Matches in SemOpenAlex for { <https://semopenalex.org/work/W1845737189> ?p ?o ?g. }
- W1845737189 endingPage "73" @default.
- W1845737189 startingPage "1356" @default.
- W1845737189 abstract "S 16924 antagonized locomotion provoked by dizocilpine and cocaine, reduced conditioned avoidance responses and blocked climbing elicited by apomorphine, models predictive of control of the positive symptoms of schizophrenia: its median inhibitory dose (ID)50 was 0.96 mg/kg, s.c. vs. 1.91 for clozapine and 0.05 for haloperidol. Rotation elicited in unilateral, substantia nigra-lesioned rats by the D1 agonist, SKF 38393, and by the D2 agonist, quinpirole, was blocked equipotently by S 16924 (0.8 and 1. 7) and clozapine (0.6 and 2.0), whereas haloperidol preferentially blocked quinpirole (0.02) vs. SKF 38393 (1.8). S 16924 more potently inhibited the head-twitches elicited by 1-(2, 5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) and the locomotion provoked by phencyclidine than it inhibited the locomotion elicited by amphetamine (ID50s = 0.15 and 0.02 vs. 2.4). Clozapine showed a similar preference (0.04 and 0.07 vs. 8.6), but not haloperidol (0. 07 and 0.08 vs. 0.04). The discriminative stimulus (DS) properties of DOI were also blocked by S 16924 (ID50 = 0.17) and clozapine (0. 05) but not by haloperidol (>0.16). S 16924 fully (100%) generalized [effective dose (ED)50 = 0.7] to a clozapine DS and clozapine (0.23) fully generalized to a S 16924 DS whereas haloperidol (>/=0.08) only partially generalized (</=50%) to their DS in each case. Power spectra analysis of electroencephalograms from frontal cortex showed that both S 16924 (2.0) and clozapine (5.0) reinforced frequencies in the 7 to 8 Hz range whereas haloperidol (0.5) preferentially reinforced frequencies in the 10 to 14 Hz range. In a model of perturbation of cognitive-attentional function, significant latent inhibition was obtained with S 16924 (0.08) and clozapine (0.16), but not haloperidol (0.0063 and 0.04): higher doses of S 16924 (2.5), clozapine (5.0) and haloperidol (0.1) all blocked disruption of latent inhibition by amphetamine (1.5). Catalepsy was provoked by haloperidol (0.04-0.63) but not by S 16924 (>/=80.0) or clozapine (>/=80.0). Further, S 16924 (ID50 = 3.2) and clozapine (5.5) inhibited induction of catalepsy by haloperidol. This action of S 16924 was abolished by the 5-HT1A receptor antagonist, WAY 100,635 (0.16), which less markedly attenuated the anticataleptic action of clozapine. Further, although gnawing elicited by methylphenidate was inhibited by S 16924 (ID50 = 8.4), clozapine (19.6) and haloperidol (0.04), only the action of S 16924 was blocked by WAY 100,635 (0.16). Haloperidol potently (0.01-0.16, approximately 24-fold) increased prolactin levels whereas they were less markedly affected by S 16924 (2.5-40.0, 4-fold) and clozapine (10.0-40.0, 3-fold). Clozapine displayed high affinity at cloned, human, muscarinic (M1) and native, histamine (H1) receptors (Kis = 4.6 and 5.4 nM, respectively), whereas S 16924 (>1000 and 158) and haloperidol (>1000 and 453) displayed low affinity. In conclusion, S 16924 displays a profile of activity in diverse models of potential antipsychotic and extrapyramidal properties similar to that of clozapine and different to that of haloperidol. In particular, reflecting its partial agonist actions at 5-HT1A receptors, S 16924 inhibits rather than induces catalepsy in rats. However, in contrast to clozapine, S 16924 displays only low affinity for muscarinic and histaminic receptors." @default.
- W1845737189 created "2016-06-24" @default.
- W1845737189 creator A5000682280 @default.
- W1845737189 creator A5016562321 @default.
- W1845737189 creator A5019072094 @default.
- W1845737189 creator A5031948317 @default.
- W1845737189 creator A5036988353 @default.
- W1845737189 creator A5039339834 @default.
- W1845737189 creator A5041008066 @default.
- W1845737189 creator A5041494494 @default.
- W1845737189 creator A5045801598 @default.
- W1845737189 creator A5058418331 @default.
- W1845737189 creator A5081653127 @default.
- W1845737189 creator A5084812739 @default.
- W1845737189 creator A5090546204 @default.
- W1845737189 date "1998-09-01" @default.
- W1845737189 modified "2023-09-27" @default.
- W1845737189 title "S 16924 ((R)-2-[1-[2-(2,3-dihydro-benzo[1,4] dioxin-5-yloxy)-ethyl]-pyrrolidin-3yl]-1-(4-fluoro-phenyl)-ethanone), a novel, potential antipsychotic with marked serotonin (5-HT)1A agonist properties: II. Functional profile in comparison to clozapine and haloperidol." @default.
- W1845737189 cites W1482168898 @default.
- W1845737189 cites W1874438046 @default.
- W1845737189 cites W1895729847 @default.
- W1845737189 cites W1956321811 @default.
- W1845737189 cites W1965171548 @default.
- W1845737189 cites W1965925977 @default.
- W1845737189 cites W1969134234 @default.
- W1845737189 cites W1969885801 @default.
- W1845737189 cites W1971851906 @default.
- W1845737189 cites W1972253384 @default.
- W1845737189 cites W1973460321 @default.
- W1845737189 cites W1981806827 @default.
- W1845737189 cites W1982539986 @default.
- W1845737189 cites W1984380541 @default.
- W1845737189 cites W1984733445 @default.
- W1845737189 cites W1985567867 @default.
- W1845737189 cites W1997886266 @default.
- W1845737189 cites W1997939697 @default.
- W1845737189 cites W1999901204 @default.
- W1845737189 cites W2006749296 @default.
- W1845737189 cites W2012183787 @default.
- W1845737189 cites W2014159141 @default.
- W1845737189 cites W2019233381 @default.
- W1845737189 cites W2023006010 @default.
- W1845737189 cites W2025690352 @default.
- W1845737189 cites W2027782078 @default.
- W1845737189 cites W2031757811 @default.
- W1845737189 cites W2031880226 @default.
- W1845737189 cites W2033428309 @default.
- W1845737189 cites W2034005051 @default.
- W1845737189 cites W2034967655 @default.
- W1845737189 cites W2034973230 @default.
- W1845737189 cites W2035723974 @default.
- W1845737189 cites W2036386823 @default.
- W1845737189 cites W2038135029 @default.
- W1845737189 cites W2039800019 @default.
- W1845737189 cites W2047540295 @default.
- W1845737189 cites W2051394658 @default.
- W1845737189 cites W2053009038 @default.
- W1845737189 cites W2053754882 @default.
- W1845737189 cites W2054279548 @default.
- W1845737189 cites W2054789315 @default.
- W1845737189 cites W2054790699 @default.
- W1845737189 cites W2060341999 @default.
- W1845737189 cites W2064032824 @default.
- W1845737189 cites W2075712526 @default.
- W1845737189 cites W2075960719 @default.
- W1845737189 cites W2077149536 @default.
- W1845737189 cites W2084269591 @default.
- W1845737189 cites W2084768065 @default.
- W1845737189 cites W2084790546 @default.
- W1845737189 cites W2087866447 @default.
- W1845737189 cites W2088857022 @default.
- W1845737189 cites W2091217798 @default.
- W1845737189 cites W2095353831 @default.
- W1845737189 cites W2096824787 @default.
- W1845737189 cites W2113671902 @default.
- W1845737189 cites W2118527319 @default.
- W1845737189 cites W2121264019 @default.
- W1845737189 cites W2142960003 @default.
- W1845737189 cites W2143080892 @default.
- W1845737189 cites W2152316240 @default.
- W1845737189 cites W2168437758 @default.
- W1845737189 cites W2168836105 @default.
- W1845737189 cites W2246134119 @default.
- W1845737189 cites W2253420311 @default.
- W1845737189 cites W2256393228 @default.
- W1845737189 cites W2263640045 @default.
- W1845737189 cites W83357382 @default.
- W1845737189 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/9732399" @default.
- W1845737189 hasPublicationYear "1998" @default.
- W1845737189 type Work @default.
- W1845737189 sameAs 1845737189 @default.
- W1845737189 citedByCount "26" @default.
- W1845737189 countsByYear W18457371892017 @default.
- W1845737189 crossrefType "journal-article" @default.
- W1845737189 hasAuthorship W1845737189A5000682280 @default.
- W1845737189 hasAuthorship W1845737189A5016562321 @default.
- W1845737189 hasAuthorship W1845737189A5019072094 @default.
- W1845737189 hasAuthorship W1845737189A5031948317 @default.