[CAS NO. 75614-89-0] (R)-(-)-α-Methylhistamine dihydrochloride

Name: (R)-(-)-α-Methylhistamine dihydrochloride
Brand: Arctom Scientific
SKU: HY-W014941

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PRODUCTS SPECIFICATIONS [75614-89-0]

Distributor

Catalog

HY-W014941

Brand

MCE

CAS

75614-89-0

DESCRIPTION [75614-89-0]

Overview

MDL	MFCD00083176
Molecular Weight	198.09
Molecular Formula	C6H13Cl2N3
SMILES	[H]Cl.[H]Cl.C[C@@H](N)CC1=CN=CN1

For research use only. We do not sell to patients.

Summary

(R)-(-)-α-Methylhistamine dihydrochloride is a potent, selective and brain-penetrant agonist of H3 histamine receptor, with a K _d of 50.3 nM ^[1] ^[2] . (R)-(-)-α-Methylhistamine dihydrochloride can enhance memory retention, attenuates memory impairment in rats ^[3] ^[4] ^[5] .

IC50 & Target

H ₃ Receptor

50.3 nM (Kd)

In Vitro

(R)-(-)-α-Methylhistamine dihydrochloride 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 dihydrochloride has only weak affinities for H1 and H2 receptor with a pK _i =4.8 and <3.5, repectively. (R)-(-)-α-Methylhistamine dihydrochloride displays >200-fold selectivity over H4 receptors ^[1] ^[2] ^[3] .

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

In Vivo

Pretreatment with (R)-(-)-α-Methylhistamine dihydrochloride (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] .

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.

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 250 mg/mL ( 1262.05 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	5.0482 mL	25.2411 mL	50.4821 mL
5 mM	1.0096 mL	5.0482 mL	10.0964 mL
10 mM	0.5048 mL	2.5241 mL	5.0482 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.08 mg/mL (10.50 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (10.50 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.08 mg/mL (10.50 mM); Clear solution

* All of the co-solvents are available by MCE.