Acute intravenous injection toxicity study of IBZM and BZM in rats.
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 microg/kg and BZM at dose levels of 250 and 1250 microg/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 microg/kg and the total body weight gains of both IBZM treated groups were significantly higher than the control group (p < 0.05).
Institute of Nuclear Energy Research, Atomic Energy Council, Tauyuan, Taiwan. asyang@iner.gov.tw
An-Shoei
AS
Yang
Tung-Chuan
TC
Chiang
Fu-Fa
FF
Hsu
Mei-Hsiu
MH
Liao
Lie-Hang
LH
Shen
D000818:Animals; D001549:Benzamides / Q000008:administration & dosage / Q000633:toxicity*; D001835:Body Weight / Q000187:drug effects; D003287:Contrast Media / Q000008:administration & dosage / Q000633:toxicity*; D018492:Dopamine Antagonists / Q000008:administration & dosage / Q000633:toxicity*; D005260:Female; D007275:Injections, Intravenous; D008297:Male; D011759:Pyrrolidines / Q000008:administration & dosage / Q000633:toxicity*; D051381:Rats; D017207:Rats, Sprague-Dawley; D013997:Time Factors; D023382:Toxicity Tests, Acute
D001549:Benzamides; D003287:Contrast Media; D018492:Dopamine Antagonists; C534457:N-(1-ethyl-2-pyrrolidinyl)methyl-2-hydroxy-6-methoxybenzamide; D011759:Pyrrolidines; C055743:3-iodo-2-hydroxy-6-methoxy-N-((1-ethyl-2-pyrrolidinyl)methyl)benzamide