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

Cat. No.: HY-100999: Data Sheet
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(R)-(-)-α-Methylhistamine dihydrobromide is a potent, selective and brain-penetrant agonist of H3 histamine receptor, with a K_d 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 화학구조

CAS No. : 868698-49-1

사이즈	가격	재고
5 mg		Ask For Quote & Lead Time
10 mg		Ask For Quote & Lead Time
25 mg		Ask For Quote & Lead Time

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

This product is a controlled substance and not for sale in your territory.

Other In-stock Forms of (R)-(-)-α-Methylhistamine dihydrobromide:

(R)-(-)-α-Methylhistamine dihydrochloride

Other Forms of (R)-(-)-α-Methylhistamine dihydrobromide:

(R)-(-)-α-Methylhistamine dihydrochloride In-stock

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Biological Activity
순도&문서
References
고객리뷰

제품 설명

(R)-(-)-α-Methylhistamine dihydrobromide 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 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 pK_i=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.

분자량

287.00

화학식

C₆H₁₃Br₂N₃

CAS No.

868698-49-1

Appearance

Oil

Color

Brown to reddish brown

SMILES

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

선적

Room temperature in continental US; may vary elsewhere.

보관

4°C, protect from light, stored under nitrogen

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

순도&문서

Purity: ≥98.0%

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Data Sheet (277 KB) SDS (252 KB)

COA (255 KB) HNMR (294 KB) LCMS (158 KB)

Handling Instructions (2659 KB)

References

[1]. Arrang JM, et al. Highly potent and selective ligands for histamine H3-receptors. Nature. 1987 May 14-20;327(6118):117-23. [Content Brief]

[2]. Mohammad Shahid, et al. Histamine, Histamine Receptors, and their Role in Immunomodulation: An Updated Systematic Review. The Open Immunology Journal, 2009, 2, 9-41.

[3]. Oishi R, et al. Effects of the histamine H3-agonist (R)-alpha-methylhistamine and the antagonist thioperamideon histamine metabolism in the mouse and rat brain. J Neurochem. 1989 May;52(5):1388-92. [Content Brief]

[4]. Yamasaki S, et al. The disposition of (R)-alpha-methylhistamine, a histamine H3-receptor agonist, in rats. J Pharm Pharmacol. 1994 May;46(5):371-4. [Content Brief]

[5]. Li WW, et al. (R)-alpha-methylhistamine suppresses inhibitory neurotransmission in hippocampal CA1 pyramidal neurons counteracting propofol-induced amnesia in rats. CNS Neurosci Ther. 2014 Sep;20(9):851-9. [Content Brief]