- Molecular Weight : 222.5 Da.
- Melting Point : 154-155 °C
- Solubility in : Soluble in water and ethanol; practically not in chloroform and benzene.
- Purity min. : 98% TLC [silufol, chloroform, methanol (5:1)].
- Physical Form : white crystal powder.
- Chemical Name : 2,3,4,10-tetrahydro-1H-pyrido[2,1-b] quinazoline hydrochloride.
- 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.
- Toxicity (LD50) : mice (i.v.): 45.4 mg/kg.
mice (i.p.): 121.4 mg/kg.
- Storage recommendations : store at +4°C, in dark place.
- CAS Reg. No. : 212607-49-3
- Bibliography :
- 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
- Spath et al., "Uber Derivate des Peganins und ihre Ring-Homologen" J. Mitt. Uber Peganin, Chem. Ber. 6 (1935). (68):2221-2226
- 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
- Tuliaganov, Higher Doctoral thesis of Medecine, Moscow (1981) (Russian). Confidential.
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