Table 2.

Pharmacological properties of the new neurohypophyseal hormones analogues together with the values for AVP and some related analogues

Analogue		Activity*
		Uterotonic in vitro no Mg2+ IU/mg or pA2	Pressor** IU/mg or pA2	Antidiuretic*** IU/mg 60 min (200 min)
AVPa		17	412	465
OTa		450	5	5
[Mpa1]OTa		803	1.44	19
Atosiban, d[d-Tyr(Et)2 ,Thr4]OVTb,c		7.71 ± 0.05	pA2 = 6.14 ± 0.02	pA2 = 5.9
[Acc2]AVPd		pA2 ~ 5.6	56.6	750–900 (~9,300)
[Mpa1,Acc2]AVPe		pA2 ~ 5.6 (0.7 IU/mg)	17.2 ± 0.8	4,500 (50,000)
[Acc2,Val4]AVPe		pA2 = 6.9	0.9 ± 0.30	2,300 (23,000)
[cis-Apc2]AVP	I	pA2 = 7.47 ± 0.30	pA2 = 6.73	10 (2,000)
[Mpa1,cis-Apc2]AVP	II	pA2 = 8.46 ± 0.20	pA2 = 7.41	45 (9,000)
[cis-Apc2,Val4]AVP	III	pA2 = 8.22 ± 0.11	pA2 = 6.85	15 (2,000)
[Mpa1,cis-Apc2,Val4]AVP	IV	pA2 = 8.40 ± 0.19	pA2 = 7.04	20 (4,500)
[cis-Apc2,d-Arg8]VP	V	pA2 = 7.98 + 0.14	pA2 ~ 7.1	1 (200)
[Mpa1,cis-Apc2,d-Arg8]VP	VI	pA2 = 8.16 + 0.02	pA2 ~ 7.1	5 (1,000)
[Cpa1,cis-Apc2]AVP	VII	pA2 = 7.85 + 0.14	pA2 ~ 6.2	0.05 (1)
Aca[cis-Apc2,Val4]AVP	VIII	pA2 = 5.7	0	<0.01 (<0.5)
t-Bba[cis-Apc2,Val4]AVP	IX	10.1 + 3.8 IU/mg	0	<0.01 (<0.5)
Hba[cis-Apc2,Val4]AVP	X	pA2 = 7.61	pA2 ~ 6.4	<0.01 (<0.5)
Aba[cis-Apc2,Val4]AVP	XI	pA2 = 7.26 + 0.40	0	0
[cis-Apc2]OT	XII	pA2 = 7.89 + 0.07	pA2 ~ 5.75	ND
[Mpa1,cis-Apc2]OT	XIII	pA2 = 8.11 + 0.18	pA2 ~ 6.0	0
[Cpa1,cis-Apc2]OT	XIV	pA2 = 7.97 + 0.24	pA2 ~ 6.73	ND

* The values are given as averages ± SEM, n = 3–5

** 0 means no activity up to the dose of 0.15 mg/kg of experimental animal

*** Activity was estimated on the threshold level of activity 60 min and on the level of the 200 min activity (in parentheses); activity of AVP taken as 465 IU/mg at both levels, ND no data available

Biological activities of the other analogues reported here as references are taken from the literature: ^aLebl (1987), ^bMelin et al. (1986), ^cManning et al. (1995), ^dJastrzębska et al. (2003), ^eKowalczyk et al. (2004)