1. GPCR/G Protein
    Neuronal Signaling
    Immunology/Inflammation
  2. Histamine Receptor
  3. (R)-(-)-α-Methylhistamine dihydrobromide

(R)-(-)-α-Methylhistamine dihydrobromide 

Cat. No.: HY-100999
Handling Instructions

(R)-(-)-α-Methylhistamine dihydrobromide is a potent and selective H3 histamine receptor agonist with a Kd of 50.3 nM. (R)-(-)-α-Methylhistamine dihydrobromide can cross the blood-brain barrier, and can enhance memory retention, attenuates memory impairment in rats.

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(R)-(-)-α-Methylhistamine dihydrobromide Chemical Structure

(R)-(-)-α-Methylhistamine dihydrobromide Chemical Structure

CAS No. : 868698-49-1

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Description

(R)-(-)-α-Methylhistamine dihydrobromide is a potent and selective H3 histamine receptor agonist with a Kd of 50.3 nM[1][2]. (R)-(-)-α-Methylhistamine dihydrobromide can cross the blood-brain barrier, and can enhance memory retention, attenuates memory impairment in rats[3][4][5].

IC50 & Target[1][2]

H3 Receptor

50.3 nM (Kd)

In Vitro

(R)-(-)-α-Methylhistamine dihydrobromide is an H3-agonist that is > 10 times as potent as histamine (HA). Its selectivity toward H3-receptors is > 1,000 times as high as that of HA. (R)-(-)-α-Methylhistamine dihydrobromide has only weak affinities for H1 and H2 receptor with a pKi=4.8 and < 3.5, repectively. (R)-(-)-α-Methylhistamine dihydrobromide displays >200-fold selectivity over H4 receptors[1][2][3].

In Vivo

Pretreatment with (R)-(-)-α-Methylhistamine dihydrobromide (RAMH; 10 mg/kg; i.p.; 60 min before training) reverses propofol‐induced (25 mg/kg; i.p.; 30 min before training) memory retention[5].
(R)-alpha-Methylhistamine dihydrochloride (6.3 mg/kg; i.p.) significantly decreases the steady-state t-MH level in the mouse brain, whereas these compounds produced no significant changes in the HA level[3].

Animal Model: Male Sprague‐Dawley rats (10-12 week)[3]
Dosage: 10 mg/kg
Administration: IP; 60 min before training
Result: Reversed propofol‐induced memory retention.
Molecular Weight

287.00

Formula

C₆H₁₃Br₂N₃

CAS No.

868698-49-1

SMILES

C[[email protected]@H](N)CC1=CN=CN1.Br.Br

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

(R)-(-)-α-Methylhistamine dihydrobromideHistamine Receptorblood-brainbarriermemoryretentionimpairmentH1H4H2histamineRAMHInhibitorinhibitorinhibit

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(R)-(-)-α-Methylhistamine dihydrobromide
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