PMID- 1826785
OWN - NLM
STAT- MEDLINE
DCOM- 19910523
LR  - 20220311
IS  - 0091-3057 (Print)
IS  - 0091-3057 (Linking)
VI  - 38
IP  - 1
DP  - 1991 Jan
TI  - 5-Iodo-2-aminoindan, a nonneurotoxic analogue of p-iodoamphetamine.
PG  - 135-9
AB  - A rigid analogue, 5-iodo-2-aminoindan (5-IAI), of the serotonin neurotoxic 
      halogenated amphetamine p-iodoamphetamine (PIA) was pharmacologically evaluated 
      for production of serotonin neurotoxicity. A comparison was also made between 
      5-IAI and PIA in the two-lever drug discrimination paradigm in rats trained to 
      discriminate saline from 3,4-methylenedioxymethamphetamine (MDMA) or saline from 
      the alpha-ethyl homologue of MDMA, MBDB. PIA and 5-IAI were both behaviorally 
      active, and fully substituted in both groups of animals, but were considerably 
      less potent than p-chloroamphetamine (PCA). PIA had about twice the potency of 
      PCA as an inhibitor of [3H]-5-HT uptake in rat brain cortical synaptosomes, while 
      5-IAI was only about 75% as potent as PCA in this assay. A single 40 mg/kg dose 
      of PIA resulted in a 40% reduction of 5-HT and 5-HIAA levels and in the number of 
      5-HT uptake sites in rat cortex at one week sacrifice. The same dose of 5-IAI 
      with one week sacrifice led to about a 15% decrease in 5-HIAA levels and number 
      of 5-HT uptake sites, but only the latter was statistically significant. In rat 
      hippocampus, PIA gave significant decreases in all serotonin markers examined, 
      while 5-IAI slightly but significantly decreased only 5-HT levels. Neither 
      compound produced any change in catecholamine or catecholamine metabolite levels. 
      The results confirm earlier reports of the selective serotonin neurotoxicity of 
      PIA, which is less severe than that of PCA, and also demonstrate that its rigid 
      analogue 5-IAI does not appear to cause significant serotonin deficits in the 
      rat.
FAU - Nichols, D E
AU  - Nichols DE
AD  - Department of Medicinal Chemistry and Pharmacognosy, School of Pharmacyand 
      Pharmacal Sciences, Purdue University, West Lafayette, IN 47907.
FAU - Johnson, M P
AU  - Johnson MP
FAU - Oberlender, R
AU  - Oberlender R
LA  - eng
GR  - DA-04578/DA/NIDA NIH HHS/United States
PT  - Journal Article
PT  - Research Support, U.S. Gov't, P.H.S.
PL  - United States
TA  - Pharmacol Biochem Behav
JT  - Pharmacology, biochemistry, and behavior
JID - 0367050
RN  - 0 (Amphetamines)
RN  - 0 (Indans)
RN  - 0 (Iodine Radioisotopes)
RN  - 0 (Piperidines)
RN  - 21894-72-4 (4-iodoamphetamine)
RN  - 41VRH5220H (Paroxetine)
RN  - 64-12-0 (p-Chloroamphetamine)
RN  - 7X16E45Y1X (5-iodo-2-aminoindan)
SB  - IM
MH  - Amphetamines/*pharmacology
MH  - Animals
MH  - Autoradiography
MH  - Binding, Competitive/drug effects
MH  - Brain/anatomy & histology
MH  - Brain Chemistry/drug effects
MH  - Chromatography, High Pressure Liquid
MH  - Conditioning, Operant/drug effects
MH  - Discrimination, Psychological/drug effects
MH  - Dose-Response Relationship, Drug
MH  - Electrochemistry
MH  - Indans/*pharmacology
MH  - Iodine Radioisotopes
MH  - Male
MH  - Paroxetine
MH  - Piperidines/metabolism
MH  - Rats
MH  - Rats, Inbred Strains
MH  - p-Chloroamphetamine/metabolism
EDAT- 1991/01/01 00:00
MHDA- 1991/01/01 00:01
CRDT- 1991/01/01 00:00
PHST- 1991/01/01 00:00 [pubmed]
PHST- 1991/01/01 00:01 [medline]
PHST- 1991/01/01 00:00 [entrez]
AID - 0091-3057(91)90601-W [pii]
AID - 10.1016/0091-3057(91)90601-w [doi]
PST - ppublish
SO  - Pharmacol Biochem Behav. 1991 Jan;38(1):135-9. doi: 10.1016/0091-3057(91)90601-w.