TABLE 1

Agonist relative efficacies and potencies at 5-HT_2B receptors measured using five assays of receptor activation

Known valvulopathic compounds are in bold type. E_max represents percentage of 5-HT.

Drugs	Calcium Flux		NFAT-bla Activity		ERK2 Phosphorylation		Arrestin Translocation		InsP Accumulation
Drugs	E_max	pEC₅₀	E_max	pEC₅₀	E_max	pEC₅₀	E_max	pEC₅₀	E_max	pEC₅₀
	%		%		%		%		%
5-HT	100.0 ± 0.7	8.75 ± 0.03	100 ± 2	9.14 ± 0.05	100	9.43 ± 0.02	100 ± 2	7.78 ± 0.06	100 ± 1	7.97 ± 0.03
BW 723C86	92.9 ± 0.9	8.85 ± 0.03	96 ± 2	8.23 ± 0.05	65.3 ± 0.8	9.04 ± 0.04	100 ± 2	6.18 ± 0.05	89.5 ± 0.6	7.58 ± 0.02
DOI	88.2 ± 6.3	8.84 ± 0.13	106.6 ± 0.9	7.86 ± 0.02	54 ± 1	8.26 ± 0.06	96 ± 1	6.99 ± 0.03	103 ± 1	7.19 ± 0.03
Ergotamine	87.2 ± 5.7	5.46 ± 0.18	88 ± 1	8.42 ± 0.04	74.0 ± 0.9	7.70 ± 0.03	98.8 ± 0.8	8.08 ± 0.03	82 ± 2	6.41 ± 0.04
TFMPP	40.3 ± 8.0	7.42 ± 0.11	24 ± 2	7.5 ± 0.2	49 ± 1	7.64 ± 0.06	126 ± 1	6.52 ± 0.02	18.3 ± 0.4	6.97 ± 0.05
Quipazine	8.4 ± 0.2	8.05 ± 0.09	7.0 ± 0.5	7.3 ± 0.2	21 ± 1	7.9 ± 0.1	60 ± 1	6.44 ± 0.04	7.1 ± 0.3	7.71 ± 0.09
RU 24969	60.1 ± 13.3	7.89 ± 0.08	43 ± 1	7.04 ± 0.06	87 ± 2	8.00 ± 0.05	91 ± 1	6.26 ± 0.02	26.7 ± 0.6	6.47 ± 0.05
SCH 23390	47.1 ± 6.4	7.18 ± 0.10	46 ± 1	7.06 ± 0.06	75 ± 2	7.05 ± 0.06	142 ± 2	5.76 ± 0.02	21.7 ± 0.6	5.95 ± 0.05
WAY 161503	72 ± 1	8.44 ± 0.05	98 ± 3	7.64 ± 0.08	68 ± 1	7.71 ± 0.04	232 ± 3	6.50 ± 0.02	91 ± 1	6.93 ± 0.03
Cabergoline	98.5 ± 1.9	6.40 ± 0.10	108 ± 4	9.1 ± 0.1	60.1 ± 0.9	8.44 ± 0.04	90.6 ± 0.6	8.23 ± 0.03	77 ± 2	8.18 ± 0.07
Dihydroergotamine	81.6 ± 7.9	5.30 ± 0.22	92 ± 1	8.32 ± 0.04	70.6 ± 0.8	8.27 ± 0.03	175 ± 4	7.65 ± 0.06	76 ± 2	7.48 ± 0.06
Ergonovine	39.7 ± 4.0	7.15 ± 0.37	54.3 ± 0.6	9.03 ± 0.03	57 ± 1	8.48 ± 0.05	74.7 ± 0.9	7.82 ± 0.03	22.2 ± 0.2	8.64 ± 0.03
Methylergonovine	49.5 ± 6.7	7.67 ± 0.07	56 ± 2	9.3 ± 0.1	52.5 ± 0.8	8.78 ± 0.05	102.4 ± 0.7	8.96 ± 0.02	18.7 ± 0.1	8.52 ± 0.02
Norfenfluramine	107.4 ± 0.6	8.61 ± 0.02	101 ± 2	7.81 ± 0.04	75 ± 1	8.85 ± 0.04	52 ± 1	6.89 ± 0.05	84 ± 2	6.73 ± 0.05
Pergolide	88.5 ± 6.4	7.13 ± 0.08	108 ± 3	7.72 ± 0.05	79 ± 1	8.99 ± 0.05	92 ± 1	7.73 ± 0.04	95 ± 1	6.94 ± 0.02
Ropinirole	73 ± 1	5.59 ± 0.02	89 ± 6	5.0 ± 0.1	67 ± 3	5.60 ± 0.05	N.D.	<5	163 ± 4	4.46 ± 0.02
Guanfacine	93 ± 1	6.91 ± 0.03	102 ± 2	6.26 ± 0.05	59 ± 1	7.04 ± 0.04	87 ± 4	5.32 ± 0.05	119 ± 3	5.16 ± 0.03
Oxymetazoline	70.9 ± 0.4	7.34 ± 0.01	80 ± 1	6.44 ± 0.03	60.0 ± 0.9	8.00 ± 0.04	130 ± 5	5.41 ± 0.04	51.8 ± 0.6	5.38 ± 0.02
Quinidine	55.9 ± 0.3	6.73 ± 0.01	63 ± 3	6.17 ± 0.09	51 ± 1	7.19 ± 0.05	119 ± 4	5.36 ± 0.03	32.2 ± 0.9	5.31 ± 0.04
Xylometazoline	55.7 ± 0.3	6.62 ± 0.01	56 ± 1	6.00 ± 0.04	53 ± 1	7.16 ± 0.06	140 ± 10	5.18 ± 0.07	47 ± 3	4.86 ± 0.06
Fenoldopam	92.5 ± 0.6	7.11 ± 0.01	87 ± 2	6.91 ± 0.06	91 ± 2	6.23 ± 0.03	207 ± 7	5.51 ± 0.04	71 ± 1	5.79 ± 0.03
SR 57227A	37.4 ± 0.4	6.97 ± 0.02	28 ± 2	7.2 ± 0.2	91 ± 2	6.72 ± 0.04	74 ± 2	5.94 ± 0.04	21.9 ± 0.2	6.58 ± 0.01
L 694247	102.2 ± 4.4	7.27 ± 0.06	N.D.	N.D.	N.D.	N.D.	N.D.	N.D.	N.D.	N.D.
DM 360	84.6 ± 7.5	8.38 ± 0.33	N.D.	N.D.	N.D.	N.D.	N.D.	N.D.	N.D.	N.D.
SKF 83566	48.6 ± 3.5	6.90 ± 0.03	56 ± 2	7.24 ± 0.09	142 ± 3	6.54 ± 0.05	134 ± 1	5.97 ± 0.02	36 ± 1	5.43 ± 0.05
CP 132484-42	92.7 ± 4.0	7.70 ± 0.28	N.D.	N.D.	N.D.	N.D.	N.D.	N.D.	N.D.	N.D.
CP 118,952	71.8 ± 10.2	7.89 ± 0.28	N.D.	N.D.	N.D.	N.D.	N.D.	N.D.	N.D.	N.D.
CP 123,479-11	93.9 ± 4.8	8.71 ± 0.17	N.D.	N.D.	N.D.	N.D.	N.D.	N.D.	N.D.	N.D.

TFMPP, 1-(3-trifluoromethylphenyl) piperazine; ND, not determined.