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1 SRIF action was blocked in cells pretreated with pertuss
2 SRIF amacrine cells, DA amacrine cells, and M1 ipRGCs fo
3 SRIF analog affinities were determined by membrane radio
4 SRIF analogs with selective affinity for this receptor m
5 SRIF and SMS increased the phosphorylation of the 71-kDa
6 SRIF immunostaining was observed in widely spaced amacri
7 SRIF increases K(+) currents, decreases Ca(2+) currents,
8 SRIF modulation of the microcircuit was investigated wit
9 SRIF reduced Ca(2+) current in rods by 33% but increased
10 SRIF, at concentrations of 100-500 nM, enhanced a delaye
11 SRIF-immunoreactive cells have two to five primary proce
12 1,2,5)-[d-Trp(8),(N(alpha)Me)IAmp(9),Tyr(11)]SRIF (34), and Des-AA(1,2,5)-[d-Agl(8)(N(beta)Me,2-napht
13 gl(8)(N(beta)Me,2-naphthoyl),IAmp(9),Tyr(11)]SRIF (42) (Agl = aminoglycine) are sst(1) agonists in th
14 es-AA(1,2,5)-[DTrp(8),IAmp(9),(125)ITyr(11)]-SRIF ((125)I-25) and des-AA(1,2,5)-[DTrp(8),IAmp(9), (12
15 and des-AA(1,2,5)-[DTrp(8),IAmp(9),Tyr(11)]-SRIF (25) are about (1)/(7), (1)/(4), (1)/(125), and (1)
17 5)-[Tyr(2),Glu(7),d-Trp(8),IAmp(9),hhLys(12)]SRIF (31) (sst(1) IC(50) = 16 nM) and cyclo(7-12) Des-AA
18 lu(7),d-Trp(8),IAmp(9),m-I-Tyr(11),hhLys(12)]SRIF (45) (sst(1) IC(50) = 6.1 nM) had equal or improved
19 1,2,5)-[d-Trp(8),IAmp(9),(N(alpha)Me)Ser(13)]SRIF (19), Des-AA(1,2,5)-[d-Trp(8),IAmp(9),(N(alpha)Me)C
20 1,2,5)-[d-Trp(8),IAmp(9),(N(alpha)Me)Cys(14)]SRIF (20), Des-AA(1,2,5)-[d-Trp(8),(N(alpha)Me)IAmp(9),T
21 Trp(8)-Lys(9)-Thr(10)-Cys(11)]Thr(12)-NH(2) (SRIF numbering), at the five known human somatostatin re
22 ls and acute and chronic pain in humans; (3) SRIF inhibits dorsal horn neuronal activity; and (4) SRI
23 ibits dorsal horn neuronal activity; and (4) SRIF reduces responses of joint mechanoreceptors to noxi
25 e the synthesis of two analogues of D-Trp(8)-SRIF in which Phe(6) and Phe(11) were replaced by the pr
26 also found that pyrazinylalanine(7)-D-Trp(8)-SRIF-14 does not bind, suggesting a repulsive interactio
28 eptors but sst(1), Des-AA(1,2,4,5)-[d-Trp(8)]SRIF (3) at sst(4) and sst(5), and Des-AA(1,2,4,5,13)-[d
31 ve (>25-fold); Des-AA(1,2,5,12,13)-[d-Trp(8)]SRIF (7) and Des-AA(1,2,4,5,12,13)-[d-Trp(8)]-SRIF (9, O
32 nalogues of des-AA(1,2,5)-[DTrp(8)/D2Nal(8)]-SRIF that contain a 4-(N-isopropyl)-aminomethylphenylala
33 RIF (7) and Des-AA(1,2,4,5,12,13)-[d-Trp(8)]-SRIF (9, ODT-8) were most potent at sst(4) and moderatel
34 Des-AA(1,2,5)-[d-Trp(8), (N(alpha)Me)IAmp(9)]SRIF (17), Des-AA(1,2,5)-[d-Trp(8),IAmp(9),(N(alpha)Me)S
36 Des-AA(1,2,5)-[d-Trp(8)/d-Nal(8),IAmp(9)]SRIF (AA = amino acid, Nal = 3-(2-naphthyl)-alanine, IAm
37 lective Des-AA(1,5)-[Tyr(2),d-Trp(8),IAmp(9)]SRIF, (14, sst(1) IC(50) = 14 nM) were prepared in which
38 o des-AA(1,5)-[(125)ITyr(2),DTrp(8),IAmp(9)]-SRIF ((125)I-16) for the detection of sst1 tumors in rec
39 7 to yield des-AA(1,2,5)-[D2Nal(8),IAmp(9)]-SRIF (13) and in 16 to yield des-AA(1,5)-[Tyr(2),D2Nal(8
40 yield des-AA(1,5)-[Tyr(2),D2Nal(8),IAmp(9)]-SRIF (17) was intended to increase chemical stability, s
41 (16), des-AA(1,2,5)-[Tyr(7),DTrp(8),IAmp(9)]-SRIF (23), and des-AA(1,2,5)-[DTrp(8),IAmp(9),Tyr(11)]-S
42 at des-AA(1,4,5,13)-[Tyr(2),DTrp(8),IAmp(9)]-SRIF (33) and des-AA(1,4,5,6,12,13)-[Tyr(2),DTrp(8),IAmp
43 s-AA(1,4,5,6,12,13)-[Tyr(2),DTrp(8),IAmp(9)]-SRIF (34) progressively lost affinity for all receptors.
44 ffinities of des-AA(1,2,5)-[DTrp(8),IAmp(9)]-SRIF (c[H-Cys-Lys-Phe-Phe-DTrp-IAmp-Thr-Phe-Thr-Ser-Cys-
45 5) (7), des-AA(1,5)-[Tyr(2),DTrp(8),IAmp(9)]-SRIF (CH-288) (16), des-AA(1,2,5)-[Tyr(7),DTrp(8),IAmp(9
46 AA(1,4-6,10,12,13)-[DPhe(2),DTrp(8),IAmp(9)]-SRIF-Thr-NH(2) (16), des-AA(1,2,4-6,10,12,13)-[DAgl(NMe,
47 ,10,12,13)-[DAgl(NMe,2naphthoyl)(8),IAmp(9)]-SRIF-Thr-NH(2) (23), and des-AA(1,2,4-6,10,12,13)-[DAgl(
48 3)-[DTyr(2),DAgl(NMe,2naphthoyl)(8),IAmp(9)]-SRIF-Thr-NH(2) (25) was radio-iodinated ((125)I-25) and
54 )]-Thr (15)-NH2 (1) (a somatostatin agonist, SRIF numbering) and H-Cpa (2)-c[DCys (3)-Tyr (7)-DTrp (8
56 = 4-(N-isopropyl)-aminomethylphenylalanine, SRIF = somatostatin), with or without a tyrosine or mono
59 eatment of hepatocytes incubated with GH and SRIF, or with GH and octreotide, abrogated the inhibitor
61 RIF) receptors (SSTRs) 1 and 2 bind SRIF and SRIF 28 with high affinity, although a number of synthet
63 statin (SRIF) receptors (SSTRs) 1 and 2 bind SRIF and SRIF 28 with high affinity, although a number o
64 nity constant (Ki) of 172 +/- 12 nM, blocked SRIF inhibition of adenylate cyclase in vitro (IC50 = 5.
70 (1,2,5)-[DTrp(8),IAmp(9), (125)ITyr(11)]-Cbm-SRIF ((125)I-27), used them as in vitro tracers, and fou
71 des-AA(1,2,5)-[DTrp(8),IAmp(9),Tyr(11)]-Cbm-SRIF (27) and des-AA(1,2,5)-[DCys(3),DTrp(8),IAmp(9),Tyr
72 des-AA(1,2,5)-[DTrp(8),IAmp(9),Tyr(11)]-Cbm-SRIF (27) increased affinity slightly as well as improve
73 1,2,5)-[DCys(3),DTrp(8),IAmp(9),Tyr(11)]-Cbm-SRIF (29) show agonistic activity in a cAMP assay; there
74 eraction of M1 ipRGCs and DA amacrine cells, SRIF amacrine cells would provide inhibitory modulation
78 nomas, the treatment with targeted cytotoxic SRIF analogue AN-238, consisting of 2-pyrrolinodoxorubic
82 Replacement of basal insulin levels during SRIF resulted in a fall of FFA levels from 545+/-47 to 2
84 ifficult to establish the role of endogenous SRIF release in the absence of pure SRIF antagonists.
85 n-14 somatotropin-release inhibiting factor (SRIF) and 2 of its analogs, (125)I-WOC 4a and (111)In-pe
86 tin [somatotropin release inhibiting factor (SRIF)] also inhibits the intrinsic light response of M1
87 tin [somatotropin release-inhibiting factor (SRIF)] is widely distributed in the body and exerts a va
88 [or somatotropin release-inhibiting factor (SRIF)] receptors, sst(2A), and studied the modulatory ac
89 in (somatotrophin release-inhibiting factor, SRIF) were determined in cultured locus coeruleus neuron
91 ter the functional expression of human fetal SRIF neurons in culture and if so, is this effect fetal-
92 xis, providing a mechanistic explanation for SRIF analog action in treating patients with GH-secretin
93 mple a 4-benzyl substituent is important for SRIF receptor binding, but the 4-desbenzyl analogue 27 w
94 rings to bind the Trp(8) binding pocket for SRIF-14 and the inability of pyrazine to do so was expla
98 ng receptor autoradiography; those with high SRIF receptor subtype 1 (sst(1)) affinity and selectivit
100 of a glucose-based peptidomimetic at a human SRIF receptor to date (K(i) 53 +/- 23 nM, n = 6 at sst4)
101 atostatin (SRIF) analogues at the five human SRIF receptors (sst) was determined to identify sterical
109 BDNF alone led to a significant increase in SRIF production (p=0.014), whereas exposure to gp120 alo
111 and gp120 led to an increase in BDNF-induced SRIF production which was significantly greater than tha
115 e numbering refers to the position in native SRIF), with Xxx(7) being Phe/Ala/Tyr, Yyy(8) being Trp/D
116 e numbering refers to the position in native SRIF), with Xxx7 being Ala/Aph, exhibit potent and highl
121 pported these results by showing that 500 nM SRIF reduced a K(+)-induced increase in intracellular Ca
123 nodoxorubicin (AN-201) linked to octapeptide SRIF carrier RC-121, may overcome this resistance by pro
125 st(2A), and studied the modulatory action of SRIF on voltage-gated K(+) and Ca(2+) currents in rod an
128 orsal root ganglion cells; (2) activation of SRIF receptors results in inhibition of both nociceptive
132 Furthermore, the sparse distribution of SRIF-immunoreactive somata, the wide-ranging, asymmetric
135 onal significance of transient expression of SRIF and its receptors in the development of the cerebel
136 lling pathway(s) mediating BDNF induction of SRIF production; an effect expressed by fetal brains thr
142 H3 cells demonstrate that basal secretion of SRIF-related material is largely calcium-dependent and t
143 (7), (1)/(4), (1)/(125), and (1)/(4) that of SRIF-28 (1) to sst1, respectively, about (1)/(65), (1)/(
145 -DTrp(8)-Lys(9)-Thr(10)-Phe(11)-Cys(14)]-OH (SRIF numbering) (ODT-8) by one of the four conformationa
146 -dTrp(8)-Lys(9)-Thr(10)-Phe(11)-Cys(14)]-OH (SRIF numbering) (ODT-8) that is potent at all SRIF recep
149 3187 to determine the role of calcium in pro-SRIF cleavage and nascent vesicle formation from the tra
150 ry GH3 cells expressing prosomatostatin (pro-SRIF) to study prohormone processing and nascent secreto
152 her, these observations demonstrate that pro-SRIF processing and budding of nascent secretory vesicle
155 show that prolonged exposure to radiolabeled SRIF analogs significantly increases their cellular inte
156 ors, the SRIF receptors (SSTR 1-5) recognize SRIF and related peptides which retain its beta-turn suc
165 7) and irreversibly reduced by somatostatin (SRIF-14); this was associated with hyperpolarization of
166 inding affinity of short chain somatostatin (SRIF) analogues at the five human SRIF receptors (sst) w
168 binding properties to all five somatostatin (SRIF) receptors using receptor autoradiography; those wi
169 that structural constraints in somatostatin (SRIF) analogues may result in receptor selectivity, and
170 hin the hippocampus, the major somatostatin (SRIF) receptor subtype, the sst2A receptor, is localized
174 Changes in the expression of somatostatin (SRIF) have been observed in the brains of HIV encephalit
175 eleasing hormone (GHRH) and of somatostatin (SRIF) in pharmacologically stimulated growth hormone (GH
177 endogenously by an infusion of somatostatin (SRIF) to produce insulinopenia in groups of lean healthy
178 rch for synthetic analogues of somatostatin (SRIF) which exhibit selective affinities for the five kn
179 rch for synthetic analogues of somatostatin (SRIF) which exhibit selective affinities for the five kn
180 synthetic peptide analogues of somatostatin (SRIF) which exhibit selective affinities for the five kn
183 ucose-based peptidomimetics of somatostatin (SRIF-14), we sought to improve the water solubility of o
185 ness to the inhibitory peptide somatostatin (SRIF) or its clinically used analogs can desensitize wit
189 We therefore tested SSTR subtype-specific SRIF analogs in primary human fetal pituitary cultures (
192 Several lines of evidence indicate that SRIF is important in nociceptive processing: (1) it is l
193 Taken together, these data indicate that SRIF-immunoreactive neurons of the rabbit retina are dis
197 to synthesize peptidomimetics that bind the SRIF receptors on AtT-20 mouse pituitary cells, five clo
199 DA amacrine cells and M1 ipRGCs express the SRIF receptor subtypes sst(2A) and sst4 respectively.
202 endent manner, intraplantar injection of the SRIF receptor antagonist cyclo-somatostatin (c-SOM) resu
203 h both bind G-protein-coupled receptors, the SRIF receptors (SSTR 1-5) recognize SRIF and related pep
204 a i3 antibody injection, suggesting that the SRIF response is mediated through G alpha i1 and/or G al
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