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Impentamine dihydrobromide

Selective H3 antagonist CAS# 149629-70-9

Impentamine dihydrobromide

Catalog No. BCC7197----Order now to get a substantial discount!

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Chemical structure

Impentamine dihydrobromide

3D structure

Chemical Properties of Impentamine dihydrobromide

Cas No. 149629-70-9 SDF Download SDF
PubChem ID 53439849 Appearance Powder
Formula C8H17Br2N3 M.Wt 315.05
Type of Compound N/A Storage Desiccate at -20°C
Synonyms VUF 4702
Solubility Soluble to 100 mM in water and to 100 mM in DMSO
Chemical Name 5-(1H-imidazol-5-yl)pentan-1-amine;dihydrobromide
SMILES C1=C(NC=N1)CCCCCN.Br.Br
Standard InChIKey QSDXAAWBBPWGEL-UHFFFAOYSA-N
Standard InChI InChI=1S/C8H15N3.2BrH/c9-5-3-1-2-4-8-6-10-7-11-8;;/h6-7H,1-5,9H2,(H,10,11);2*1H
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Impentamine dihydrobromide

DescriptionPotent and highly selective histamine H3 receptor antagonist (pA2 = 8.4); displays > 30000-fold selectivity over H1 and H2 receptors. Can act as a partial agonist in SK-N-MC cells expressing human H3 receptors. Produces antinociception, possibly via a non-H1, -H2 or -H3 receptor-mediated mechanism, following central administration in vivo.

Impentamine dihydrobromide Dilution Calculator

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Preparing Stock Solutions of Impentamine dihydrobromide

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.1741 mL 15.8705 mL 31.741 mL 63.482 mL 79.3525 mL
5 mM 0.6348 mL 3.1741 mL 6.3482 mL 12.6964 mL 15.8705 mL
10 mM 0.3174 mL 1.587 mL 3.1741 mL 6.3482 mL 7.9352 mL
50 mM 0.0635 mL 0.3174 mL 0.6348 mL 1.2696 mL 1.587 mL
100 mM 0.0317 mL 0.1587 mL 0.3174 mL 0.6348 mL 0.7935 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on Impentamine dihydrobromide

Constitutive activity of histamine h(3) receptors stably expressed in SK-N-MC cells: display of agonism and inverse agonism by H(3) antagonists.[Pubmed:11714875]

J Pharmacol Exp Ther. 2001 Dec;299(3):908-14.

Agonist-independent activity of G-protein-coupled receptor, also referred to as constitutive activity, is a well-documented phenomenon and has been reported recently for both the histamine H(1) and H(2) receptors. Using SK-N-MC cell lines stably expressing the human and rat H(3) receptors at physiological receptor densities (500-600 fmol/mg of protein), we show that both the rat and human H(3) receptors show a high degree of constitutive activity. The forskolin-mediated cAMP production in SK-N-MC cells is inhibited strongly upon expression of the G(i)-coupled H(3) receptor. The cAMP production can be further inhibited upon agonist stimulation of the H(3) receptor and can be enhanced by a variety of H(3) antagonists acting as inverse agonists at the H(3) receptor. Thioperamide, clobenpropit, and iodophenpropit raise the cAMP levels in SK-N-MC cells with potencies that match their receptor binding affinities. Surprisingly, impentamine and burimamide act as effective H(3) agonists. Modification of the amine group of impentamine dramatically affected the pharmacological activity of the ligand. Receptor affinity was reduced slightly for most impentamine analogs, but the functional activity of the ligands varied from agonist to neutral antagonist and inverse agonist, indicating that subtle changes in the chemical structures of impentamine analogs have major impact on the (de)activation steps of the H(3) receptor. In conclusion, upon stable expression of the rat and human H(3) receptor in SK-N-MC cells constitutive receptor activity is detected. In this experimental system, H(3) receptors ligands, previously identified as H(3) antagonists, cover the whole spectrum of pharmacological activities, ranging from full inverse agonists to agonists.

Antinociceptive activity of impentamine, a histamine congener, after CNS administration.[Pubmed:10072195]

Life Sci. 1999;64(5):PL79-86.

The brain neuromodulator histamine induces antinociception when administered directly into the rodent CNS. However, several compounds derived from H2 and H3 antagonists also produce antinociception after central administration. Pharmacological studies have shown that a prototype of these agents, improgan, induces analgesia that is not mediated by actions on known histamine receptors. Presently, the antinociceptive properties of a compound that chemically resembles both improgan and histamine were investigated in rats. Intraventricular (i.v.t.) administration of impentamine (4-imidazolylpentylamine) induced reversible, near-maximal antinociception on the hot plate and tail flick tests (15 microg, 98 nmol). The dose-response function was extremely steep, however, since other doses showed either no effect or behavioral toxicity. On the tail flick test, impentamine antinociception was resistant to antagonism by blockers of H1, H2, or H3 receptors, similar to characteristics previously found for improgan. In contrast, histamine antinociception was highly attenuated by H1 and H2 antagonists. These findings suggest that: 1) the histamine congener impentamine may induce antinociception by a mechanism similar to that produced by improgan, and 2) additional histamine receptors may be discovered that are linked to pain-attenuating processes.

Homologs of histamine as histamine H3 receptor antagonists: a new potent and selective H3 antagonist, 4(5)-(5-aminopentyl)-1H-imidazole.[Pubmed:7830269]

J Med Chem. 1995 Jan 20;38(2):266-71.

The influence of alkyl chain length variation on the histamine H3 receptor activity of histamine homologs 1 was investigated. A series of 4(5)-(omega-aminoalkyl)-1H-imidazoles 1 was prepared with an alkyl chain length varying from one methylene group to 10 methylene groups. Besides the H3 activity, the affinities of these compounds for the H1 and H2 receptors were determined. The ethylene chain of histamine is optimal for agonistic activity on all three histamine receptor subtypes. For the H3 receptor, elongation of the alkyl chain from three methylene groups on leads to compounds with antagonistic properties. 4(5)-(5-Aminopentyl)-1H-imidazole (impentamine, 1e) is the most potent and selective H3 antagonist from this series of 4(5)-(omega-aminoalkyl)-1H-imidazoles 1, with a pA2 value of 8.4 (on guinea pig jejunum). A specific antagonistic binding site for this compound is proposed.

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