The broad-spectrum antiemetic effects ETI-385 result from stimulation of 5-HT1A and 5-HT1D receptors.

In the present study, we describe how a nonstoichiometric ratio of the isomers of 8-hydroxy-2-(di-n-propylamino)tetralin (DPAT) produce a broad-spectrum of antiemetic effects in cats and shrews. Determination of the receptor profile of the isomers and testing them separately in cats revealed superior antiemetic effects but severe defensive behavior with the R isomer compared with the S isomer. Differing ratios yielded the best results with the 1:8 (R-S) ratio producing a drug more potent than DPAT and with negligible defensive behavior side effects.

Multicenter evaluation of automated immunoturbidimetric assays for measurement of apolipoproteins A-I and B in serum and plasma.

Results of a multicenter evaluation of automated assays for measurement of apolipoproteins (apo) A-I and B with the Paramax analytical system are reported. Apo A-I and apo B response surface models were used to optimize concentrations of critical assay variables. Overall imprecision for apo A-I controls at concentrations of 1.

Identification of the metabolites of erythro-9-(2-hydroxy-3-nonyl)hypoxanthine from laboratory animals.

After administration of erythro-9-(2-hydroxy-3-nonyl)hypoxanthine, eight compounds were isolated from the urine of rats, dogs, and monkeys. All of the drug metabolites were modified on the nonyl side chain. The oxidatively degraded metabolites included an alcohol (9-(2,8-dihydroxy-3-nonyl)hypoxanthine), the corresponding ketone (erythro-9-(2-hydroxy-8-keto-3-nonyl)hypoxanthine), and three carboxylic acids [erythro-6-hydroxy-5-(9- hypoxanthyl ) hepanoic acid, erythro-7-hydroxy-6-(9- hypoxanthyl )octanoic acid, and erythro-8-hydroxy-7-(9- hypoxanthyl )nonanoic acid].

Inosiplex: metabolism and excretion of the dimethylaminoisopropanol and p-acetamidobenzoic acid components in rhesus monkeys.

The principal excretion products derived from radiolabeled N,N-dimethylaminoisopropanol (Dip) and p-acetamidobenzoic acid (PAcBA) components of inosiplex (Isoprinosine) were identified and quantified in urine following single iv and oral administration of the drug in rhesus monkeys. The major metabolite derived from [3H] PAcBA was identified as PAcBA-O-acylglucuronide by 1) positive naphthorescorcinol reaction for glucuronic acid and 2) hydrolysis of the metabolite to PAcBA and glucuronic acid, using either dilute base (but not acid) or beta-glucuronidase. This metabolite accounted for 50% of the administered dose in orally dosed animals and 31% in iv dosed animals.