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

(R)-(-)-α-Methylhistamine dihydrobromide is a potent, selective and brain-penetrant agonist of H3 histamine receptor, with a Kd of 50.3 nM. (R)-(-)-α-Methylhistamine dihydrobromide 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, selective and brain-penetrant agonist of H3 histamine receptor, with a Kd of 50.3 nM[1][2]. (R)-(-)-α-Methylhistamine dihydrobromide 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 >1000 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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)-(-)-α-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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Appearance

Oil

Color

Brown to reddish brown

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Purity & Documentation
References
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(R)-(-)-α-Methylhistamine dihydrobromide Related Classifications

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Help & FAQs
  • How should lyophilized recombinant proteins be reconstituted and stored?

    1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss. 2. Taking 10 μg as an example, first add 20 μL of reconstituted solution provided by MCE and use a pipette to gently resuspend the lyophilized protein until it is fully dissolved.. (For most proteins, the reconstitution solution we provide is sterile water. If a diluent other than water is required, it will be indicated in the product's Certificate of Analysis (COA).). 3. Add an additional 80 μL of buffer/culture medium containing carrier protein (either 0.1% BSA, 5% HSA, 10% FBS, or 5% trehalose), and then use a pipette to gently mix until uniform. The final concentration is should not be lower than 100 μg/mL. 4. Aliquot at least 20 μL per tube. 5. After aliquoting, store it frozen at a temperature ranging from -20ºC to -80ºC, and it can be preserved for 3 to 6 months.

  • How should solution-form recombinant proteins be stored?

    1. The product can be stored in its original form and diluted as needed upon use. 2. Alternatively, dilute with a buffer/culture medium containing a carrier protein (either 0.1% BSA, 5% HSA, 10% FBS, or 5% alginate), mix well by pipetting, and ensure that

  • Why is it necessary to add carrier proteins?

    Carrier proteins are commonly added to enhance the stability of recombinant proteins, preventing them from adhering to the walls of the container during freezing or thawing processes. Plastic tubes have a certain adsorptive capacity for proteins, which may lead to difficulty in separating the protein from the tube walls, resulting in a decrease in the actual concentration of the protein in the solution and thus affecting its activity. To minimize such losses, it is recommended to add a commonly used carrier protein solution prior to the long-term storage of recombinant protein products.

  • Carrier protein types and options?

    In cases where the carrier protein is not expected to influence the experimental outcomes, an appropriate carrier protein, such as 0.1% BSA (Bovine Serum Albumin), 5% HSA (Human Serum Albumin), 10% FBS (Fetal Bovine Serum), or 5% trehalose, can be incorpo

Keywords:

(R)-(-)-α-Methylhistamine dihydrobromide868698-49-1Histamine Receptorblood-brainbarriermemoryretentionimpairmentH1H4H2histamineRAMHInhibitorinhibitorinhibit

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