Ionamin online research references
Int J Nucl Med Biol. 1985;12(4):321-5.
Preparation and evaluation of 3-[125I]iodo-4-aminophentermine as a brain perfusion imaging agent. Comparison with labeled phentermine derivatives.
Hanson RN, Jones GS Jr, Franke L, Kizuka H, Elmaleh DR.
A radioiodinated derivative of the anorexinergic drug phentermine was synthesized and evaluated as a potential brain imaging agent. Stoichiometric iodination of the intermediate 4-aminophentermine (AmP) gave a mixture of mono and diiodo products, while the radioiodination at the no-carrier-added (NCA) level gave 73% isolated yield of the 3-[125I]iodo-4-aminophentermine with less than 2% of the diiodo derivative. The tissue distribution of the radiochemical in rats showed that it was readily extracted by the brain followed by relatively slow clearance from that organ. However, a comparison with other labeled phentermine derivatives indicated that the total brain uptake, retention and selectivity of the new agent were poorer, probably as a result of the presence of the 4-amino substituent.
http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=4086198&dopt=Abstract
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Drug Metab Dispos. 1979 Nov-Dec;7(6):420-4.
Studies on the persistence of basic amines in the rabbit lung.
Wilson AG, Pickett RD, Eling TE, Anderson MW.
We have investigated the time-course of the pulmonary deposition of imipramine (IMIP) following a single iv injection into rabbits. A pool of IMIP and its demethylated metabolites, which exhibited considerable persistence (half-life of decay = 4 hr), was formed in the lung. This pool, now called the slowly effluxable pool (SEP), appears to be synonymous with the noneffluxable pool (NEP), which we have previously shown to be formed with IMIP in the isolated perfused lung (PL). Furthermore, this pool appears to be responsible for the pulmonary persistence of IMIP, inasmuch as 24 hr after an iv injection it contributes greater than 90% of the total lung concentration. Chlorphentermine and methadone formed SEP's in the IPL of comparable size to that formed with IMIP, whereas phentermine formed a considerably smaller SEP. These results suggest that the degree of hydrophobicity of the amine is an important determinant of the size of the SEP formed. This further supported by the lack of an SEP with the relatively polar amines, 5-hydroxytryptamine and amphetamine. The 10-fold difference in the size of the SEP for compounds known to induce pulmonary phospholipidosis (chlorphentermine and IMIP) and known not to induce lipidosis (phentermine and amphetamine) may suggest a possible involvement of the SEP in the onset of phospholipidosis; this possibility is discussed.
http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=43231&dopt=Abstract
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J Pharmacol Exp Ther. 1979 Dec;211(3):514-8.
Effect of desmethylimipramine on the kinetics of chlorphentermine accumulation in isolated perfused rat lung.
Minchin RF, Madsen BW, Ilett KF.
A number of basic amines are preferentially accumulated by the lung and there is the possibility that drug interactions in this organ may be important in vivo. In this study, the kinetics of the accumulation process for chlorphentermine were examined in a "single pass" isolated perfused rat lung. Chlorphentermine (2.5 x 10-7-2.5 x 10-5 M) was rapidly taken up over the 10-min perfusion period, and the rate of uptake was well described by a biexponential equation. One component of the uptake was small in capacity and nonsaturable while the other was large in capacity and saturable. The smaller component could not be explained solely by distribution into total lung water. When desmethylimipramine (10-6-10-3 M) was added to the perfusate, it had little effect on the nonsaturable component but markedly affected the other; the initial velocity of uptake was decreased and the (negative) rate of change of uptake was increased with increased desmethylimipramine concentration. The data suggested that there were at least two mechanisms involved in uptake of chlorphentermine: a saturable transport process and tissue binding. It is not clear without further work whether the transport saturability is a mainfestation of a carrier-mediated process or of drug-induced membrane changes affecting diffusion.
http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=512916&dopt=Abstract
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