1997, 20 (4): 8 87 J ou ra l of N aj ig A g ricu ltu ra l U iversity 52 α (, 210095) 52 (52H T ) : (1) 10 - mo lgl 10-4 mo lgl 52H T 0 m i,, 10-5 mo lgl, 10 - mo lgl (tryp tam ie), 10-4 mo lgl 10-5 mo lgl, (2) 10 - mo lgl (cyp rohep tadie) (trazodoe) (m iaseri) (sp iroperido l) (haloperido l) 1 h, haloperido l, () 10-4 mo lgl 52H T 0 m i,, 1 h, cyp rohep tadie m iaseri trazodoe, sp iroperido l, haloperido l, 52H T, 52H T, 52H T ; ; 52 ; ; S852175 THE EFFECTS OF SEVERAL 5-HT RECEPTOR ANTAGON ISTS ON THE MOTOR ACTIV ITY IN SCH ISTOSOM A J A PON ICUM W ag L ip ig, Sh i X iao li ad She L ili (Co llege of V eteriary M edicie, N a jig A gric U iv, N a jig 210095) ABSTRACT M o to r activity w as determ ied w ith drugs at differet cocetratio uder a m icro scope. T he results show ed that S. jap oicum s w ere obviously stim ulated by 52hydroxytryp tam ie (10 -, 10-4 mo lgl ) ad tryp tam ie (10 - mo lgl ). Several vertebrate 52hydroxytryp tam ie atagoists, cyp rohep ta2 die, m iaseri ad trazodoe, at cocetratio aroud 10 - mo lgl o t oly blocked the effects of edoge2 ous 52H T but also reduced exogeous 52H T 2iduced icreases i the mo to r activity of S. Sp iroperido l, the o ther 52H T atagoist, had o ifluece o the mo tility. had coo rdiated excitatio all alog. to r i S. jap oicum ad it s differece from m amm alia s. jap oicum. To our iterest, haloperido l T he above effects p relim iarily suggested the p resece of 52H T recep2 Key words S ch istosom a jap oicum ; atagoists; 52H T; recep to r; mo to r activity,,, ( ), α : 1997201226
84 20, 52H T, 52H T 52H T 52H T [ 1 4 ], 52H T, 52H T tryp tam ie 5 52H T, 52H T,, 1 111, 5 40 d,, (Υ) 10% Earle s, 7 EBSS : N ac l 68 g, KC l 0. 4 g, CaC l2 0. 2 g, M gso 4 7H 2O 0. 2 g, N ah 2PO 4 2H 2O 0. 14 g, N ahco 2. 2 g, 110 g ph 7. 4, 112 [5 ] [6 ] 24 serum gebss,, 7 015 1 h,, (4 10 ) 5 m i, ( ) ( ),, : (1) ; (2) ; (), ; (4),,, ; (5),,,, ; (6),, 6,, t 11 52 (52H T ),, N o. 65202225, (tryp tam ie), L. L igh t & Co. L td, N o. T 29511 (cyp rohep tadie),n o. C26022; (sp iroperido l), N o. (trazodoe), N o. S2795; (haloperido l), N o. H 21512; T 26154 (m ia seri), N o. M 22525 Sigm a, 2 211 5-HT tryptam ie 52H T (10 -, 10-4, 10-5 m o lgl ), 0 m i, 10-5 m o lgl 52H T, 52H T ( 1)
4 : 52 85 1 5-HT Table 1 Effects of 5-HT at differe t coce tratio o the m otor activ ity of Sch istosom a j ap o icum 52H T cgmo l L - 1 M o to r activity 52H T T reated w ith 52H T D ifferece 16 10-1. 1 0. 0 2. 81 0. 21 + 148. 67 14 10-4 1. 5 0. 22 2. 79 0. 47 + 106. 67 16 10-5 1. 5 0. 42 2. 25 0. 11 + 66. 67 P < 0. 01 (t2test). So as the fo llow ṡ = - EBSS mo to r activity after drug- mo to r activity i EBSS 100%, = 100% EBSS mo to r i EBSS tryp tam ie ( 10 -, 10-4, 10-5 m o lgl ), 10 - m o lgl tryp tam ie, 10-4 10-5 m o lgl tryp tam ie, tryp tam ie 52H T ( 2) 2 tryptam ie Table 2 Effects of tryptam ie at differe t coce tratio o the m otor activ ity of Sch istosom a j ap o icum P < 0. 05 T ryp tam ie cgmo l L - 1 M o to r activity T reated w ith tryp tam ie D ifferece 12 10-2. 18 0. 17. 25 0. 10 + 49. 08 12 10-4 2. 15+ 0. 26 2. 65+ 0. 18 + 2. 26 12 10-5 1. 84 0. 16 2. 00 0. 17 + 8. 70 212 5 5-HT 5 52H T 10 - m o lgl, cyp rohep tadie trazodoe m ia seri ; haloperido l, ; sp iroperido l ( ) 5 5-HT Table Effects of 5-HT receptor a tago ists at 10 - molgl o the motor activ ity of Sch istosom a j ap o icum M o to r activity T reated w ith drugsg10 - mo l L - 1 D ifferece 14 2. 77 0. 57 cyp rohep tadie 1. 00 0. 2-6. 5 14 2. 90 0. 57 m iaseri 1. 60 0. 26-44. 8 1. 00 0. 19 trazodoe 2. 00 0. 15 -. 1 2. 67 0. 21 sp iroperido l 2. 7 0. 19 + 1. 49 12 2. 56 0. 11 haloperido l. 90 0. 87 + 52. 4 P < 0. 001, P < 0. 05; + : Excitem et, - : Ih ib itio. 21 5-HT 5-HT 10-4 m o lgl 52H T, 0 m i 5 m i, ; 10 - m o lgl, 1 h, cyp rohep2
86 20 tadie m ia seri trazodoe, cyp rohep tadie m ia seri, haloperido l ( 4) 4 5 5-HT 5-HT Table 4 Effects of 5-HT receptor a tago ists o the m otor activ ity icreased by 10-4 m olgl 5- HT of Sch istosom a j ap o icum 52H T T reated w ith 52H T M o to r activity T reated w ith drugs D ifferece 1. 70 0. 18 cyp rohep tadie 1. 10 0. 18-70. 14. 84 0. 21 m iaseri 1. 54 0. 41-59. 90 14 4. 46 0. 12 trazodoe 2. 81 0. 15-7. 00 12. 00 0. 1 sp iroperido l 2. 9 0. 12-2. 8 1 4. 16 0. 12 haloperido l 4. 86 0. 1 + 16. 8 P < 0. 01, P < 0. 05 = - 52H T 52H T 100% mo to r activity after drugs- mo to r activity after 52H T = 100% mo to r activity after 52H T, 52H T, [ 7 ] [ 4 ], 52H T, cyp rohep ta2 die trazadoe m ia seri, ; 52H T, 52H T, 52H T, 52H T, haloperido l 52H T,, W illcack so H illm a [ 8 ] haloperi2 do l,,,, haloperido l,, 52H T,,, sp iroperido l 52H T, 52H T, 52H T 52H T 1 sp iroperido l [ 9 52H T 2 ], 52 H T 1, 52H T 2,, 52H T Perou tka Syder [ 9 ],, 52H T sp iroperido l> m ia seri > cyp rohep tadie> haloperido l; 52H T cyp rohep tadie> m ia seri> trazodoe> sp iroperido l sp iroperido l,,
4 : 52 87, [ 10, 11, ], 52H T, 2 1 Beett J L, Buedig E, T imm s A R, et al. O ccurrece ad levels of 52hydroxytryp tam ie i S ch isto2 som a m asoi. M o l Phar, 1969, 5: 542 545 2 Chou T 2C T, Beett J L, Buedig E. O ccurrece ad cocetratios of biogeic am ies i trem a2 todeṡ T he Joural of Parasito logy, 1972, 58 (6): 1098 1102, 1 52H T 1, 1997, 20 (1): 7 78 4, 1 1, 1995, 18 (4): 79 85 5 1 1, 1980, 1 (1): 51 55 6 M elli T N, Busch R D, W ag C C, et al. N europharm aco logy of the parasitic trem atode: S ch istosom a m asoi. Am erica Joural of T rop ic M edicie ad H ygie, 198, 1: 8 9 7 M asour T E. T he Effect of lysergic acid diethylam ide, 52hydroxytryp tam ie, ad related compouds o the liver fluke F asciola hep atica. B rit J Pharm aco logy, 1957, 12: 406 409 8 W illcok so WM S, H illm em G R. D rug effects o the 52H T respose of S ch istosom a m asoi. B iochem ad Physio l, 1984, 77: 199 20 Comp 9 Stephe J Peroutka, Sdyer S H. M ultip le sero toi recep to rs: differetial bidig of [ H ] 52H T, [ H ] L SD ad [ H ] sp iroperido l. M o lecular Pharm aco logy, 1979, 16: 687 699 10 M cn all S, M asour T E. N ovel sero toi recep to rs i F asciola: Characterizatio by studies o adey2 late cyclase activatio ad [ H ] L SD bidig. B ic Phar, 1984, : 2789 2797 11 R ibeiro P, W ebb R A. D emostratio of specific h igh2affiity bidig sites fo r [ H ] 52H T i the ces2 tode H em eolep is d im iu ta. Comp B iochem Physio l, 1986, 84 (): 5 58 ( )