Acute Intravenous Injection Toxicity Study of IBZM and BZM in Rats

• Published in: Drug and chemical toxicology (New York, N.Y. 1978) Vol. 31; no. 4; pp. 529 - 533
• Main Authors: Yang, An-Shoei, Chiang, Tung-Chuan, Hsu, Fu-Fa, Liao, Mei-Hsiu, Shen, Lie-Hang
• Format: Journal Article
• Language: English
• Published: New York, NY Informa UK Ltd 01.01.2008; Taylor & Francis; Informa Healthcare
• Subjects: [123I]IBZM; Animals; Benzamide; Benzamides - administration & dosage; Benzamides - toxicity; Biological and medical sciences; Body Weight - drug effects; CNS D2 Dopamine receptor; Contrast Media - administration & dosage; Contrast Media - toxicity; Dopamine Antagonists - administration & dosage; Dopamine Antagonists - toxicity; Drug toxicity and drugs side effects treatment; Female; Injections, Intravenous; Male; Medical sciences; Miscellaneous (drug allergy, mutagens, teratogens...); Pharmacology. Drug treatments; Pyrrolidines - administration & dosage; Pyrrolidines - toxicity; Rats; Rats, Sprague-Dawley; Time Factors; Toxicity Tests, Acute; Nuclear medicine; Intravenous administration; Rat; Toxicity; Acute; Rodentia; Injection; Benzamide; IBZM; Vertebrata; Mammalia; D2 Dopamine receptor; CNS D2 Dopamine receptor; Animal; Benzamide derivatives; Medical imagery; Computerized axial tomography
• ISSN: 0148-0545; 1525-6014
• DOI: 10.1080/01480540802393332

S-3-iodo-N-(1-ethyl-2-pyrrolidinyl)methyl-2-hydroxy-6-methoxybenzamide (IBZM) is one of the several benzamide derivatives showing a high affinity for the central nervous system (CNS) D2 dopamine receptor. Carrier-free [123I]IBZM is potentially useful as a nuclear medicine imaging agent for investigating the CNS D2 dopamine receptor in humans. This study describes the acute toxicity of IBZM and S-N-(1-ethyl-2-pyrrolidinyl)methyl-2-hydroxy-6-methoxybenzamide (BZM) in the rats. Treated rats were administered with IBZM at dose levels of 1 and 5 μg kg and BZM at dose levels of 250 and 1250 μg kg with dose volumes of 1 and 5 mL kg. The control rats were administered 5 mL kg of vehicle control. The rats were observed for 14 days. Observations included general demeanor, clinical signs, mortality, body weights total body weight gains, and gross necropsy findings. None of the animals died during the 14-day study period. In female rats, the body weight gained at the first week of BZM treatment at a dose level of 1250 μg kg and the total body weight gains of both IBZM treated groups were significantly higher than the control group (p < 0.05).