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Image Search Results
Journal:
Article Title: CGRP receptors mediating CGRP-, adrenomedullin- and amylin-induced relaxation in porcine coronary arteries. Characterization with 'Compound 1' (WO98/11128), a non-peptide antagonist
doi: 10.1038/sj.bjp.0704210
Figure Lengend Snippet: αCGRP, βCGRP, AM and amylin concentration-reponse relationship in porcine coronary arteries. Points represent mean values and vertical lines indicate s.e.mean. Relative responses are given as percentage fraction of the initial vessel response to U46619 (10−7 M) just before they were challenged with the relaxant peptides.
Article Snippet: Human αCGRP, βCGRP, AM, amylin and the
Techniques: Concentration Assay
Journal:
Article Title: CGRP receptors mediating CGRP-, adrenomedullin- and amylin-induced relaxation in porcine coronary arteries. Characterization with 'Compound 1' (WO98/11128), a non-peptide antagonist
doi: 10.1038/sj.bjp.0704210
Figure Lengend Snippet: (a–d) Vasorelaxant effect of αCGRP (10−10–10−7 M) and βCGRP (10−10–10−7 M) in the porcine LAD contracted with U46619 (10−7 M). The antagonists αCGRP8–37 (10−7–10−5 M), βCGRP8–37 (10−7–10−5 M) were added 15 min and U46619 10 min prior to the αCGRP/βCGRP challenge. Points represent mean values and vertical lines indicate s.e.mean. Relative responses are given as percentage fraction of the initial vessel response to U46619 (10−7 M) just before they were challenged with αCGRP/βCGRP.
Article Snippet: Human αCGRP, βCGRP, AM, amylin and the
Techniques:
Journal:
Article Title: CGRP receptors mediating CGRP-, adrenomedullin- and amylin-induced relaxation in porcine coronary arteries. Characterization with 'Compound 1' (WO98/11128), a non-peptide antagonist
doi: 10.1038/sj.bjp.0704210
Figure Lengend Snippet: Schild plots for αCGRP8–37 and βCGRP8–37 tested with human αCGRP and βCGRP as agonists in isolated porcine LAD. The Schild plot curve for αCGRP8–37 (10−7–10−5 M) tested with αCGRP was equal to 1.48× +10.3 (r=0.62; P=0.0011). The pA2 value=7.0 (6.4–8.6). The Schild plot curve for αCGRP8–37 (10−7–10−5 M) tested with βCGRP was equal to 1.23× +7.8 (r=0.63; P=0.0007). The pA2 value=6.9 (6.2–8.7). The Schild plot curve for βCGRP8–37 (10−7–10−5 M) tested with αCGRP was equal to 1.05× +7.2 (r=0.61; P=0.0031). The pA2 value=6.3 (5.9–7.0). The Schild plot curve for βCGRP8–37 (10−6–10−5 M) tested with βCGRP was equal to 1.68× +10.0 (r=0.65; P=0.0002). The pA2 value=5.9 (5.7–6.5). Each point represents mean values and vertical lines indicate s.e.mean.
Article Snippet: Human αCGRP, βCGRP, AM, amylin and the
Techniques: Isolation
Journal:
Article Title: CGRP receptors mediating CGRP-, adrenomedullin- and amylin-induced relaxation in porcine coronary arteries. Characterization with 'Compound 1' (WO98/11128), a non-peptide antagonist
doi: 10.1038/sj.bjp.0704210
Figure Lengend Snippet: Vasorelaxant effect of AM in the porcine LAD contracted with U46619 (10−7 M). The proposed antagonists αCGRP8–37 (10−6 M), βCGRP8–37 (10−6 M) and AM22–52 (10−6 M) were added 15 min and U46619 10 min prior to the αCGRP (10−9–10−6 M) challenge. Points represent mean values and vertical lines indicate s.e.mean. Relative responses are given as percentage fraction of the initial vessel response to U46619 (10−7 M) just before they were challenged with AM.
Article Snippet: Human αCGRP, βCGRP, AM, amylin and the
Techniques:
Journal:
Article Title: CGRP receptors mediating CGRP-, adrenomedullin- and amylin-induced relaxation in porcine coronary arteries. Characterization with 'Compound 1' (WO98/11128), a non-peptide antagonist
doi: 10.1038/sj.bjp.0704210
Figure Lengend Snippet: Vasorelaxant effect of amylin in the porcine LAD contracted with U46619 (10−7 M). The proposed antagonists αCGRP8–37 (10−6 M), βCGRP8–37 (10−6 M) and AM22–52 (10−6 M) were added 15 min and U46619 10 min prior to the αCGRP (10−9–10−6 M) challenge. Points represent mean values and vertical lines indicate s.e.mean. Relative responses are given as percentage fraction of the initial vessel response to U46619 (10−7 M) just before they were challenged with amylin.
Article Snippet: Human αCGRP, βCGRP, AM, amylin and the
Techniques:
Journal:
Article Title: CGRP receptors mediating CGRP-, adrenomedullin- and amylin-induced relaxation in porcine coronary arteries. Characterization with 'Compound 1' (WO98/11128), a non-peptide antagonist
doi: 10.1038/sj.bjp.0704210
Figure Lengend Snippet: (a,b) Vasorelaxant effect of αCGRP (10−10–10−7 M) and βCGRP (10−10–10−7 M) in the porcine LAD contracted with U46619 (10−7 M). The antagonist AM22–52 (10−6 M) was added 15 min and U46619 10 min prior to the αCGRP/βCGRP challenge. Points represent mean values and vertical lines indicate s.e.mean. Relative responses are given as percentage fraction of the initial vessel response to U46619 (10−7 M) just before they were challenged with αCGRP/βCGRP.
Article Snippet: Human αCGRP, βCGRP, AM, amylin and the
Techniques:
Journal:
Article Title: CGRP receptors mediating CGRP-, adrenomedullin- and amylin-induced relaxation in porcine coronary arteries. Characterization with 'Compound 1' (WO98/11128), a non-peptide antagonist
doi: 10.1038/sj.bjp.0704210
Figure Lengend Snippet: Vasorelaxant effect of αCGRP in the porcine LAD contracted with U46619 (10−7 M). The non-peptide CGRP antagonist ‘Compound 1' (10−7–10−5 M) was added 15 min and U46619 10 min prior to the αCGRP (10−10–10−7 M) challenge. Points represent mean values and vertical lines indicate s.e.mean. Relative responses are given as percentage fraction of the initial vessel response to U46619 (10−7 M) just before they were challenged with αCGRP.
Article Snippet: Human αCGRP, βCGRP, AM, amylin and the
Techniques:
Journal:
Article Title: CGRP receptors mediating CGRP-, adrenomedullin- and amylin-induced relaxation in porcine coronary arteries. Characterization with 'Compound 1' (WO98/11128), a non-peptide antagonist
doi: 10.1038/sj.bjp.0704210
Figure Lengend Snippet: αCGRP, βCGRP, AM and amylin concentration-reponse relationship in porcine coronary arteries. Points represent mean values and vertical lines indicate s.e.mean. Relative responses are given as percentage fraction of the initial vessel response to U46619 (10−7 M) just before they were challenged with the relaxant peptides.
Article Snippet: Drugs Human αCGRP, βCGRP, AM, amylin and the fragments αCGRP 8–37 ,
Techniques: Concentration Assay
Journal:
Article Title: CGRP receptors mediating CGRP-, adrenomedullin- and amylin-induced relaxation in porcine coronary arteries. Characterization with 'Compound 1' (WO98/11128), a non-peptide antagonist
doi: 10.1038/sj.bjp.0704210
Figure Lengend Snippet: (a–d) Vasorelaxant effect of αCGRP (10−10–10−7 M) and βCGRP (10−10–10−7 M) in the porcine LAD contracted with U46619 (10−7 M). The antagonists αCGRP8–37 (10−7–10−5 M), βCGRP8–37 (10−7–10−5 M) were added 15 min and U46619 10 min prior to the αCGRP/βCGRP challenge. Points represent mean values and vertical lines indicate s.e.mean. Relative responses are given as percentage fraction of the initial vessel response to U46619 (10−7 M) just before they were challenged with αCGRP/βCGRP.
Article Snippet: Drugs Human αCGRP, βCGRP, AM, amylin and the fragments αCGRP 8–37 ,
Techniques:
Journal:
Article Title: CGRP receptors mediating CGRP-, adrenomedullin- and amylin-induced relaxation in porcine coronary arteries. Characterization with 'Compound 1' (WO98/11128), a non-peptide antagonist
doi: 10.1038/sj.bjp.0704210
Figure Lengend Snippet: Schild plots for αCGRP8–37 and βCGRP8–37 tested with human αCGRP and βCGRP as agonists in isolated porcine LAD. The Schild plot curve for αCGRP8–37 (10−7–10−5 M) tested with αCGRP was equal to 1.48× +10.3 (r=0.62; P=0.0011). The pA2 value=7.0 (6.4–8.6). The Schild plot curve for αCGRP8–37 (10−7–10−5 M) tested with βCGRP was equal to 1.23× +7.8 (r=0.63; P=0.0007). The pA2 value=6.9 (6.2–8.7). The Schild plot curve for βCGRP8–37 (10−7–10−5 M) tested with αCGRP was equal to 1.05× +7.2 (r=0.61; P=0.0031). The pA2 value=6.3 (5.9–7.0). The Schild plot curve for βCGRP8–37 (10−6–10−5 M) tested with βCGRP was equal to 1.68× +10.0 (r=0.65; P=0.0002). The pA2 value=5.9 (5.7–6.5). Each point represents mean values and vertical lines indicate s.e.mean.
Article Snippet: Drugs Human αCGRP, βCGRP, AM, amylin and the fragments αCGRP 8–37 ,
Techniques: Isolation
Journal:
Article Title: CGRP receptors mediating CGRP-, adrenomedullin- and amylin-induced relaxation in porcine coronary arteries. Characterization with 'Compound 1' (WO98/11128), a non-peptide antagonist
doi: 10.1038/sj.bjp.0704210
Figure Lengend Snippet: (a,b) Vasorelaxant effect of αCGRP (10−10–10−7 M) and βCGRP (10−10–10−7 M) in the porcine LAD contracted with U46619 (10−7 M). The antagonist AM22–52 (10−6 M) was added 15 min and U46619 10 min prior to the αCGRP/βCGRP challenge. Points represent mean values and vertical lines indicate s.e.mean. Relative responses are given as percentage fraction of the initial vessel response to U46619 (10−7 M) just before they were challenged with αCGRP/βCGRP.
Article Snippet: Drugs Human αCGRP, βCGRP, AM, amylin and the fragments αCGRP 8–37 ,
Techniques:
Journal:
Article Title: CGRP receptors mediating CGRP-, adrenomedullin- and amylin-induced relaxation in porcine coronary arteries. Characterization with 'Compound 1' (WO98/11128), a non-peptide antagonist
doi: 10.1038/sj.bjp.0704210
Figure Lengend Snippet: Vasorelaxant effect of αCGRP in the porcine LAD contracted with U46619 (10−7 M). The non-peptide CGRP antagonist ‘Compound 1' (10−7–10−5 M) was added 15 min and U46619 10 min prior to the αCGRP (10−10–10−7 M) challenge. Points represent mean values and vertical lines indicate s.e.mean. Relative responses are given as percentage fraction of the initial vessel response to U46619 (10−7 M) just before they were challenged with αCGRP.
Article Snippet: Drugs Human αCGRP, βCGRP, AM, amylin and the fragments αCGRP 8–37 ,
Techniques:
Journal:
Article Title: CGRP receptors mediating CGRP-, adrenomedullin- and amylin-induced relaxation in porcine coronary arteries. Characterization with 'Compound 1' (WO98/11128), a non-peptide antagonist
doi: 10.1038/sj.bjp.0704210
Figure Lengend Snippet: αCGRP, βCGRP, AM and amylin concentration-reponse relationship in porcine coronary arteries. Points represent mean values and vertical lines indicate s.e.mean. Relative responses are given as percentage fraction of the initial vessel response to U46619 (10−7 M) just before they were challenged with the relaxant peptides.
Article Snippet:
Techniques: Concentration Assay
Journal:
Article Title: CGRP receptors mediating CGRP-, adrenomedullin- and amylin-induced relaxation in porcine coronary arteries. Characterization with 'Compound 1' (WO98/11128), a non-peptide antagonist
doi: 10.1038/sj.bjp.0704210
Figure Lengend Snippet: (a–d) Vasorelaxant effect of αCGRP (10−10–10−7 M) and βCGRP (10−10–10−7 M) in the porcine LAD contracted with U46619 (10−7 M). The antagonists αCGRP8–37 (10−7–10−5 M), βCGRP8–37 (10−7–10−5 M) were added 15 min and U46619 10 min prior to the αCGRP/βCGRP challenge. Points represent mean values and vertical lines indicate s.e.mean. Relative responses are given as percentage fraction of the initial vessel response to U46619 (10−7 M) just before they were challenged with αCGRP/βCGRP.
Article Snippet:
Techniques:
Journal:
Article Title: CGRP receptors mediating CGRP-, adrenomedullin- and amylin-induced relaxation in porcine coronary arteries. Characterization with 'Compound 1' (WO98/11128), a non-peptide antagonist
doi: 10.1038/sj.bjp.0704210
Figure Lengend Snippet: Schild plots for αCGRP8–37 and βCGRP8–37 tested with human αCGRP and βCGRP as agonists in isolated porcine LAD. The Schild plot curve for αCGRP8–37 (10−7–10−5 M) tested with αCGRP was equal to 1.48× +10.3 (r=0.62; P=0.0011). The pA2 value=7.0 (6.4–8.6). The Schild plot curve for αCGRP8–37 (10−7–10−5 M) tested with βCGRP was equal to 1.23× +7.8 (r=0.63; P=0.0007). The pA2 value=6.9 (6.2–8.7). The Schild plot curve for βCGRP8–37 (10−7–10−5 M) tested with αCGRP was equal to 1.05× +7.2 (r=0.61; P=0.0031). The pA2 value=6.3 (5.9–7.0). The Schild plot curve for βCGRP8–37 (10−6–10−5 M) tested with βCGRP was equal to 1.68× +10.0 (r=0.65; P=0.0002). The pA2 value=5.9 (5.7–6.5). Each point represents mean values and vertical lines indicate s.e.mean.
Article Snippet:
Techniques: Isolation
Journal:
Article Title: CGRP receptors mediating CGRP-, adrenomedullin- and amylin-induced relaxation in porcine coronary arteries. Characterization with 'Compound 1' (WO98/11128), a non-peptide antagonist
doi: 10.1038/sj.bjp.0704210
Figure Lengend Snippet: (a,b) Vasorelaxant effect of αCGRP (10−10–10−7 M) and βCGRP (10−10–10−7 M) in the porcine LAD contracted with U46619 (10−7 M). The antagonist AM22–52 (10−6 M) was added 15 min and U46619 10 min prior to the αCGRP/βCGRP challenge. Points represent mean values and vertical lines indicate s.e.mean. Relative responses are given as percentage fraction of the initial vessel response to U46619 (10−7 M) just before they were challenged with αCGRP/βCGRP.
Article Snippet:
Techniques:
Journal: Headache
Article Title: Development and pharmacological characterization of novel multi‐ calcitonin gene‐related peptide and pituitary adenylate cyclase‐activating peptide receptor antagonists
doi: 10.1111/head.14916
Figure Lengend Snippet: Schematic of novel multi‐receptor CGRP‐ and PACAP‐responsive receptor antagonists. CGRP 8‐37 and PACAP 6‐38 were joined at different linker positions (highlighted in red) through 1,3‐dipolar cycloaddition. The chemical linker used to join the three antagonists is shown between residues 21 G of CGRP 8‐37 and 21 K of PACAP 6‐38 . The covalent linkage of CGRP 8‐37 to PACAP 6‐38 at amino acids 21, 34, and 38 were named DA1, DA2, and DA3, respectively. CGRP, calcitonin gene‐related peptide; PACAP, pituitary adenylate cyclase‐activating polypeptide. [Colour figure can be viewed at wileyonlinelibrary.com ]
Article Snippet: Native human and rat αCGRP, human PACAP‐38, PACAP‐27, VIP, and CGRP 8‐37 were synthesized in‐house as previously described.,
Techniques:
Journal: Headache
Article Title: Development and pharmacological characterization of novel multi‐ calcitonin gene‐related peptide and pituitary adenylate cyclase‐activating peptide receptor antagonists
doi: 10.1111/head.14916
Figure Lengend Snippet: DA1 blocked PACAP‐27 and VIP but not PACAP‐38‐stimulated receptor signaling in transfected Cos7 cells. Data were normalized to the maximal cAMP accumulation produced by PACAP‐38, PACAP‐27, or VIP at each receptor and expressed as a percentage. Data points are the mean ± standard error of the mean from three (PACAP‐38 at all receptors, all agonists at VPAC 1 ) or five independent experiments. cAMP, cyclic adenosine monophosphate; PACAP, pituitary adenylate cyclase‐activating polypeptide; VIP, vasoactive intestinal peptide. [Colour figure can be viewed at wileyonlinelibrary.com ]
Article Snippet: Native human and rat αCGRP, human PACAP‐38, PACAP‐27, VIP, and CGRP 8‐37 were synthesized in‐house as previously described.,
Techniques: Transfection, Produced
Journal: Headache
Article Title: Development and pharmacological characterization of novel multi‐ calcitonin gene‐related peptide and pituitary adenylate cyclase‐activating peptide receptor antagonists
doi: 10.1111/head.14916
Figure Lengend Snippet: DA2 blocked PACAP‐27 and VIP but not PACAP‐38‐stimulated receptor signaling in transfected Cos7 cells. Data were normalized to the maximal cAMP accumulation produced by PACAP‐38, PACAP‐27, or VIP at each receptor and expressed as a percentage. Data points are the mean ± standard error of the mean from three (PACAP‐38 at all receptors, all agonists at VPAC 1 ) or five independent experiments. cAMP, cyclic adenosine monophosphate; PACAP, pituitary adenylate cyclase‐activating polypeptide; VIP, vasoactive intestinal peptide. [Colour figure can be viewed at wileyonlinelibrary.com ]
Article Snippet: Native human and rat αCGRP, human PACAP‐38, PACAP‐27, VIP, and CGRP 8‐37 were synthesized in‐house as previously described.,
Techniques: Transfection, Produced
Journal: Headache
Article Title: Development and pharmacological characterization of novel multi‐ calcitonin gene‐related peptide and pituitary adenylate cyclase‐activating peptide receptor antagonists
doi: 10.1111/head.14916
Figure Lengend Snippet: DA3 blocked PACAP‐27 and VIP but not PACAP‐38‐stimulated receptor signaling in transfected Cos7 cells. Data were normalized to the maximal cAMP accumulation produced by PACAP‐38, PACAP‐27 or VIP at each receptor and expressed as a percentage. Data points are the mean ± standard error of the mean from three (PACAP‐38 at all receptors, all agonists at VPAC 1 ) or five independent experiments. cAMP, cyclic adenosine monophosphate; PACAP, pituitary adenylate cyclase‐activating polypeptide; VIP, vasoactive intestinal peptide. [Colour figure can be viewed at wileyonlinelibrary.com ]
Article Snippet: Native human and rat αCGRP, human PACAP‐38, PACAP‐27, VIP, and CGRP 8‐37 were synthesized in‐house as previously described.,
Techniques: Transfection, Produced
43 * p < 0.05 compared to unlinked PACAP 6‐38 with the same agonist by unpaired Student's t ‐test or one‐way ANOVA with Dunnett's test. PACAP, pituitary adenylate cyclase‐activating polypeptide; VIP, vasoactive intestinal peptide. " width="100%" height="100%">
Journal: Headache
Article Title: Development and pharmacological characterization of novel multi‐ calcitonin gene‐related peptide and pituitary adenylate cyclase‐activating peptide receptor antagonists
doi: 10.1111/head.14916
Figure Lengend Snippet: Similar to PACAP 6‐38 , multi‐receptor antagonists potently blocked PACAP‐27 and VIP but not PACAP‐38‐stimulated receptor signaling at PAC and VPAC 2 receptors in transfected Cos7 cells. Heat maps show the mean potency (A 2 /K B in nM) of responses that could be quantified from three to five independent experiments (Table ). PACAP 6‐38 K B values are taken from Tasma et al.
Article Snippet: Native human and rat αCGRP, human PACAP‐38, PACAP‐27, VIP, and CGRP 8‐37 were synthesized in‐house as previously described.,
Techniques: Transfection
Journal: Headache
Article Title: Development and pharmacological characterization of novel multi‐ calcitonin gene‐related peptide and pituitary adenylate cyclase‐activating peptide receptor antagonists
doi: 10.1111/head.14916
Figure Lengend Snippet: Multi‐receptor antagonists blocked CGRP‐ and PACAP‐responsive receptor signaling in rat dissociated spinal cord cell cultures. Data were normalized to the maximal cAMP accumulation produced by CGRP, PACAP‐38, PACAP‐27, or VIP and expressed as a percentage. Data points are the mean ± standard error of the mean of five independent experiments. cAMP, cyclic adenosine monophosphate; CGRP, calcitonin gene‐related peptide; PACAP, pituitary adenylate cyclase‐activating polypeptide; VIP, vasoactive intestinal peptide. [Colour figure can be viewed at wileyonlinelibrary.com ]
Article Snippet: Native human and rat αCGRP, human PACAP‐38, PACAP‐27, VIP, and CGRP 8‐37 were synthesized in‐house as previously described.,
Techniques: Produced
43 * p < 0.05 compared to PACAP 6‐38 with the same agonist by one‐way ANOVA with Dunnett's test using the log pA 2 /pK B values. CGRP, calcitonin gene‐related peptide; PACAP, pituitary adenylate cyclase‐activating polypeptide. " width="100%" height="100%">
Journal: Headache
Article Title: Development and pharmacological characterization of novel multi‐ calcitonin gene‐related peptide and pituitary adenylate cyclase‐activating peptide receptor antagonists
doi: 10.1111/head.14916
Figure Lengend Snippet: Similar to their parental CGRP 8‐37 and PACAP 6‐38 , multi‐receptor antagonists blocked CGRP‐ and PACAP‐responsive receptor signaling in rat dissociated spinal cord cell cultures. Data are the mean potency (A 2 K B in nM) of five independent experiments (Table in Data S1). PACAP 6‐38 K B values were originally derived from Tasma et al.
Article Snippet: Native human and rat αCGRP, human PACAP‐38, PACAP‐27, VIP, and CGRP 8‐37 were synthesized in‐house as previously described.,
Techniques: Derivative Assay