Drugs online research references
Psychopharmacology (Berl). 1985;86(3):356-8.
Discriminative stimulus properties of tripelennamine in the pigeon.
Karas CA, Picker M, Poling A.
Pigeons trained under a two-key drug discrimination procedure eventually learned to discriminate the antihistaminic tripelennamine (5 mg/kg) from saline. When 0.63-7.5 mg/kg doses of tripelennamine were administered in generalization test sessions, the percentage of responses directed to the tripelennamine-appropriate key varied directly with dose. At certain doses, the discriminative stimulus properties of the antihistaminics, diphenhydramine and pyrilamine, clearly generalized to tripelennamine, whereas intermediate generalization was evident with the antihistaminics, chlorpheniramine and promethazine. Chlorpromazine, cimetidine, d-amphetamine, diazepam, morphine, pentazocine, phenobarbital, and sodium valproate failed to produce tripelennamine-like patterns of responding.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2863839&dopt=Abstract
Psychopharmacology (Berl). 1984;83(2):200-4.
Discriminative stimulus properties of pizotifen maleate (BC105): a putative serotonin antagonist.
Minnema DJ, Hendry JS, Rosecrans JA.
Rats were trained to discriminate the putative serotonin (5-HT) antagonist, pizotifen maleate (BC105), from saline using a two-lever drug discrimination paradigm. Pizotifen maleate (6 mg/kg, 14.6 mumol/kg, IP) or saline was administered 55 min prior to the operant training session. The pizotifen discriminative stimulus (DS) had a rapid onset (less than 7 min) and was of long duration. The pizotifen DS was dose dependent. The pizotifen DS did not generalize to the putative 5-HT antagonists, methiothepin, xylamidine, and cinanserin. Partial generalization was observed to methysergide and metergoline, and complete generalization to cyrproheptadine and the phenothiazine antihistamine, promethazine. The pizotifen DS failed to generalize to the antipsychotic chlorpromazine, the ethanolamine antihistamine diphenhydramine, the CNS stimulant, d-amphetamine, and the putative 5-HT agonists, LSD and quipazine. LSD and quipazine failed to antagonize the pizotifen DS. The results of this study suggest that different DS properties are associated with the different putative 5-HT antagonists and that pizotifen and cyproheptadine, in addition to their reported 5-HT antagonist properties, share a common property that is also associated with promethazine, probably involving antihistaminergic activity.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=6431474&dopt=Abstract
Agents Actions. 1984 Jun;14(5-6):590-7.
Evaluation of the CNS properties of SCH 29851, a potential non-sedating antihistamine.
Barnett A, Iorio LC, Kreutner W, Tozzi S, Ahn HS, Gulbenkian A.
SCH 29851 [8-chloro[6,11-dihydro-11-(1-carboethoxy-4-piperidylidene)- 5-H-benzo [5,6]cyclohepta[1,2-b]-pyridine] was discovered as part of a search for a new antihistamine without effects on the central nervous system (CHS). Antihistaminic potency and duration of action of SCH 29851 and other antihistamines were assessed by inhibition of histamine-induced lethality in guinea pigs and histamine-induced paw edema in mice. Evaluation of possible CNS effects included gross observation of mice, rats, dogs and monkeys, prevention of electroshock-induced convulsions, acetic acid-induced writhing and physostigmine-induced lethality in mice and biochemical measures related to sedative liability such as displacement of in vivo 3H-mepyramine binding in mouse brain and in vitro 3H-WB 4101 binding in guinea pig cortex. Comparisons were made to several antihistamines considered to be sedative to varying degrees, including diphenhydramine, promethazine, chlorpheniramine and azatadine and to the newer antihistamines terfenadine and astemizole which are reported to be non-sedating in man at doses that antagonize the effects of histamine peripherally. SCH 29851 had antihistamine activity in the tests used with a potency at least comparable to most standards and was devoid of activity in all the functional and biochemical models used as indices of CNS activity. It is expected that SCH 29851 should be an effective, long acting, antihistamine in man without sedative effects at therapeutic doses.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=6236679&dopt=Abstract
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