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Description
Biochem/physiol Actions
CAS Number
Product #
(R)(−)-α-
Methylhistamine dihydrochloride solid, ≥98% (HPLC)
Potent, selective H
3
histamine receptor agonist which crosses the blood-brain barrier; inhibits histamine synthesis and release.
75614-89-0
H128
1-Methylhistamine dihydrochloride ≥98% (TLC), powder
Major metabolite of histamine by histamine N-methyltransferase.
6481-48-7
M4910
2-((3-
Trifluoromethyl)phenyl)histamine dimaleate ≥98% (HPLC), solid
2-((3-Trifluoromethyl)phenyl)histamine dimaleate was found to be the most potent and selective H
1
histamine receptor agonist of a panel of compounds in functional in vitro studies on histamine H
2
, H
3
, and other neurotransmitter receptors. It showed better potency at the guinea pig H
1
histamine receptor than at the human H
1
histamine receptor (pKi : 5.9). The selectivity of 2-((3-Trifluoromethyl)phenyl)histamine dimaleate was found to be 2138 (H
1
:H
2
), > 64 (H
1
:H
3
), 1000 (H
1
:M
3
), 105 (H
1
: a
1
), 708 (H
1
:ß
1
), and 71 (H
1
:5HT
2A
). 2-((3-Trifluoromethyl)phenyl)histamine dimaleate does not cross the blood-brain barrier.
162049-83-4
T4951
Amthamine dihydrobromide ≥98% (HPLC), solid
Amthamine dihydrobromide is a H
2
histamine receptor agonist. Amthamine dihydrobromide, similar to histamine, inhibits H
2
receptor-mediated eosinophil peroxidase (EPO) release with IC
50
= 0.4 μM; a weak antagonist at H
3
and shows no activity at H
1
receptors.
142457-00-9
A4730
Desloratadine powder, ≥98% (HPLC)
Desloratadine is a a selective and nonsedating histamine H1 receptor antagonist, an active metabolite of loratadine (Claritin), used to relieve hay fever and allergy symptoms with less drowsiness than other antihistamines; does not significantly inhibits cardiac K+ channels at clinically achievable blood levels. Free from antimuscarinic/anticholinergic effects.
100643-71-8
D1069
Histamine bisphosphate monohydrate
51-74-1
H7375
Histamine dihydrochloride ≥99% (TLC), powder
Endogenous H
1
and H
2
histamine receptor agonist; H
1
activation mobilizes Ca
2+
; H
2
activation stimulates adenylate cyclase activity in neurons; activates nitric oxide synthetase; potent vasodilator.
56-92-8
H7250
Histamine ≥97.0%
Endogenous H
1
and H
2
histamine receptor agonist; H
1
activation mobilizes Ca
2+
; H
2
activation stimulates adenylate cyclase activity in neurons; activates nitric oxide synthetase; potent vasodilator.
51-45-6
H7125
Imetit dihydrobromide solid, ≥98% (HPLC)
Potent and selective H
3
histamine receptor agonist.
32385-58-3
I135
Immepip dihydrobromide ≥98% (HPLC), solid
Immepip is a H
3
and H
4
histamine receptor agonist. Immepip is a selective H
3
agonist equipotent to (R)-α-methylhistamine and also effective
in vitro
and
in vivo
. It is devoid of side activities elicited at H
1
and α
2
receptors and 5-HT3 receptors.
164391-47-3
I4034
Immethridine hydrobromide ≥98% (HPLC), solid
Potent, highly selective H
3
histamine receptor agonist
87976-03-2
I1909
N-Methylhistaprodifen dioxalate salt ≥98% (HPLC), solid
N-methylhistaprodifen is more potent than histamine by a factor of 3.5 on guinea pig ileum; more potent than histamine by a factor of 4.3 on guinea pig arterial H
1
-receptor-mediated vasoconstriction; most potent H
1
-receptor agonist on the guinea pig ileum out of 17 agonists tested. pEC
50
= 7.24 in contraction of guinea pig ileal whole segments; pEC
50
= 6.31 in contraction of guinea pig aortic segments. N-methylhistaprodifen does not stimulate H
2
and H
3
histamine receptors; potential use in the study of H
1
-receptor-mediated physiological and pathophysiological functions.
270079-48-6
M7320
N
α
-
Methylhistamine dihydrochloride solid
Production of N-alpha-methyl-histamine (NAMH), a histamine H(3) receptor (H3R) agonist, is promoted in
Helicobacter pylori
infected human gastric mucosa. NAMH acts directly on histamine H(2) receptors (H2Rs) in animals to stimulate acid secretion and to be a H2R agonist. NAMH dose dependently stimulated cAMP productions in CHO-H2R cells. This production was inhibited by famotidine but not by thioperamide. Control CHO cells were unresponsive to either histamine or NAMH. In addition, the effect of NAMH, in terms of cAMP production in CHO-H2R cells, was more potent than that of histamine-that is, with a lower EC
50
concentration and higher maximal cAMP production. Both NAMH and histamine, but not R-alpha-methyl-histamine, effectively inhibited [(3)H] tiotidine binding to CHO-H2R cells. These results confirm that NAMH, which is produced in the gastric mucosa by H pylori, is a potent H2R agonist as well as a H3R agonist.
16503-22-3
H5914
S15535 ≥98% (HPLC), solid
Potent, orally active, partial 5-HT
1A
receptor agonist
146998-34-7
S5321
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