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 ǰȳ  Ű   Pharmacology

Histamine Small Molecules

Histamine receptor õ small molecule ȳմϴ.

TOCRIS
ǰ ϱ
μϱ




Agonists
Cat. No. Product Name / Activity
3545 Histamine dihydrochloride
Endogenous histamine receptor agonist
0646 HTMT dimaleate
H1/ H2 agonist
2478 2-Pyridylethylamine dihydrochloride
H1 agonist
Inverse Agonists
Cat. No. Product Name / Activity
0660 Mepyramine maleate
Selective H1 inverse agonist
Antagonists
Cat. No. Product Name / Activity
3489 Astemizole
Orally active, potent H1 antagonist; also KV11.1 (hERG) channel blocker
2577 Cetirizine dihydrochloride
Selective H1 antagonist
1453 Clemastine fumarate
H1 antagonist
5371 Clemizole hydrochloride
Histamine H1 antagonist; also TRPC5 blocker
5958 Desloratadine
High affinity H1 antagonist; anti-inflammatory
1425 (S)-(+)-Dimethindene maleate
H1 antagonist. Also M2 muscarinic antagonist
3072 Diphenhydramine hydrochloride
H1 antagonist
2429 Fexofenadine hydrochloride
H1 receptor antagonist; non-sedating antiallergic agent
0784 Ketotifen fumarate
H1 antagonist
1944 Loratidine
Peripheral H1 antagonist; antiallergic agent
4245 Meclizine dihydrochloride
H1 antagonist; human pregnane X receptor agonist
2018 Mirtazapine
Potent H1 antagonist; also 5-HT2, 5-HT3 and α2 antagonist; antidepressant
4241 Olopatadine hydrochloride
H1 antagonist; ocular antiallergic agent
3948 Terfenadine
H1 antagonist. Also KV11.1 (hERG) and Kir6 (KATP) channel blocker
0662 trans-Triprolidine hydrochloride
Highly potent H1 antagonist
3996 Zotepine
Potent H1 antagonist; also 5-HT2A and D2 antagonist; atypical antipsychotic



Agonists
Cat. No. Product Name / Activity
0668 Amthamine dihydrobromide
Highly selective standard H2 agonist
0506 Dimaprit dihydrochloride
Standard H2 selective agonist
3545 Histamine dihydrochloride
Endogenous histamine receptor agonist
0646 HTMT dimaleate
H2/ H1 agonist
Antagonists
Cat. No. Product Name / Activity
0721 Aminopotentidine
H2 antagonist
0902 Cimetidine
H2 antagonist, I1 agonist
0833 ICI 162,846
Potent H2 antagonist, active in vivo
1967 Ranitidine hydrochloride
Selective H2 antagonist
0826 Tiotidine
Potent and selective H2 antagonist
1070 Zolantidine dimaleate
Potent, centrally active H2 antagonist


Agonists
Cat. No. Product Name / Activity
3545 Histamine dihydrochloride
Endogenous histamine receptor agonist
0729 Imetit dihydrobromide
Standard H3 and H4 agonist (H3 > H4)
0932 Immepip dihydrobromide
Standard H3 agonist. Also H4 agonist
2315 Immethridine dihydrobromide
Potent H3 agonist, highly selective over H4
0569 (R)-(-)-α-Methylhistamine dihydrobromide
Potent, standard H3 agonist
0572 (S)-(+)-α-Methylhistamine dihydrobromide
H3 agonist, less active enantiomer
0573 Nα-Methylhistamine dihydrochloride
Non-selective H3 agonist
2477 Proxyfan oxalate
High affinity H3 ligand
Inverse Agonists
Cat. No. Product Name / Activity
3743 BF 2649 hydrochloride
Potent and selective H3 inverse agonist
Antagonists
Cat. No. Product Name / Activity
4697 A 331440 dihydrochloride
Selective H3 antagonist
2211 Carcinine ditrifluoroacetate
Highly selective H3 antagonist
0752 Clobenpropit dihydrobromide
Highly potent H3 antagonist and H4 partial agonist
2419 GT 2016
Selective H3 antagonist
1858 Impentamine dihydrobromide
Selective H3 antagonist
0779 Iodophenpropit dihydrobromide
Potent, selective H3 antagonist
4019 JNJ 10181457 dihydrochloride
H3 antagonist
4020 JNJ 5207852 dihydrochloride
High affinity H3 antagonist
2034 ROS 234 dioxalate
Potent H3 antagonist
6778 S 38093
Selective H3 antagonist and inverse agonist; also σ1 receptor antagonist; antinociceptive
4441 SEN 12333
Histamine H3 antagonist; also α7 nAChR agonist
0644 Thioperamide
H3 antagonist; also H4 inverse agonist
2493 VUF 5681 dihydrobromide
Potent H3 receptor silent antagonist


Agonists
Cat. No. Product Name / Activity
0752 Clobenpropit dihydrobromide
H4 partial agonist and H3 antagonist
3545 Histamine dihydrochloride
Endogenous histamine agonist
0729 Imetit dihydrobromide
Standard H3 and H4 agonist
0932 Immepip dihydrobromide
H4 and H3 agonist
2342 4-Methylhistamine dihydrochloride
Selective, high affinity H4 agonist
4769 VUF 10460
Selective H4 agonist
2494 VUF 8430 dihydrobromide
Potent and high affinity H4 agonist
Inverse Agonists
Cat. No. Product Name / Activity
0644 Thioperamide
H4 inverse agonist; also H3 antagonist
Antagonists
Cat. No. Product Name / Activity
3753 A 943931 dihydrochloride
Potent and selective H4 antagonist
3640 A 987306
Potent and selective H4 antagonist
2441 JNJ 10191584 maleate
Selective H4 antagonist; orally active
6279 JNJ 39758979 dihydrochloride
High affinity and selective histamine H4 antagonist; orally bioavailable
4021 JNJ 7777120
Selective H4 antagonist