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  • Title: Pharmacological aspects of R-(+)-7-OH-DPAT, a putative dopamine D3 receptor ligand.
    Author: Damsma G, Bottema T, Westerink BH, Tepper PG, Dijkstra D, Pugsley TA, MacKenzie RG, Heffner TG, Wikström H.
    Journal: Eur J Pharmacol; 1993 Nov 16; 249(3):R9-10. PubMed ID: 8287911.
    Abstract:
    The R-(+)-isomer of 7-hydroxy-2-(N,N-di-n-propylamino)tetralin (7-OH-DPAT) bound with a more than 200-fold higher affinity to cloned human dopamine D3 receptors (Ki = 0.57 nM) than to dopamine D2 receptors; the corresponding S-(-)-enantiomer had considerably less affinity for both dopamine receptor subtypes, indicating that the known enantiomer selectivity of 7-OH-DPAT for the 'classical' dopamine D2 receptor subtype extends to the recently discovered dopamine D3 receptor subtype. In rats R-(+)-7-OH-DPAT dose dependently (10-1000 nmol/kg) decreased dopamine release and induced yawning, while sniffing behaviour occurred at the highest dose tested (1000 nmol/kg). The possibility that the inhibition of dopamine release and the elicitation of yawning are mediated by dopamine D3 receptors is considered.
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