CAS 86-22-6|brompheniramine

Introduction：Basic information about CAS 86-22-6|brompheniramine, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. brompheniramine BiologicalActivity
3. Chemical & Physical Properties
4. Synonyms

Common Name	brompheniramine
CAS Number	86-22-6	Molecular Weight	319.23900
Density	1.265 g/cm3	Boiling Point	403ºC at 760 mmHg
Molecular Formula	C₁₆H₁₉BrN₂	Melting Point	/
MSDS	/	Flash Point	197.5ºC

Names

Name	brompheniramine
Synonym	More Synonyms

brompheniramine BiologicalActivity

Description	Brompheniramine ((±)-Brompheniramine) is a potent and orally active antihistamine of the alkylamine class. Brompheniramine is a selective histamine H1 receptor antagonist with a Kd of 6.06 nM. Brompheniramine can block the hERG channels, calcium channels, and sodium channels with IC50s of 0.90 μM, 16.12 μM and 21.26 μM, respectively. Brompheniramine has anticholinergic, antidepressant and anesthetic properties and can be used for allergic rhinitis research[1][2][3][4].
Related Catalog	Signaling Pathways >>Membrane Transporter/Ion Channel >>Sodium ChannelSignaling Pathways >>Membrane Transporter/Ion Channel >>Calcium ChannelSignaling Pathways >>Neuronal Signaling >>mAChRSignaling Pathways >>Immunology/Inflammation >>Histamine ReceptorResearch Areas >>EndocrinologySignaling Pathways >>GPCR/G Protein >>mAChRResearch Areas >>Inflammation/ImmunologyResearch Areas >>Neurological DiseaseSignaling Pathways >>Membrane Transporter/Ion Channel >>Potassium ChannelSignaling Pathways >>GPCR/G Protein >>Histamine Receptor
In Vitro	Brompheniramine (0.1-100 μM) blocks hERG K+ channels expressed in CHO cells in a concentration-dependent manner with an IC50 of 0.90±0.14 μM, and reduced peak tail current amplitude measured at -60 mV (cells are depolarized for 2 s to +20 mV from a holding potential of -80 mV followed by a 3s repolarization back to -60 mV)[3]. Brompheniramine (1, 10 and 100 μM) significantly shortens the APD50 and depresses the plateau phase on the action potential in guinea pig papillary muscle, as well as slightly prolongs the APD90 in guinea pig papillary muscle at 10 and 100 μM[3]. Brompheniramine (0.1-100 μM) inhibit the amplitude of the Ca2+ channel currents in rat ventricular myocytes by 14.1±1.1, 31.1±5.8, 38.0±3.8 and 90.2±3.7% at 0.1, 1, 10 and 100 μM, respectively[3]. Brompheniramine blocks muscarinic cholinergic receptors in human chinese hamster ovary (CHO) cells[4].
In Vivo	Brompheniramine (0.3-3 μM; SC, single dosage) induces cutaneous analgesia in rats[1]. Animal Model: Male Sprague-Dawley rats[1] Dosage: 0.3, 0.6, 1.1, 1.5 and 3.0  μM Administration: SC, single dosage Result: Provoked cutaneous analgesia in a dose-dependent manner, with an EC50 value of 0.66 μM, and induced prolonged analgesic duration.
References	[1]. Chong-Chi Chiu, et al. Subcutaneous brompheniramine for cutaneous analgesia in rats. Eur J Pharmacol. 2019 Oct 5;860:172544. [2]. B Cusack, et al. Binding of antidepressants to human brain receptors: focus on newer generation compounds. Psychopharmacology (Berl). 1994 May;114(4):559-65. [3]. Shin WH, Kim KS, Kim EJ. Electrophysiological effects of brompheniramine on cardiac ion channels and action potential. Pharmacol Res. 2006 Dec;54(6):414-20. [4]. Yasuda SU, Yasuda RP. Affinities of brompheniramine, chlorpheniramine, and terfenadine at the five human muscarinic cholinergic receptor subtypes. Pharmacotherapy. 1999 Apr;19(4):447-51.

Chemical & Physical Properties

Density	1.265 g/cm3
Boiling Point	403ºC at 760 mmHg
Molecular Formula	C₁₆H₁₉BrN₂
Molecular Weight	319.23900
Flash Point	197.5ºC
Exact Mass	318.07300
PSA	16.13000
LogP	3.92770
Index of Refraction	1.577
InChIKey	ZDIGNSYAACHWNL-UHFFFAOYSA-N
SMILES	CN(C)CCC(c1ccc(Br)cc1)c1ccccn1
Storage condition	2-8°C

Synonyms

Brompheniramine

MFCD00865691

EINECS 201-657-8

(+/-)-1-(4-bromophenyl)-1-(2-pyridyl)-3-dimethylaminopropane

(±)-brompheniramine

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