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Home Page > Alphabetical Index > TETRAZOLINE HCl

TETRAZOLINE HCl Prod. No L6217 - CAS # 212607-49-3
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Product Name TETRAZOLINE HCl
Product Code L6217
TETRAZOLINE HCl

C12H14N2.HCl
Molecular Formula C12H14N2.HCl
Description

Cholinesterase and monoamine oxidase (MAO) inhibitor; weak muscarinic receptors antagonist.

Quinazoline alkaloid C12H14N2.HCl ‚ synthetic.
 
Biological Activity

In vitro: IC50 = 9.7x10-7 g/ml for cholinesterase activity. In vivo: half LD50 (i.p. mice) dose blocks 52% of cholinesterase activity.

In vitro: 10-4 M result in 42.6 % inhibition of MAO activity‚ 10-3 M: 54%.
In isolated small intestine section‚ 10-6 g/ml and 10-5 g/ml moderately increase the contractions caused by ACh. On the contrary‚ contractions are inhibited by 10-4 g/ml. In consequence‚ Tetrazoline HCl is a blocker of muscarinic cholinoreceptors located in isolated small intestine section. This explains its muscle relaxant effect. 100-130 mg/kg (i.p.) in mice cause breathing disruption then death by asphyxia.

It has no significant effect on cholinoreceptors of the C.N.S. It does not prolong the quiver caused by arecholine‚ but doubles this caused by nicotine.
 
Chemical and Physical Properties
 
CAS No. 212607-49-3 Molecular Weight 222.5 Da.
RTECS Physical Form white crystal powder.
Merck Index No (13th Ed.) Melting point 154-155 °C
PubChem SID Solubility Soluble in water and ethanol; practically not in chloroform and benzene.
Purity 98% TLC [silufol‚ chloroform‚ methanol (5:1)]. Optical Activity no optical activity.
Toxicity (LD50) mice (i.v.): 45.4 mg/kg.
mice (i.p.): 121.4 mg/kg.
Chemical Names 2‚3‚4‚10-tetrahydro-1H-pyrido[2‚1-b] quinazoline hydrochloride.
Storage & Reconstitution Recommendations store at +4°C‚ in dark place.
Safety Recommendations
 
Bibliographic References
  1. Fitzgerald et al., "6, 7, 8, 9-tetrahydropyrido-quinazoline, a new class of alkaloids from Mackinlava species (Araliaceae)" Aust. J. Chem. (1966). 19(1):151-159
  2. Spath et al., "Uber Derivate des Peganins und ihre Ring-Homologen" J. Mitt. Uber Peganin, Chem. Ber. 6 (1935). (68):2221-2226
  3. Jen et al., "A new class of antihypertensive agents, 1, 2, 3, 5-Tetrahydroimidazo [2,1-b] quinazoline." J. Med. Chem.1 (1972). 15(7):727-731
  4. Tuliaganov, Higher Doctoral thesis of Medecine, Moscow (1981) (Russian). Confidential.
 
Prices
Code
Quantity
US $
€uro
L6217
20 mg
130.20
93.00
100 mg
520.80
372.00
 
External Links PubMed Biomedical Citations From PubMed Toxicology Citations From PubMed PubChem SID

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