Disease relevance of GR-73632

• Injections of the selective neurokinin-1 (NK-1) receptor agonist drug GR-73632 also caused bradycardia, however the rapid onset of agonist induced desensitization prevented an evaluation of potential effects on AV conduction in the iNA-VL [1].

High impact information on GR-73632

• Ava[L-Pro9,N-MeLeu10] substance P(7-11) (GR 73632) and Sar9, Met(O2)11 increase distention-induced peristalsis through activation of neurokinin-1 receptors on smooth muscle and interstitial cells of cajal [2].
• Activation of NK1 receptors by Ava[l-Pro(9),N-MeLeu10] substance P(7-11) (GR 73632) and Sar(9), Met(O(2))(11) on smooth muscle cells resulted in prolongation of the activity periods and increased action potential generation occurring superimposed on the intestinal slow wave activity [2].
• In vivo central administration of HK-1 to gerbils and mice induced foot-tapping and scratching behaviors, respectively, similar to those observed following central administration of SP or the NK1 receptor agonist, GR-73632 [3].
• In the prostatic urethra the rank order of agonist potency was GR 64349 > NKA-(4-10) > SP > GR 73632, whereas in the prostate it was: GR 64349 >> [beta Ala8 (NKA-(4-10)] > NKA-(4-10) > SP; GR 73632 was ineffective up to 30 microM [4].
• Only the hyperpolarizing effects, which were in contrast mimicked by the specific NK1 receptor agonists GR 73632 and [Sar9, Met (O2)11]-SP, would be mediated by the few typical NK1 receptors which have been demonstrated in the medial vestibular nucleus [5].

Biological context of GR-73632

• GR-73632 only slightly increased renal nerve firing and heart rate and lowered blood pressure in WKYs [6].

Anatomical context of GR-73632

• Moreover, TAK-637 reduced the TTX-resistant component of the response to GR-73632 suggesting that NK(1) receptors expressed by epithelial cells are inhibited by TAK-637 [7].
• ICV administration of 4.2 pmol of GR-73632 produced a rapid onset and sustained rCBV increase in several brain structures, such as the amygdala, the caudate putamen and the cortex [8].

Associations of GR-73632 with other chemical compounds

• The other NK1 receptor agonists used, GR 73632, [Pro9]SP and septide, which did not interfere with the RIA, increased SP-LI basal outflow by 1807 +/- 713% (n = 3), 1259 +/- 160% (n = 3) and 620 +/- 69% (n = 3) at 10 nM, 1 nM and 1 microM, respectively.(ABSTRACT TRUNCATED AT 250 WORDS)[9]
• Furthermore, GR 73632-induced hind paw tapping was significantly attenuated by co-administration of the peptide tachykinin NK1 receptor antagonist, GR 82334, or intravenous injection of CP-99,994 [10].

Gene context of GR-73632

• The in vivo pharmacological profiles of the selective tachykinin NK1 receptor agonists, [Sar9,Met(O2)11]substance P and GR 73632, were examined in gerbils [10].
• Moreover, GR 73632 increased the efflus of SP to a greater extent in the absence of peptidase inhibitors [11].

Analytical, diagnostic and therapeutic context of GR-73632

• Microinjections of 16 or 12 nmol/0.25 microl of the NK(1) agonist, GR 73632, resulted in facilitation of defensive rage [12].

References