Abstract
The novel, naphtylpiperazine 5-HT 1A agonist, S 14671 (4-[(thenoyl-2)aminoethyl]-l-(7-methoxynaphtylpiperazine)), displayed very high affinity for S-HT 1A binding sites (pK i = 9.3) as compared to the serotonin (5-HT) 1A agonists, 8-OH-DPAT (9.2) and (+)-flesinoxan (8.7) and the 5 HT 1A partial agonists, buspirone (7.9) and BMY 7378 (8.8). In vivo, S 14671 induced the typical 5-HT 1A agonist-induced responses of hypothermia and spontaneous tail-flicks at doses as low as ⩾ 5μg/kg s.c. and ⩾ 40 μg/kg s.c., respectively. In each test, it was about 10-fold more potent than 8-OH-DPAT and 100-fold more potent than (+)-flesinoxan and buspirone. The actions of S 14671 could be blocked by BMY 7378 and the 5-HT 1A receptor antagonist, (−)-alprenolol, but not by the 5-HT 1C 2 receptor antagonist, ritanserin, nor the 5-HT 3 receptor antagonist, ICS 205930. Thus, S 14671 is a novel 5-HT 1A ligand of high efficacy and exceptional in vivo potency.
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