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Mequitazine

pharmaceutical raw materials
Mequitazine structure

Mequitazine 

structure
  • CAS No:

    29216-28-2

  • Formula:

    C20H22N2S

  • Chemical Name:

    Mequitazine

  • Synonyms:

    10H-Phenothiazine,10-(1-azabicyclo[2.2.2]oct-3-ylmethyl)-;Phenothiazine,10-(3-quinuclidinylmethyl)-;10-(1-Azabicyclo[2.2.2]oct-3-ylmethyl)-10H-phenothiazine;LM 209;Mequitazine;Nipolazin;Mircol;Metaplexan;Zesulan;Primalan;Butix;NSC 303612;Quitadrill;10-(1-Azabicyclo[2.2.2]octan-3-ylmethyl)phenothiazine;10-(Quinuclidin-3-ylmethyl)phenothiazine

  • Categories:

    Active Pharmaceutical Ingredients  >  Antiallergic Drugs

Description

Mequitazine is a potent, nonsedative and long-acting histamine H1 antagonist.


Solid


Mequitazine is a member of phenothiazines.|Mequitazine is a histamine H1 antagonist (antihistamine). It competes with histamine for the normal H1-receptor sites on effector cells of the gastrointestinal tract, blood vessels and respiratory tract. It provides effective, temporary relief of sneezing, watery and itchy eyes, and runny nose due to hay fever and other upper respiratory allergies.

Mequitazine Basic Attributes

322.47

322.47

249-521-7

303612

DTXSID8023262

R - Respiratory system

2934300000

Characteristics

31.8

4.7

Solid

1.3±0.1 g/cm3

130.5 °C

469.4±24.0 °C at 760 mmHg

237.7±22.9 °C

1.707

>48.4 [ug/mL]

Refrigerator

Safety Information

6.1

UN 2811 6.1/PG III

SP5080000

P261, P264, P270, P271, P272, P273, P280, P301+P310, P301+P312, P302+P352, P304+P312, P304+P340, P305+P351+P338, P310, P312, P321, P322, P330, P332+P313, P333+P313, P362, P363, P391, P405, P501

H301

|Danger|H301 (60%): Toxic if swallowed [Danger Acute toxicity, oral]|P261, P264, P270, P271, P272, P273, P280, P301+P310, P301+P312, P302+P352, P304+P312, P304+P340, P305+P351+P338, P310, P312, P321, P322, P330, P332+P313, P333+P313, P362, P363, P391, P405, and P501|Aggregated GHS information provided by 5 companies from 3 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Drug Information

For the treatment of Hay fever, urticaria (hives) and allergic rhinitis

In allergic reactions an allergen interacts with and cross-links surface IgE antibodies on mast cells and basophils. Once the mast cell-antibody-antigen complex is formed, a complex series of events occurs that eventually leads to cell-degranulation and the release of histamine (and other chemical mediators) from the mast cell or basophil. Once released, histamine can react with local or widespread tissues through histamine receptors. Histamine, acting on H1-receptors, produces pruritis, vasodilatation, hypotension, flushing, headache, tachycardia, and bronchoconstriction. Histamine also increases vascular permeability and potentiates pain. Mequitazine is a histamine H1 antagonist. It competes with histamine for the normal H1-receptor sites on effector cells of the gastrointestinal tract, blood vessels and respiratory tract. It provides effective, temporary relief of sneezing, watery and itchy eyes, and runny nose due to hay fever and other upper respiratory allergies.

Drugs that selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine. Included here are the classical antihistaminics that antagonize or prevent the action of histamine mainly in immediate hypersensitivity. They act in the bronchi, capillaries, and some other smooth muscles, and are used to prevent or allay motion sickness, seasonal rhinitis, and allergic dermatitis and to induce somnolence. The effects of blocking central nervous system H1 receptors are not as well understood. (See all compounds classified as Histamine H1 Antagonists.)

Mequitazine binds to the histamine H1 receptor sites on effector cells in the gastrointestinal tract, blood vessels, and respiratory tract. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine.

3-methylquinuclidinyl-10-phenothiazine

Mequitazine Use and Manufacturing

It is an antihistamine

Computed Properties

Molecular Weight:322.5
XLogP3:4.6
Hydrogen Bond Acceptor Count:3
Rotatable Bond Count:2
Exact Mass:322.15036988
Monoisotopic Mass:322.15036988
Topological Polar Surface Area:31.8
Heavy Atom Count:23
Complexity:398
Undefined Atom Stereocenter Count:1
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

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