against histamine H1, α1 and SR-1A. CAS # 127625-29-0

Thioperamide·maleatesc-201092Thioperamide·maleate is a selective histamine H3 receptor antagonist that has been shown to cross the blood-brain barrier. This compound binds to rat cerebral cortical cells in vitro, has a pKi value of 8.4. CAS # 106243-16-7

trans-Triprolidine hydrochloridesc-204354trans-Triprolidine hydrochloride is a potent H1 receptor antagonist. CAS # 6138-79-0

VUF 5681 dihydrobromidesc-204389VUF 5681 dihydrobromide is a potent histamine H3 receptor silent antagonist (pKi = 8.35). CAS # 639089-06-8

Zolantidine dimaleatesc-364691Zolantidine dimaleate is a selective, potent and penetrating H2 receptor antagonist. CAS # 104076-38-2

(S)-(+)-Dimethindene maleatesc-361329(S)-(+)-Dimethindene maleate has been shown to be an enantiomer that is a subtype-selective mAChR M2 antagonist as well as a histamine H1 receptor antagonist. CAS # 121367-05-3

Zotepinesc-360895Zotepine is a SR-2A and D2DR inhibitor (Ki values are 0.69 and 2.3 nM respectively). Zotepine is also a potent histamine H1 receptor antagonist (IC50 = 8.0 nM). CAS # 26615-21-4

Mirtazapinesc-204088Mirtazapine is a potent SR-2 and SR-3 antagonist. In addition, it is a moderately potent α2 adrenoceptor and histamine H1-antagonist. CAS # 85650-52-8

2'-O-(tert-Butyldimethylsilyl)-6,7-dehydropaclitaxelsc-206548 CAS # 165065-02-1

Meclizine Dihydrochloridesc-211779Meclizine Dihydrochloride is a pregnane X receptor (PXR) agonist and histamine H1 receptor antagonist. CAS # 1104-22-9

Olopatadine Hydrochloridesc-212473Olopatadine Hydrochloride CAS # 140462-76-6

Terfenadinesc-208421Terfenadine is a histamine H1-receptor antagonist, which blocks HERG and KATP (KIR6) channels. CAS # 50679-08-8

BF 2649sc-361119BF 2649 has been shown to be a histamine H3 receptor antagonist and inverse agonist. CAS # 903576-44-3

JNJ 10181457 dihydrochloridesc-361216JNJ 10181457 dihydrochloride has been shown to be a membrane permeable histamine H3 receptor antagonist. CAS # 544707-19-9